Protein Information

Name Potassium channel (protein family or complex)
Synonyms Potassium channel

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
10725353 Millar JA, Barratt L, Southan AP, Page KM, Fyffe RE, Robertson B, Mathie A: A functional role for the two-pore domain potassium channel TASK-1 in cerebellar granule neurons. Proc Natl Acad Sci U S A. 2000 Mar 28;97(7):3614-8.

IK (SO) is blocked by Ba (2+) ions and is regulated by activation of muscarinic M (3) receptors, but it is insensitive to the classical broad-spectrum potassium channel blocking drugs 4-aminopyridine and tetraethylammonium ions.
84(1,1,1,4) Details
14594030 Fu ZJ, Cheng HW, Zhang LF, Ma J, Zhang LN, Ma XW: [Changes of potassium channel activity of hindlimb arterial smooth muscle cells in tail-suspended rats]. Space Med Med Eng. 2003 Aug;16(4):253-6.

METHOD: The contractile responsiveness of femoral arterial rings of 1-wk and 4-wk tail-suspended rats to potassium channel blockers, tetraethylammonium chloride (TEA) and 4-aminopyridine (4-AP), were recorded, and the currents of large conductance calcium-dependent potassium channel (BK (Ca)) and voltage activated potassium channel (Kv) of vascular smooth muscle cells (VSMCs) in saphenous arteries from 1-wk tail-suspended rats were recorded using the whole cell recording mode of patch clamp technique.
83(1,1,1,3) Details
20179886 Song SL, Wei CL, Gu HG, Liu ZQ, Ren W: [The modulation of 4-aminopyridine sensitive potassium channel to bifurcation scenario of the spontaneous neural firing rhythms.]. Sheng Li Xue Bao. 2010 Feb 25;62(1):35-41.
81(1,1,1,1) Details
19657079 Deng P, Pang ZP, Lei Z, Xu ZC: Excitatory roles of protein kinase C in striatal cholinergic interneurons. J Neurophysiol. 2009 Oct;102(4):2453-61. Epub 2009 Aug 5.

These excitatory effects of PKC could be partially mimicked and occluded by blockade of I (A) with potassium channel blocker 4-aminopyridine.
31(0,1,1,1) Details
16641238 Hanus C, Ehrensperger MV, Triller A: Activity-dependent movements of postsynaptic scaffolds at inhibitory synapses. J Neurosci. 2006 Apr 26;26(17):4586-95.

Moreover, the action of the potassium channel blocker 4-aminopyridine and receptor antagonists indicate that the dynamics of postsynaptic gephyrin scaffolds are controlled by synaptic activity.
31(0,1,1,1) Details
19922891 Vollmer T, Henney HR 3rd: Pharmacokinetics and tolerability of single escalating doses of fampridine sustained-release tablets in patients with multiple sclerosis: a Phase I-II, open-label trial. Clin Ther. 2009 Oct;31(10):2206-14.

BACKGROUND: Fampridine (4-aminopyridine) is a potassium channel-blocking agent that has been reported to have therapeutic potential for improving walking and mobility in patients with multiple sclerosis (MS).
31(0,1,1,1) Details
11431490 Nunemaker CS, DeFazio RA, Geusz ME, Herzog ED, Pitts GR, Moenter SM: Long-term recordings of networks of immortalized GnRH neurons reveal episodic patterns of electrical activity. J Neurophysiol. 2001 Jul;86(1):86-93.

The A-type potassium-channel antagonist 4-aminopyridine (1 mM) increased both firing rate and GnRH secretion, demonstrating the presence of A-type currents in these cells and supporting the hypothesis that electrical activity is associated with GnRH release.
31(0,1,1,1) Details
12853442 Jensen JM, Shi R: Effects of 4-aminopyridine on stretched mammalian spinal cord: the role of potassium channels in axonal conduction. J Neurophysiol. 2003 Oct;90(4):2334-40. Epub 2003 Jul 9.

Axonal conduction deficit is a major contributor to various degrees of disability after spinal cord injury. 4-aminopyridine (4-AP), a potassium channel blocker, has been shown to restore some conduction and improve neurological function in both animal and human studies.
31(0,1,1,1) Details
19061970 Montes FR, Cabrera M, Delgadillo A, Salgar C, Echeverri D: The role of potassium channels in the vasodilatory effect of caffeine in human internal mammary arteries. Vascul Pharmacol. 2009 Mar-Apr;50(3-4):132-6. Epub 2008 Nov 24.

The response to caffeine was also evaluated after incubation with adenosine 3',5'-triphosphate (ATP)-dependent potassium channel blocker glibenclamide, voltage-dependent potassium channel blocker 4-aminopyridine and large-conductance calcium-activated potassium channel inhibitor tetraethylammonium.
31(0,1,1,1) Details
19171133 Yaktubay Dondas N, Karatas Y, Kaya D, Soylu N, Singirik E, Baysal F: Molecular mechanism of KCl-induced relaxation of the esophagus. . Eur J Pharmacol. 2009 Mar 1;605(1-3):123-8. Epub 2009 Jan 10.

Similarly, potassium channel blockers such as 4-aminopyridine (4-AP; 100 microM) and tetraethylammonium (TEA; 100 microM) caused a significant inhibition on relaxations to KCl.
31(0,1,1,1) Details
17437050 Yan N, Li XH, Cheng Q, Yan J, Ni X, Sun JH: [Decreased A-type potassium current mediates the hyperexcitability of nociceptive neurons in the chronically compressed dorsal root ganglia]. Sheng Li Xue Bao. 2007 Apr 25;59(2):240-6.

We examined the effects of 4-aminopyridine (4-AP), a specific antagonist of A-type potassium channel, on the excitability of the control DRG neurons.
81(1,1,1,1) Details
17041732 Pi YL, Ma JH, Zhang PH, Duan JJ: [Calcium-dependent chloride channels in plasma membrane of oocytes from toad, Bufo bufo gargarizans]. Sheng Li Xue Bao. 2006 Oct 25;58(5):471-6.

Potassium channel blockers (tetraethylammonium chloride, TEA, 10 mmol/L and 4-aminopyridine, 4-AP, 10 mmol/L) reduced the outward current to (23.4+/-0.72)% of the maximum.
31(0,1,1,1) Details
14506322 Magdalan J: New treatment methods in verapamil poisoning: experimental studies. Pol J Pharmacol. 2003 May-Jun;55(3):425-32.

The aim of this study was to evaluate the effectiveness of the treatment with 4-aminopyridine (4-AP, potassium channel inhibitor) and Bay K 8644 (calcium channel activator) in experimentally evoked verapamil poisoning in rats and to compare the results of this treatment with the effectiveness of widely accepted methods (adrenaline, calcium compounds).
31(0,1,1,1) Details
17592231 Bagcivan I, Gursoy S, Yildirim MK, Kaya Temiz T, Yildirim S, Yilmaz A, Turan M: Investigation of relaxant effects of propofol on sheep sphincter of Oddi. . Pancreatology. 2007;7(2-3):174-9. Epub 2007 Jun 21.

METHODS: SO rings were mounted in a tissue bath and tested for changes in isometric tension in response to propofol (10 (-8)-10 (-4) M) in the presence or absence of L-NAME (3 x 10 (-5) M), a non-specific inhibitor of nitric oxide (NO) synthase; indomethacin (10 (-5) M), an inhibitor of cyclooxygenase; glibenclamide (10 (-5) M), an inhibitor of ATP-sensitive potassium channels; tetraethylammonium (3 x 10 (-4) M), inhibitors of calcium-activated potassium channels; 4-aminopyridine (10 (-3) M), a voltage-dependent potassium channel blocker.
31(0,1,1,1) Details
11102477 Ango F, Pin JP, Tu JC, Xiao B, Worley PF, Bockaert J, Fagni L: Dendritic and axonal targeting of type 5 metabotropic glutamate receptor is regulated by homer1 proteins and neuronal excitation. J Neurosci. 2000 Dec 1;20(23):8710-6.

Depolarization of the neurons with a mixture of ionotropic glutamate receptor agonists, NMDA and kainate, or potassium channel blockers, tetraethylammonium and 4-aminopyridine, induced transient expression of endogenous Homer1a and persistent neuritic localization of transfected mGluR5 even long after degradation of Homer1a.
31(0,1,1,1) Details
17624584 Nacitarhan C, Bayram Z, Eksert B, Usta C, Golbasi I, Ozdem SS: The effect of hydrogen peroxide in human internal thoracic arteries: role of potassium channels, nitric oxide and cyclooxygenase products. Cardiovasc Drugs Ther. 2007 Aug;21(4):257-62.

Incubation of endothelium-intact or endothelium-denuded human ITA rings with voltage-dependent potassium channel blocker 4-aminopyridine (5 mM) significantly inhibited the relaxant responses to H (2) O (2).
31(0,1,1,1) Details
17673572 Juvin V, Penna A, Chemin J, Lin YL, Rassendren FA: Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate. Mol Pharmacol. 2007 Nov;72(5):1258-68. Epub 2007 Aug 2.

Besides the classic TRP inhibitors ruthenium red (RR) and 1-(beta-[3-(4-methoxyphenyl) propoxy]-4-methoxyphenethyl)-1H-imidazole hydrochloride (SKF96365), two potassium channel blockers, tetraethylammonium (TEA) and 4-aminopyridine, and an inhibitor of capacitative calcium entry, 1-(2-(trifluoromethyl) phenyl) imidazole (TRIM), were found to inhibit TRPV2 activation by 100 microM 2APB.
31(0,1,1,1) Details
17525359 Stojic D, Pesic S, Radenkovic M, Popovic-Roganovic J, Pesic Z, Grbovic L: Responses of the human submandibular artery to ACh and VIP. J Dent Res. 2007 Jun;86(6):565-70.

We evaluated the contributions of endothelial vasodilatory substances to vessel relaxation in response to ACh and VIP, using different inhibitors of endothelial vasodilation, the nitric oxide synthase inhibitor, the cyclo-oxygenase inhibitor, indomethacin, the potassium channel blocker, and 4-aminopyridine.
31(0,1,1,1) Details
15051158 Wang SJ, Wang KY, Wang WC: Mechanisms underlying the riluzole inhibition of glutamate release from rat cerebral cortex nerve terminals (synaptosomes). Neuroscience. 2004;125(1):191-201.

Riluzole inhibited the calcium-dependent release of glutamate that was evoked by exposing cerebrocortical synaptosomes to the potassium channel blocker 4-aminopyridine, and this presynaptic inhibition was concentration-dependent.
31(0,1,1,1) Details
10761168 Segal JL, Hayes KC, Brunnemann SR, Hsieh JT, Potter PJ, Pathak MS, Tierney DS, Mason D: Absorption characteristics of sustained-release 4-aminopyridine (fampridine SR) in patients with chronic spinal cord injury. J Clin Pharmacol. 2000 Apr;40(4):402-9.

Fampridine SR (4-aminopyridine) is a potassium channel-blocking drug currently being investigated for its therapeutic efficacy in ameliorating central conduction deficits due to demyelination in patients with spinal cord injury (SCI).
31(0,1,1,1) Details
16165285 Fatehi M, Kombian SB, Saleh TM: 17beta-estradiol inhibits outward potassium currents recorded in rat parabrachial nucleus cells in vitro. Neuroscience. 2005;135(4):1075-86. Epub 2005 Sep 13.

The 17beta-estradiol-induced inhibition of the outward current was blocked by pretreatment with the potassium channel blockers tetraethylammonium and 4-aminopyridine.
31(0,1,1,1) Details
17664175 Kalla R, Glasauer S, Buttner U, Brandt T, Strupp M: 4-aminopyridine restores vertical and horizontal neural integrator function in downbeat nystagmus. Brain. 2007 Sep;130(Pt 9):2441-51. Epub 2007 Jul 29.

Since cerebellar involvement is suspected to be the underlying pathomechanism of DBN, we tested in 15 patients with DBN whether the application of the potassium-channel blocker 4-aminopyridine (4-AP), which increases the excitability of cerebellar Purkinje cells as shown in animal experiments, reduces the vertical ocular drift leading to nystagmus.
31(0,1,1,1) Details
11746768 Lohr C, Oland LA, Tolbert LP: Olfactory receptor axons influence the development of glial potassium currents in the antennal lobe of the moth Manduca sexta. Glia. 2001 Dec;36(3):309-20.

At all developmental stages investigated, the outward currents were partly blocked by bath application of the potassium channel blocker 4-aminopyridine (4AP, 10 mM) or by including tetraethylammonium (TEA, 30 mM) in the pipette solution.
31(0,1,1,1) Details
11166687 Sperlagh B, Zsilla G, Vizi ES: K (ATP) channel blockers selectively interact with A (1)-adenosine receptor mediated modulation of acetylcholine release in the rat hippocampus. Brain Res. 2001 Jan 19;889(1-2):63-70.

Glibenclamide and glipizide (10-100 microM) completely prevented the inhibitory effect of 0.1 microM CHA and shifted the concentration response curve of CHA to the right. 4-Aminopyridine (10-100 microM), the non-selective potassium channel blocker, increased the evoked release of [3H] ACh, but in the presence of 4-aminopyridine, the inhibitory effect of CHA (0.1 microM) still persisted.
31(0,1,1,1) Details
11152736 Zhang YH, Kenyon JL, Nicol GD: Phorbol ester-induced inhibition of potassium currents in rat sensory neurons requires voltage-dependent entry of calcium. J Neurophysiol. 2001 Jan;85(1):362-73.

The potassium channel blockers tetraethylammonium (TEA, 10 mM) and 4-aminopyridine (4-AP, 3 mM and 30 microM) reduced I (K), but only TEA attenuated the ability of PDBu to further inhibit the current, suggesting that the I (K) modified by PDBu was sensitive to TEA.
31(0,1,1,1) Details
19443164 Schwam E: Severe accidental overdose of 4-aminopyridine due to a compounding pharmacy error. J Emerg Med. 2009 May 12.

Background: 4-Aminopyridine (4-AP) is a potassium channel-blocking drug used to ameliorate symptoms of multiple sclerosis and spinal cord injury by facilitating neural impulse conduction.
31(0,1,1,1) Details
12686577 Boller M, Schmidt M: GABAC receptors in the rat superior colliculus and pretectum participate in synaptic neurotransmission. J Neurophysiol. 2003 Apr;89(4):2035-45.

To increase the likelihood to record IPSCs we induced spontaneous activity by application of the potassium channel blocker 4-aminopyridine (4-AP) and blocked glutamate-mediated excitatory neurotransmission with kynurenic acid.
31(0,1,1,1) Details
15979855 Thuault SJ, Brown JT, Calver AR, Collingridge GL, Randall A, Davies CH: Mechanisms contributing to the exacerbated epileptiform activity in hippocampal slices expressing a C-terminal truncated GABA (B2) receptor subunit. Epilepsy Res. 2005 Jun;65(1-2):41-51.

Furthermore, synchronous GABA (A) receptor-mediated potentials recorded in the presence of the potassium channel blocker 4-aminopyridine (4-AP, 100muM) and the ionotropic glutamate receptor antagonists NBQX (20muM) and D-AP5 (50muM) were significantly prolonged in duration in DeltaGB2-Ct versus WT slices.
31(0,1,1,1) Details
12913062 Souza HC, Salgado HC, Ballejo G, Salgado MC: SR141716A-sensitive enhancement of ET-1 hypotensive effect by chronic NOS inhibition. Hypertension. 2003 Oct;42(4):802-5. Epub 2003 Aug 11.

The enhanced ET-1 hypotensive effect in L-NAME-treated rats was abolished by the ETB receptor antagonist BQ-788 but was unaltered by the cyclooxygenase inhibitor diclofenac, the cytochrome P450 inhibitor fluconazole, or the potassium channel blockers apamin, glibenclamide, tetraethylammonium, and 4-aminopyridine.
31(0,1,1,1) Details
12975592 Pataricza J, Krassoi I, Hohn J, Kun A, Papp JG: Functional role of potassium channels in the vasodilating mechanism of levosimendan in porcine isolated coronary artery. Cardiovasc Drugs Ther. 2003 Mar;17(2):115-21.

The interaction of levosimendan with the specific calcium-activated potassium channel (KCa) blocker, iberiotoxin (IBTX), and the voltage-sensitive potassium channel (KV) blocker, 4-aminopyridine (4-AP), was also studied.
31(0,1,1,1) Details
10634884 Solessio E, Linn DM, Perlman I, Lasater EM: Characterization with barium of potassium currents in turtle retinal Muller cells. J Neurophysiol. 2000 Jan;83(1):418-30.

These currents are insensitive to broadband potassium channel blockers, tetraethylammonium (TEA) and 4-aminopyridine (4-AP) and well blocked by barium.
31(0,1,1,1) Details
12126879 Gulyas-Kovacs A, Doczi J, Tarnawa I, Detari L, Banczerowski-Pelyhe I, Vilagi I: Comparison of spontaneous and evoked epileptiform activity in three in vitro epilepsy models. Brain Res. 2002 Aug 2;945(2):174-80.

Rat neocortical slices express spontaneous epileptiform activity after incubation with GABA (A) receptor blocker bicuculline (BIC, 20 microM), with potassium channel blocker 4-aminopyridine (4-AP, 50 microM) or in Mg (2+)-free medium (LMG).
31(0,1,1,1) Details
15592580 Hayes KC: The use of 4-aminopyridine (fampridine) in demyelinating disorders. . CNS Drug Rev. 2004 Winter;10(4):295-316.

4-Aminopyridine (4-AP or fampridine) is a potassium channel-blocking agent that has been shown to restore conduction in focally demyelinated axons.
31(0,1,1,1) Details
10832015 Chung J, Chang S, Kim Y, Shin H: Zinc increases the excitability of dopaminergic neurons in rat substantia nigra. Neurosci Lett. 2000 Jun 9;286(3):183-6.

Voltage-clamp studies showed that Zn (2+) decreased 4-aminopyridine-sensitive outward currents, suggesting that a transient A-like potassium channel be one of the major targets Zn (2+) can modulate in the SN neurons.
31(0,1,1,1) Details
19818752 de Matos Silva LF, de Paula Ramos ER, Ambiel CR, Correia-de-Sa P, Alves-Do-Prado W: Apamin reduces neuromuscular transmission by activating inhibitory muscarinic M (2) receptors on motor nerve terminals. Eur J Pharmacol. 2010 Jan 25;626(2-3):239-43. Epub 2009 Oct 8.

The effects of apamin were compared with those produced by another potassium channel blocker, 4-aminopyridine, on rat hemidiaphragm preparations stimulated at a 100 Hz frequency via the phrenic nerve.
6(0,0,1,1) Details
19966074 Smith W, Swan S, Marbury T, Henney H 3rd: Single-Dose pharmacokinetics of sustained-release fampridine (Fampridine-SR) in healthy volunteers and adults with renal impairment. J Clin Pharmacol. 2010 Feb;50(2):151-9. Epub 2009 Dec 4.

Fampridine-SR is a sustained-release formulation of fampridine (4-aminopyridine), a potassium channel blocker demonstrated to improve walking ability in patients with multiple sclerosis.
6(0,0,1,1) Details
12522206 Powers RK, Binder MD: Persistent sodium and calcium currents in rat hypoglossal motoneurons. J Neurophysiol. 2003 Jan;89(1):615-24.

In the presence of potassium channel blockers (internal cesium and external 4-aminopyridine and tetraethylammonium), net inward currents were present on both the rising and falling phases of the voltage-clamp command.
6(0,0,1,1) Details
16716270 Wang D, Schreurs BG: Characteristics of IA currents in adult rabbit cerebellar Purkinje cells. . Brain Res. 2006 Jun 22;1096(1):85-96. Epub 2006 May 23.

Classical conditioning the rabbit nictitating membrane involves changes in synaptic and intrinsic membrane properties of cerebellar Purkinje cell dendrites, and a 4-aminopyridine (4-AP)-sensitive potassium channel underlies these membrane properties.
6(0,0,1,1) Details
11463634 Loboda A, Armstrong CM: Resolving the gating charge movement associated with late transitions in K channel activation. Biophys J. 2001 Aug;81(2):905-16.

We examined the late transitions in the activation sequence of potassium channels by analyzing gating currents of mutant Shaker IR channels and using the potassium channel blocker 4-aminopyridine (4AP).
31(0,1,1,1) Details
12897638 Hayes KC, Potter PJ, Hansebout RR, Bugaresti JM, Hsieh JT, Nicosia S, Katz MA, Blight AR, Cohen R: Pharmacokinetic studies of single and multiple oral doses of fampridine-SR (sustained-release 4-aminopyridine) in patients with chronic spinal cord injury. Clin Neuropharmacol. 2003 Jul-Aug;26(4):185-92.

Fampridine (4-aminopyridine) is a potassium channel blocking agent that restores conduction in demyelinated axons and improves neurologic function in patients with chronic spinal cord injury (SCI).
31(0,1,1,1) Details
17416285 Grijalva I, Guizar-Sahagun G, Rodriguez-Pacheco D, Francisco-Arguelles C, Castaneda-Hernandez G, Palma-Aguirre JA: Gastric emptying effect by 4-aminopyridine in patients with chronic spinal cord injury. Arch Med Res. 2007 May;38(4):392-7. Epub 2007 Mar 12.

BACKGROUND: 4-Aminopyridine (4-AP) given to patients with chronic spinal cord injury (SCI) has shown beneficial effects in some somatic and autonomic functions, although patients often develop dyspeptic symptoms. 4-AP is a potassium-channel blocker capable of altering gastro-pyloric functions as demonstrated experimentally.
31(0,1,1,1) Details
18037462 Cheng YC, Wang JJ, Chang LS: B chain is a functional subunit of beta-bungarotoxin for inducing apoptotic death of human neuroblastoma SK-N-SH cells. Toxicon. 2008 Feb;51(2):304-15. Epub 2007 Oct 13.

MK801 (an NMDA receptor antagonist), antibodies against NMDA receptor and 4-aminopyridine (a potassium channel blocker) markedly reduced the cytotoxic effects of beta-Bgt, B chain and catalytically inactivated beta-Bgt.
31(0,1,1,1) Details
11934483 Shi R, Pryor JD: Pathological changes of isolated spinal cord axons in response to mechanical stretch. Neuroscience. 2002;110(4):765-77.

Three types of conduction blocks resulting from stretch injury were identified: an immediate, spontaneously reversible component, which may result from a transient increase in membrane permeability and consequent disturbance of ionic distribution; a second component that was irreversible within 30-60 min of recording, perhaps resulting from profound axolemmal disruption; and a third component, which may be due to perturbation of the myelin sheath, that was reversible with application of 100 microM of the potassium channel blocker, 4-aminopyridine.
31(0,1,1,1) Details
17164473 Ghatta S, Tunstall RR, Kareem S, Rahman M, O'Rourke ST: Sirolimus causes relaxation of human vascular smooth muscle: a novel action of sirolimus mediated via ATP-sensitive potassium channels. J Pharmacol Exp Ther. 2007 Mar;320(3):1204-8. Epub 2006 Dec 12.

In U46619-contracted rings, the response to sirolimus was markedly inhibited in the presence of the specific ATP-sensitive potassium (K (ATP)) channel blocker, glyburide (10 (-6) M), but was unaffected by treatment with blockers of large conductance, calcium-activated potassium channel (iberiotoxin, 10 (-7) M), small conductance, calcium-activated potassium channel (apamin, 10 (-6) M), or voltage-gated potassium channel (4-aminopyridine, 10 (-3) M).
31(0,1,1,1) Details
16677766 Laursen M, Rekling JC: The Edinger-Westphal nucleus of the juvenile rat contains transient- and repetitive-firing neurons. Neuroscience. 2006 Aug 11;141(1):191-200. Epub 2006 May 4.

Transient-firing neurons had an outward rectifying response inhibiting firing, possibly due to slowly inactivating I (D)-like potassium channels since low concentrations (200 microM) of the potassium channel blocker 4-aminopyridine elicited repetitive firing.
31(0,1,1,1) Details
14970964 Hayes KC, Potter PJ, Hsieh JT, Katz MA, Blight AR, Cohen R: Pharmacokinetics and safety of multiple oral doses of sustained-release 4-aminopyridine (Fampridine-SR) in subjects with chronic, incomplete spinal cord injury. Arch Phys Med Rehabil. 2004 Jan;85(1):29-34.

OBJECTIVE: To examine the pharmacokinetics and safety of sustained-release 4-aminopyridine (Fampridine-SR), a potassium channel blocker, in subjects with chronic, incomplete spinal cord injury (SCI).
6(0,0,1,1) Details
12509600 Velez L, Shirazi F, Goto C, Shepherd G, Roth BA: Opisthotonic posturing with neuromuscular irritability attributable to 4-aminopyridine ingestion by a healthy pediatric patient. Pediatrics. 2003 Jan;111(1):e82-4.

INTRODUCTION: 4-Aminopyridine (4-AP) is a potassium channel blocker used to increase muscle strength in the treatment of demyelinating diseases such as multiple sclerosis.
6(0,0,1,1) Details
11136357 Tallaksen CM, Tauboll E: Excitatory effect of thiamin on CA1 pyramidal neurones in rat hippocampal slices in vitro. Eur J Neurol. 2000 Nov;7(6):693-8.

Additional experiments with low concentrations of the potassium channel blocker 4-aminopyridine showed similar findings.
6(0,0,1,1) Details
10583911 Hendriks R, Morest DK, Kaczmarek LK: Role in neuronal cell migration for high-threshold potassium currents in the chicken hindbrain. J Neurosci Res. 1999 Dec 15;58(6):805-14.

These currents were completely suppressed by the potassium channel blockers, 1.0 mM tetraethylammonium chloride (TEA) or 1.0 mM 4-aminopyridine (4-AP).
31(0,1,1,1) Details
12377604 Chen M, Sun HY, Wang Y, Gao TM: Protection of potassium channel inhibitors against hypoxia/reoxygenation-induced death of cultured hippocampal neurons. Di Yi Jun Yi Da Xue Xue Bao. 2002 Oct;22(10):872-4.

However, A-type potassium channel inhibitor 4-aminopyridine presented no protection against neuron death (P> 0.05).
5(0,0,0,5) Details
11906724 Stafford JL, Galvez F, Goss GG, Belosevic M: Induction of nitric oxide and respiratory burst response in activated goldfish macrophages requires potassium channel activity. Dev Comp Immunol. 2002 Jun;26(5):445-59.

Since relatively little is known about the types of potassium channels present in fish macrophages, pharmacological blockers with broad ranges of activity were tested: 4-aminopyridine (4-AP), quinine, and tetraethylammonium chloride (TEA).
4(0,0,0,4) Details
14618675 Yang TT, Hung CF, Lee YJ, Su MJ, Wang SJ: Morphine inhibits glutamate exocytosis from rat cerebral cortex nerve terminals (synaptosomes) by reducing Ca2+ influx. Synapse. 2004 Feb;51(2):83-90.

Morphine, a mu-opioid agonist, suppressed the Ca (2+)-dependent release of glutamate that was evoked by exposing cerebrocortical synaptosomes to the potassium channel blocker 4-aminopyridine.
31(0,1,1,1) Details
19643095 Smith AJ, Tauskela JS, Stone TW, Smith RA: Preconditioning with 4-aminopyridine protects cerebellar granule neurons against excitotoxicity. Brain Res. 2009 Oct 19;1294:165-75. Epub 2009 Jul 28.

We report here the potential of an alternative strategy, tested on rat neonatal cerebellar granule neurons, which involves a 48-hour preconditioning step using the potassium channel blocker 4-aminopyridine (4-AP), at a low (50 microM) and at a higher (2500 microM) concentration (in the presence or absence of the GABA (A) receptor antagonist, bicuculline). 4-Aminopyridine gave extensive protection against a number of stressors (glutamate, NMDA and 3-nitropropionic acid) applied 24 h following the end of the preconditioning period.
31(0,1,1,1) Details
19302905 Blight AR, Henney HR 3rd: Pharmacokinetics of 14C-radioactivity after oral intake of a single dose of 14C-labeled fampridine (4-aminopyridine) in healthy volunteers. Clin Ther. 2009 Feb;31(2):328-35.

BACKGROUND: Fampridine (4-aminopyridine) is a potassium channel blocker that has been evaluated as a treatment for patients with spinal cord injury and multiple sclerosis.
6(0,0,1,1) Details
16554499 Ziburkus J, Cressman JR, Barreto E, Schiff SJ: Interneuron and pyramidal cell interplay during in vitro seizure-like events. J Neurophysiol. 2006 Jun;95(6):3948-54. Epub 2006 Mar 22.

We describe a novel pattern of interleaving EI activity during spontaneous in vitro SLEs generated by the potassium channel blocker 4-aminopyridine in the presence of decreased magnesium.
6(0,0,1,1) Details
17395137 Strupp M, Zwergal A, Brandt T: Episodic ataxia type 2. . Neurotherapeutics. 2007 Apr;4(2):267-73.

Two effective treatment options have been established for EA 2: acetazolamide (ACTZ), which probably changes the intracellular pH and thereby the transmembraneous potential, and 4-aminopyridine (4-AP), a potassium channel blocker.
6(0,0,1,1) Details
17542761 Segal JL, Thompson JF, Tayek JA: Effects of long-term 4-aminopyridine therapy on glucose tolerance and glucokinetics in patients with spinal cord injury. Pharmacotherapy. 2007 Jun;27(6):789-92.

STUDY OBJECTIVE: To assess the effects of the potassium channel blocker, 4-aminopyridine, on glucose tolerance and glucokinetics in patients with spinal cord injury.
6(0,0,1,1) Details
10623483 Banchelli G, Raimondi L, Ghelardini C, Pirisino R, Bertini V, De Munno A, Lucchesini F: Benzylamine-related compounds stimulate rat vas deferens neurotransmission and potentiate memory in the mouse acting as potassium channel blockers. Pharmacol Res. 2000 Feb;41(2):151-62.

To verify if this effect could be referred to as a modulation of potassium channels the activity of some benzylamines, KCl, tetraetylammonium (TEA), BaCl (2), 4-aminopyridine (4-AP), glibenclamide (GLI), charibdotoxin (ChTX) and apamin (APA) has been compared.
3(0,0,0,3) Details
15127611 Pan YP, Xu XH, Wang XL: [High throughput screening method of potassium channel regulators] . Yao Xue Xue Bao. 2004 Feb;39(2):85-8.


AIM: To discover new regulators of potassium channel, an in vitro assay based on DiBAC4 (3) to determine the fluorescence was established for high throughput screening.
3(0,0,0,3) Details
11136940 Horiuchi T, Dietrich HH, Tsugane S, Dacey RG Jr: Role of potassium channels in regulation of brain arteriolar tone: comparison of cerebrum versus brain stem. Stroke. 2001 Jan;32(1):218-24.

The internal diameter of cannulated and pressurized vessel was monitored with the inverted microscope before and after administration of potassium channel inhibitors.
RESULTS: Cerebral and brain stem arterioles were significantly constricted by 4-aminopyridine and low concentration of BaCl (2) but not by glibenclamide.
2(0,0,0,2) Details
17532582 Collins A, Larson MK, Pfaff JE, Ishmael JE: Survival of Swiss-Webster mouse cerebellar granule neurons is promoted by a combination of potassium channel blockers. Toxicol Lett. 2007 Jun 15;171(1-2):60-8. Epub 2007 Apr 24.

Potassium channel blockers, 2 mM 4-aminopyridine (4-AP), 2 mM tetraethylammonium (TEA) or 1 mM Ba (2+), individually afforded limited protection in 5.6 mM K (+).
8(0,0,1,3) Details
17629412 McBride JM, Smith DT, Byrn SR, Borgens RB, Shi R: 4-Aminopyridine derivatives enhance impulse conduction in guinea-pig spinal cord following traumatic injury. Neuroscience. 2007 Aug 10;148(1):44-52. Epub 2007 Jul 12.

4-Aminopyridine (4-AP), a potassium channel blocker, is capable of restoring conduction in the injured spinal cord.
7(0,0,1,2) Details
11739602 Lambe EK, Aghajanian GK: The role of Kv1.2-containing potassium channels in serotonin-induced glutamate release from thalamocortical terminals in rat frontal cortex. J Neurosci. 2001 Dec 15;21(24):9955-63.

Here, we investigate parallels in EPSCs induced by either serotonin or the potassium channel blockers 4-aminopyridine (4-AP) or alpha-dendrotoxin (DTX).
7(0,0,1,2) Details
15655396 Straube A: Pharmacology of vertigo/nystagmus/oscillopsia. Curr Opin Neurol. 2005 Feb;18(1):11-4.

A new pharmacological treatment option for downbeat nystagmus is the administration of potassium channel blockers (e.g. 4-aminopyridine).
7(0,0,1,2) Details
12969154 Achar E, Achar RA, Paiva TB, Campos AH, Schor N: Amitriptyline eliminates calculi through urinary tract smooth muscle relaxation. Kidney Int. 2003 Oct;64(4):1356-64.

This effect was prevented by pretreatment of urethral rings with 4-aminopyridine (4-AP), a voltage-dependent potassium channel blocker.
6(0,0,1,1) Details
16297607 McBride JM, Smith DT, Byrn SR, Borgens RB, Shi R: Dose responses of three 4-aminopyridine derivatives on axonal conduction in spinal cord trauma. Eur J Pharm Sci. 2006 Feb;27(2-3):237-42. Epub 2005 Nov 16.

The tested compounds significantly enhanced axonal conduction to the stretch injured cord at 1 microM, a dose that coincides with the clinically relevant dose of potassium channel blocker 4-aminopyridine (4-AP).
6(0,0,1,1) Details
19470382 Zhao P, Huang X, Wang ZY, Qiu ZX, Han YF, Lu HL, Kim YC, Xu WX: Dual effect of exogenous hydrogen sulfide on the spontaneous contraction of gastric smooth muscle in guinea-pig. Eur J Pharmacol. 2009 Aug 15;616(1-3):223-8. Epub 2009 May 23.

The excitatory effect on spontaneous contraction, caused by low concentrations of NaHS, was abolished when the muscle strips were pretreated with 10 mM tetraethylammonium (TEA), a nonselective potassium channel blocker, or 0.5 mM 4-Aminopyridine (4-AP), a voltage-gated K (+) channel blocker.
6(0,0,1,1) Details
19443939 Eksert B, Usta C: Role of potassium channels in the relaxant effect of levosimendan in guinea pig tracheal preparations. Pharmacol Rep. 2009 Mar-Apr;61(2):275-80.

Incubation of guinea pig tracheal rings with the ATP-dependent potassium channel (K (ATP)) blocker glibenclamide for 30 min significantly inhibited the relaxant responses to both levosimendan and cromakalim.
However, incubation of the tracheal rings with the voltage-dependent potassium channel blocker 4-aminopyridine for 10 min did not cause significant alterations on relaxant responses to levosimendan.
2(0,0,0,2) Details
15730786 Zhao LM, Xu YJ, Zhang ZX, Ni W, Chen SX: [Effect of potassium channel on the proliferation, apoptosis and related-gene expression in human bronchial smooth muscle cells]. Zhonghua Jie He He Hu Xi Za Zhi. 2004 Dec;27(12):841-6.

The cultured HBSMCs were divided into four groups: (1) control group; (2) 4-aminopyridine (4-AP) group: containing 4 mmol/L 4-AP; (3) TEA group: containing 1 mmol/L TEA; (4) Glib group: containing 0.1 mmol/L Glib.
2(0,0,0,2) Details
18565223 Klassen TL, Spencer AN, Gallin WJ: A naturally occurring omega current in a Kv3 family potassium channel from a platyhelminth. BMC Neurosci. 2008 Jun 19;9:52.

The inward rectifier channels (wild-type and mutant) are sensitive to 4-aminopyridine (4-AP) but not tetra-ethyl ammonium (TEA), whereas the delayed rectifier mutants are sensitive to TEA but not 4-AP.
2(0,0,0,2) Details
12804404 Solari A, Uitdehaag B, Giuliani G, Pucci E, Taus C: Aminopyridines for symptomatic treatment in multiple sclerosis. . Cochrane Database Syst Rev. 2003;(2):CD001330.

BACKGROUND: The potassium channel blockers 4-aminopyridine (AP) and 3,4-diaminopyridine (DAP) increase nerve conduction in demyelinated nerve fibers, and have been proposed as a symptomatic therapy for people with multiple sclerosis (MS).
6(0,0,1,1) Details
19445932 Vilagi I, Dobo E, Borbely S, Czege D, Molnar E, Mihaly A: Repeated 4-aminopyridine induced seizures diminish the efficacy of glutamatergic transmission in the neocortex. Exp Neurol. 2009 Sep;219(1):136-45. Epub 2009 May 13.

Systemic administration of the potassium channel blocker 4-aminopyridine (4-AP) elicits acute convulsions.
6(0,0,1,1) Details
11401416 Koyuncuoglu H, Nurten A, Enginar N, Ozerman B, Kara I: The effects of different 4-aminopyridine and morphine combinations on the intensity of morphine abstinence. Pharmacol Res. 2001 Mar;43(3):245-50.

In this study the effect of the increase in the endogenous glutamate (GLU) release due to 4-aminopyridine (4-AP), a potassium channel blocker, during the development of morphine (M) physical dependence and during the naloxone (NL)-precipitated abstinence syndrome was investigated.
6(0,0,1,1) Details
15608074 Tertyshnikova S, Knox RJ, Plym MJ, Thalody G, Griffin C, Neelands T, Harden DG, Signor L, Weaver D, Myers RA, Lodge NJ: BL-1249 [(5,6,7,8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine] : a putative potassium channel opener with bladder-relaxant properties. J Pharmacol Exp Ther. 2005 Apr;313(1):250-9. Epub 2004 Dec 17.

The BL-1249-evoked outward K+ current was insensitive to blockade by glyburide, tetraethylammonium, iberiotoxin, 4-aminopyridine, apamin, or Mg2+.
2(0,0,0,2) Details
11880492 Faber ES, Sah P: Physiological role of calcium-activated potassium currents in the rat lateral amygdala. J Neurosci. 2002 Mar 1;22(5):1618-28.

Blockade of large conductance calcium-activated potassium channel (BK) channels with paxilline, iberiotoxin, or TEA revealed that BK channels are involved in action potential repolarization but only make a small contribution to the fast AHP that follows action potentials.
The fast AHP was, however, markedly reduced by low concentrations of 4-aminopyridine and alpha-dendrotoxin, indicating the involvement of voltage-gated potassium channels in the fast AHP.
2(0,0,0,2) Details
15716550 Glasauer S, Kalla R, Buttner U, Strupp M, Brandt T: 4-aminopyridine restores visual ocular motor function in upbeat nystagmus. . J Neurol Neurosurg Psychiatry. 2005 Mar;76(3):451-3.

The effect of the potassium channel blocker 4-aminopyridine (4-AP) on spontaneous upbeat nystagmus (UBN) was investigated with the search coil technique during fixation in different gaze positions and smooth pursuit in a patient before and after ingestion of 10 mg 4-AP.
6(0,0,1,1) Details
18718349 Glasauer S, Rossert C: Modelling drug modulation of nystagmus. . Prog Brain Res. 2008;171:527-34.

A treatment option for downbeat nystagmus (DBN), a common form of acquired fixation nystagmus that often occurs with cerebellar degeneration, is low doses of the potassium channel blocker 4-aminopyridine (4-AP).
6(0,0,1,1) Details
15827015 Glasauer S, Strupp M, Kalla R, Buttner U, Brandt T: Effect of 4-aminopyridine on upbeat and downbeat nystagmus elucidates the mechanism of downbeat nystagmus. Ann N Y Acad Sci. 2005 Apr;1039:528-31.

The potassium channel blocker 4-aminopyridine (4-AP) restored vertical smooth pursuit and gaze holding in light in one patient with upbeat (UBN) and in one with downbeat nystagmus (DBN).
6(0,0,1,1) Details
18414393 Albus K, Wahab A, Heinemann U: Standard antiepileptic drugs fail to block epileptiform activity in rat organotypic hippocampal slice cultures. Br J Pharmacol. 2008 Jun;154(3):709-24. Epub 2008 Apr 14.

SLEs were induced by lowering magnesium concentration or by applying the potassium channel blocker 4-aminopyridine.
6(0,0,1,1) Details
19548855 Bever CT, Judge SI: Sustained-release fampridine for multiple sclerosis. . Expert Opin Investig Drugs. 2009 Jul;18(7):1013-24.

Fampridine (4-aminopyridine) is a potassium channel blocker that can increase action potential duration and amplitude, leading to improved conduction in demyelinated nerve fibers and to increased neurotransmitter release at synaptic endings.
6(0,0,1,1) Details
16829109 Usta C, Eksert B, Golbasi I, Bigat Z, Ozdem SS: The role of potassium channels in the vasodilatory effect of levosimendan in human internal thoracic arteries. Eur J Cardiothorac Surg. 2006 Aug;30(2):329-32. Epub 2006 Jul 7.

Incubation of human internal thoracic artery rings with adenosine 3',5'-triphosphate (ATP)-dependent potassium channel blocker glibenclamide (10 (-6) M) for 30 min significantly inhibited the relaxant responses to both levosimendan and cromakalim.
Incubation of the rings with the voltage-dependent potassium channel blocker 4-aminopyridine (5 mM) for 10 min did not cause significant alterations in relaxant responses to levosimendan.
2(0,0,0,2) Details
16448858 Iwasaki-Kurashige K, Loyaga-Rendon RY, Matsumoto H, Tokunaga T, Azuma H: Possible mediators involved in decreasing peripheral vascular resistance with blackcurrant concentrate (BC) in hind-limb perfusion model of the rat. Vascul Pharmacol. 2006 Apr;44(4):215-23. Epub 2006 Jan 30.


The decrease in PP with BC was abolished by endothelial removal, nitroarginine plus tetraethylammonium, nitroarginine plus catalase or 1H-[1,2,4] oxadiazolo [4,3-a] quinoxaline-1-one as an inhibitor of guanylyl cyclase and potassium channel (s), and accompanied by the increased cyclic GMP level.
2(0,0,0,2) Details
15943238 Kuznetzova IV, Evstigneev DA, Glukhova NV: [Transformation of electrical activity in the myelinated nerve fibres of amphibia by 4-aminopyridine]. Fiziol Zh. 2005;51(2):96-103.

Using the extracellular recording we studied the effect of 4-aminopyridine (4-AP), a potassium channel blocker on the electrical activity of the myelinated nerve fibres of amphibia Rana ridibunda Pallas.
6(0,0,1,1) Details
17822718 Wang Y, Shi JG, Wang MZ, Che CT, Yeung JH: Mechanisms of the vasorelaxant effect of 1-hydroxy-2, 3, 5-trimethoxy-xanthone, isolated from a Tibetan herb, Halenia elliptica, on rat coronary artery. Life Sci. 2007 Sep 1;81(12):1016-23. Epub 2007 Aug 17.

In endothelium-denuded coronary artery rings, the vasorelaxant effect of HM-1 was unaffected by potassium channel blockers such as tetraethylammonium (10 mM), iberiotoxin (100 nM), barium chloride (100 microM) and 4-aminopyridine (1 mM).
6(0,0,1,1) Details
11687106 Solari A, Uitdehaag B, Giuliani G, Pucci E, Taus C: Aminopyridines for symptomatic treatment in multiple sclerosis. . Cochrane Database Syst Rev. 2001;(4):CD001330.

BACKGROUND: Because of their ability to increase nerve conduction in demyelinated nerve fibers, potassium channel blockers 4-aminopyridine (AP) and 3,4-diaminopyridine (DAP) have been proposed as a symptomatic therapy for people with multiple sclerosis (MS).
6(0,0,1,1) Details
11217039 Sabbah S, Scriba GK: Development and validation of a capillary electrophoresis assay for the determination of 3,4-diaminopyridine and 4-aminopyridine including related substances. J Chromatogr A. 2001 Jan 12;907(1-2):321-8.

A capillary electrophoresis (CE) assay has been developed for the quantitation and determination of the impurity profile of the potassium channel blockers 3,4-diaminopyridine and 4-aminopyridine.
6(0,0,1,1) Details
11376889 Huang H, Gao TM, Gong L, Zhuang Z, Li X: Potassium channel blocker TEA prevents CA1 hippocampal injury following transient forebrain ischemia in adult rats. Neurosci Lett. 2001 Jun 8;305(2):83-6.

To understand the role of the enhanced potassium current in the pathogenesis of neuronal damage after ischemia, we examined the effects of tetraethylammonium (TEA) and 4-aminopyridine (4-AP) on the neuronal injury of CA1 region induced by 15 min forebrain ischemia using a four-vessel occlusion model.
2(0,0,0,2) Details
15746700 Bisseling TM, Versteegen MG, van der Wal S, Copius Peereboom-Stegeman JJ, Borggreven JM, Steegers EA, van der Laak JA, Russel FG, Smits P: Impaired KATP channel function in the fetoplacental circulation of patients with type 1 diabetes mellitus. Am J Obstet Gynecol. 2005 Mar;192(3):973-9.

Because potassium channels play an important role in the regulation of vascular tone, this study explores the impact of diabetes on potassium channel function in the fetoplacental vascular bed.
RESULTS: Glibenclamide (KATP channel blocker) increased perfusion pressure to a maximum fetoplacental arterial pressure of 37 +/- 6 mm Hg in controls versus 15 +/- 6 mm Hg in diabetes (P < .05). 4-Aminopyridine (KV channel blocker) equally increased fetoplacental arterial pressure in controls, and in diabetes (21 +/- 4 mm Hg vs 22 +/- 2 mm Hg).
2(0,0,0,2) Details
16481434 Sakurai A, Darghouth NR, Butera RJ, Katz PS: Serotonergic enhancement of a 4-AP-sensitive current mediates the synaptic depression phase of spike timing-dependent neuromodulation. J Neurosci. 2006 Feb 15;26(7):2010-21.

The potentiation phase of STDN was unaffected by spike broadening produced by the potassium channel blocker 4-aminopyridine (4-AP).
6(0,0,1,1) Details
18206155 Trailovic SM, Verma S, Clark CL, Robertson AP, Martin RJ: Effects of the muscarinic agonist, 5-methylfurmethiodide, on contraction and electrophysiology of Ascaris suum muscle. Int J Parasitol. 2008 Jul;38(8-9):945-57. Epub 2007 Dec 8.

In a larval migration assay we demonstrated that 4-aminopyridine (4-AP: a potassium channel blocker) potentiated the effects of levamisole but MFI did not.
6(0,0,1,1) Details
15965357 Regan CP, Cresswell HK, Zhang R, Lynch JJ: Novel method to assess cardiac electrophysiology in the rat: characterization of standard ion channel blockers. J Cardiovasc Pharmacol. 2005 Jul;46(1):68-75.

The potassium channel blocker 4-aminopyridine caused significant increases in atrial and ventricular refractoriness.
6(0,0,1,1) Details
10890901 Sanna PP, Berton F, Cammalleri M, Tallent MK, Siggins GR, Bloom FE, Francesconi W: A role for Src kinase in spontaneous epileptiform activity in the CA3 region of the hippocampus. Proc Natl Acad Sci U S A. 2000 Jul 18;97(15):8653-7.

Spontaneous epileptiform discharges were induced in vitro in the CA3 region of rat hippocampal slices by superfusion with the potassium channel blocker 4-aminopyridine in Mg (2+)-free medium.
6(0,0,1,1) Details
10729327 Hoffman AF, Lupica CR: Mechanisms of cannabinoid inhibition of GABA (A) synaptic transmission in the hippocampus. J Neurosci. 2000 Apr 1;20(7):2470-9.

The presynaptic effect of WIN 55,212-2 was also investigated using the potassium channel blockers barium and 4-aminopyridine.
6(0,0,1,1) Details
16914950 Wang D, Darwish DS, Schreurs BG: Effects of 4-aminopyridine on classical conditioning of the rabbit (Oryctolagus cuniculus) nictitating membrane response. Behav Pharmacol. 2006 Jun;17(4):319-29.

Previous in-vitro research in a number of species including Hermissenda and the rabbit suggests that a 4-aminopyridine-sensitive transient potassium channel may be involved in classical conditioning.
6(0,0,1,1) Details
14534264 Cabanes C, Viana F, Belmonte C: Differential thermosensitivity of sensory neurons in the guinea pig trigeminal ganglion. J Neurophysiol. 2003 Oct;90(4):2219-31.

However, after application of submillimolar concentrations (100 microM) of the potassium channel blocker 4-aminopyridine (4-AP), 29% previously unresponsive neurons developed cold sensitivity.
6(0,0,1,1) Details
10640333 Smith GT, Zakon HH: Pharmacological characterization of ionic currents that regulate the pacemaker rhythm in a weakly electric fish. J Neurobiol. 2000 Feb 5;42(2):270-86.

Two potassium channel blockers, 4-aminopyridine (4AP) and kappaA-conotoxin SIVA, increased pacemaker firing rates by approximately 20% and then stopped pacemaker firing.
6(0,0,1,1) Details
19915712 Renganathan M, Sidach S, Blight AR: Effects of 4-Aminopyridine on Cloned hERG Channels Expressed in Mammalian Cells. Arch Drug Inf. 2009 Sep;2(3):51-57.

INTRODUCTION: Non-clinical evaluation of a medication's potential to induce cardiac toxicity is recommended by regulatory agencies. 4-Aminopyridine (fampridine) is a potassium channel blocker with the demonstrated ability to improve walking ability in patients with multiple sclerosis.
6(0,0,1,1) Details
11159264 Walcourt A, Scott RL, Nash HA: Blockage of one class of potassium channel alters the effectiveness of halothane in a brain circuit of Drosophila. Anesth Analg. 2001 Feb;92(2):535-41.

Shaker channels were specifically inactivated either by genetic means, using strains with two different severe Shaker mutations, or by pharmacologic means, using ingestion of millimolar concentrations of 4-aminopyridine.
2(0,0,0,2) Details
12958834 Liu XS, Xu YJ, Zhang ZX, Ni W: [Effects of potassium channel blockers on the proliferation of rat bronchial smooth muscle cells]. Yao Xue Xue Bao. 2003 May;38(5):333-6.

RESULTS: The KV blocker 4-aminopyridine (4-AP) was shown to significantly increase the expression of proliferating cell nucleus antigen in cultured rat BSMCs (P < 0.01), but the KCa blocker tetraethylammonium (TEA) and KATP blocker glibenclamide (Glib) did not show such effect (P > 0.05). 4-AP was found to significantly increase the optical density value of the cultured BSMCs (P < 0.01) by MTT method and the numbers of S + G2M BSMCs (P < 0.05) by flow-cytometry.
2(0,0,0,2) Details
16289841 Taccola G, Nistri A: Fictive locomotor patterns generated by tetraethylammonium application to the neonatal rat spinal cord in vitro. Neuroscience. 2006;137(2):659-70. Epub 2005 Nov 14.

Rhythmic alternating patterns elicited by tetraethylammonium on ventral roots were relatively stereotypic, had limited synergy with fictive locomotion induced by dorsal root stimuli, and were not accelerated by 4-aminopyridine.
The present electrophysiological investigation examined whether the broad spectrum potassium channel blocker tetraethylammonium could generate locomotor-like patterns.
2(0,0,0,2) Details
14529953 Roshan-Milani S, Ferrigan L, Khoshnood MJ, Davies CH, Cobb SR: Regulation of epileptiform activity in hippocampus by nicotinic acetylcholine receptor activation. Epilepsy Res. 2003 Sep;56(1):51-65.

Bath application of the potassium channel blocker 4-aminopyridine (4AP; 10-50 microM) resulted in the development of spontaneous epileptiform bursting activity in area CA3 that consisted of short duration (257+/-15 ms) field events occurring regularly at a frequency of 0.4+/-0.02 Hz.
6(0,0,1,1) Details
11249722 Darlington C: Fampridine Acorda Therapeutics. Curr Opin Investig Drugs. 2000 Nov;1(3):375-9.

Fampridine (EL-970; 4-aminopyridine), a potassium channel blocker, is in phase II development by Acorda for the potential treatment of spinal cord injuries and multiple sclerosis (MS) [385529].
6(0,0,1,1) Details
12686578 Pais I, Hormuzdi SG, Monyer H, Traub RD, Wood IC, Buhl EH, Whittington MA, LeBeau FE: Sharp wave-like activity in the hippocampus in vitro in mice lacking the gap junction protein connexin 36. J Neurophysiol. 2003 Apr;89(4):2046-54.

However, bath application of the potassium channel blocker 4-aminopyridine (4-AP; 20-80 microM) produced a pattern of activity in control mice (13/16 slices), consisting of burst discharges occurring in conjunction with kainate-evoked gamma-frequency oscillations, that was similar to that seen in Cx36KO mice.
6(0,0,1,1) Details
11409423 Yang XF, Rothman SM: Focal cooling rapidly terminates experimental neocortical seizures. Ann Neurol. 2001 Jun;49(6):721-6.

After creating a cranial window in anesthetized rats, we induced seizures by injecting artificial cerebrospinal fluid containing 4-aminopyridine (4-AP), a potassium channel blocker.
6(0,0,1,1) Details
15278774 Wohlrab D, Vocke M, Klapperstuck T, Hein W: Effects of potassium and anion channel blockers on the cellular response of human osteoarthritic chondrocytes. J Orthop Sci. 2004;9(4):364-71.

The potassium channel blocker 4-aminopyridine (4-AP) and the chloride and anion channel blocker 4-acetamido-4'-isothiocyano-2,2'-disulfonic acid stilbene (SITS) were used as ion channel modulators.
6(0,0,1,1) Details
19041986 Sun W, Smith D, Bryn S, Borgens R, Shi R: N-(4-pyridyl) methyl carbamate inhibits fast potassium currents in guinea pig dorsal root ganglion cells. J Neurol Sci. 2009 Feb 15;277(1-2):114-8. Epub 2008 Nov 29.

Previous studies demonstrated that 4-Aminopyridine, a fast potassium channel blocker, enhances impulse conduction on damaged and/or demyelinated axons, allowing for functional recovery in spinal cord injuries and MS, but with severe therapeutic limitations.
6(0,0,1,1) Details
11743993 Ohno K, Higashima M: Effects of antiepileptic drugs on afterdischarge generation in rat hippocampal slices. Brain Res. 2002 Jan 4;924(1):39-45.

ADs were progressively enhanced following repetitive high-frequency stimulations to slices treated with 4-aminopyridine, a proconvulsive A-type potassium channel blocker.
6(0,0,1,1) Details
17565871 Tang ZG, Liang CZ, Shen B, Hao ZY, Zhou ZX: [Changes in potassium channel currents of prostate epithelial cell of old rats and significance thereof]. Zhonghua Yi Xue Za Zhi. 2007 Mar 27;87(12):842-6.

5(0,0,0,5) Details
15755482 del Carmen Godino M, Torres M, Sanchez-Prieto J: The modulation of Ca2+ and K+ channels but not changes in cAMP signaling contribute to the inhibition of glutamate release by cannabinoid receptors in cerebrocortical nerve terminals. Neuropharmacology. 2005 Mar;48(4):547-57. Epub 2005 Jan 25.

Furthermore, WIN55,212-2 reduced 4-aminopyridine (4AP) evoked glutamate release to a larger extent by modulating the behavior of both Ca2+ and K (+)-channels.
The inhibition of 4AP-evoked release was associated with a decrease in cytoplasmic free Ca2+ and in plasma membrane depolarization that was reverted by the potassium channel blocker, tetraethylammonium.
1(0,0,0,1) Details
11872913 Horiuchi T, Dietrich HH, Hongo K, Goto T, Dacey RG Jr: Role of endothelial nitric oxide and smooth muscle potassium channels in cerebral arteriolar dilation in response to acidosis. Stroke. 2002 Mar;33(3):844-9.

Tetraethylammonium ion (1 mmol/L; calcium-activated potassium channel inhibitor) and 4-aminopyridine (100 micromol/L; voltage-dependent potassium channel inhibitor) as well as ouabain (10 micromol/L; Na-K ATPase inhibitor) and N-methylsulphonyl-6-(2-proparglyloxyphenyl) hexanamide (1 micromol/L; cytochrome P450 epoxygenase inhibitor) did not alter acidotic dilation.
RESULTS: The dilation was significantly inhibited by potassium chloride (30 mmol/L) and glibenclamide (3 micromol/L; ATP-sensitive potassium channel inhibitor).
1(0,0,0,1) Details
12874393 Strupp M, Schuler O, Krafczyk S, Jahn K, Schautzer F, Buttner U, Brandt T: Treatment of downbeat nystagmus with 3,4-diaminopyridine: a placebo-controlled study. Neurology. 2003 Jul 22;61(2):165-70.

In view of animal studies reporting that micromolar concentrations of 4-aminopyridine increased the excitability of Purkinje cells, it is suggested that the efficacy of 3,4-DAP may be due to an increase of the physiologic inhibitory influence of the vestibulocerebellum on the vestibular nuclei.
OBJECTIVE: To evaluate the effects of a single dose of the potassium channel blocker 3,4-diaminopyridine (3,4-DAP), which is known to increase the excitability of Purkinje cells, on DBN in a prospective, placebo-controlled, double-blind study with a crossover design.
1(0,0,0,1) Details
20112006 Husseini L, Leussink VI, Kieseier BC, Hartung HP: [4-Aminopyridine (Fampridine). Nervenarzt. 2010 Feb;81(2):203-11.

For years results of animal experiments and clinical experience have indicated that the potassium channel blocker 4-aminopyridine improves axonal excitatory circuits and thus muscular strength in demyelinating diseases.
6(0,0,1,1) Details
10992005 Brandsgaard R, Barrett JE, Rosenzweig-Lipson S: Pharmacological characterization of the discriminative stimulus effects of the potassium channel blocker 4-aminopyridine in rats. J Pharmacol Exp Ther. 2000 Oct;295(1):382-91.
6(0,0,1,1) Details
18442126 Lohle M, Schrempf W, Wolz M, Reichmann H, Storch A: Potassium channel blocker 4-aminopyridine is effective in interictal cerebellar symptoms in episodic ataxia type 2--a video case report. Mov Disord. 2008 Jul 15;23(9):1314-6.
6(0,0,1,1) Details
15136697 Strupp M, Kalla R, Dichgans M, Freilinger T, Glasauer S, Brandt T: Treatment of episodic ataxia type 2 with the potassium channel blocker 4-aminopyridine. Neurology. 2004 May 11;62(9):1623-5.

The authors report three patients with EA2 (two with proven mutations in the CACNA1A gene) whose attacks were prevented with the potassium channel blocker 4-aminopyridine (4-AP; 5 mg tid).
37(0,1,2,2) Details
16631661 Yildiz O, Seyrek M, Yildirim V, Demirkilic U, Nacitarhan C: Potassium channel-related relaxation by levosimendan in the human internal mammary artery. Ann Thorac Surg. 2006 May;81(5):1715-9.

Levosimendan-induced relaxations were tested in the presence of cyclooxygenase inhibitor indomethacin (10 micromol/L), nitric oxide synthase inhibitor N122-nitro-L-arginine methyl ester (100 micromol/L), large-conductance calcium-activated potassium-channel inhibitor tetraethylammonium (1 mmol/L), adenosine triphosphate-sensitive potassium-channel inhibitor glibenclamide (10 micromol/L), and voltage-sensitive potassium-channel inhibitor 4-aminopyridine (1 mmol/L).
33(0,1,1,3) Details
10960187 Biagi G, Calderone V, Giorgi I, Livi O, Scartoni V, Baragatti B, Martinotti E: 5-(4'-Substituted-2'-nitroanilino)-1,2,3-triazoles as new potential potassium channel activators. Eur J Med Chem. 2000 Jul-Aug;35(7-8):715-20.

Such a vasorelaxing activity was significantly reduced by the increase of the level of membrane depolarisation and by the potassium channel blocker 4-aminopyridine with a pharmacodynamic behaviour consistent with a potassium channel activation.
33(0,1,1,3) Details
14555824 Oh SJ, Ahn SC: Inhibitory effects of potassium channel blockers on carbachol-induced contraction in rat detrusor muscle. J Korean Med Sci. 2003 Oct;18(5):701-6.

We present accidental findings that potassium channel blockers, such as tetraethyl-ammonium (TEA) or 4-aminopyridine (4-AP), inhibit the sustained tonic contraction induced by carbachol in rat detrusor muscle strips.
33(0,1,1,3) Details
10800933 Morgan AC, Chang HY, Liu JS, Hua LL, Lee SC: High extracellular potassium modulates nitric oxide synthase expression in human astrocytes. J Neurochem. 2000 May;74(5):1903-12.

In addition, several potassium channel inhibitors such as CsCl, tetraethylammonium, and 4-aminopyridine as well as nigericin inhibited astrocyte iNOS expression induced by IL-1/IFNgamma.
32(0,1,1,2) Details
16243464 Rattmann YD, Cipriani TR, Sassaki GL, Iacomini M, Rieck L, Marques MC, da Silva-Santos JE: Nitric oxide-dependent vasorelaxation induced by extractive solutions and fractions of Maytenus ilicifolia Mart ex Reissek (Celastraceae) leaves. J Ethnopharmacol. 2006 Apr 6;104(3):328-35. Epub 2005 Oct 21.

Further, relaxation induced by this ethanolic supernatant have been strongly inhibited by the guanylate cyclase inhibitors methylene blue and ODQ, as well as by the potassium channel blockers 4-aminopyridine and tetraethylammonium, but was unchanged by the cyclooxygenase inhibitor indomethacin and the membrane receptor antagonists atropine, HOE-140 and pirilamine.
32(0,1,1,2) Details
10960595 Sanz AG, Hospital S, Badia A, Clos MV: Presynaptic effect of 7-OH-DPAT on evoked [3H]-acetylcholine release in rat striatal synaptosomes. Brain Res. 2000 Aug 25;874(2):116-22.

The objective of the present experiments was to study the presynaptic effect of 7-hydroxy-N,N-di-n-propyl-2-aminotetraline (7-OH-DPAT, a D (2)-like dopamine receptor agonist) on [3H]-acetylcholine ([3H]-ACh) release induced by potassium (15 mM, 25 mM and 60 mM), potassium channel-blockers (4-aminopyridine, 4-AP; tetraethylammonium, TEA and quinine) and veratridine to gain insight into the mechanisms involved in the activation of the D (2) dopamine-receptor subtype located at striatal cholinergic nerve terminals. 7-OH-DPAT (1 microM) inhibited the evoked [3H]-ACh release induced by K (+) 15 mM in a similar percentage than that obtained during basal conditions (30% and 27%, respectively).
32(0,1,1,2) Details
19406003 Alda JO, Valero MS, Pereboom D, Gros P, Garay RP: Endothelium-independent vasorelaxation by the selective alpha estrogen receptor agonist propyl pyrazole triol in rat aortic smooth muscle. J Pharm Pharmacol. 2009 May;61(5):641-6.

KEY FINDINGS: PPT vasorelaxation was largely reduced by the selective ERalpha antagonist methyl-piperidinopyrazole (MPP; -91.6+/-2.5%), by the selective PKG inhibitor Rp-8-Br-cGMP (-78.6+/-4.9%), by the specific soluble guanylyl cyclase inhibitor ODQ (1H-(1,2,4)-oxadiazolo [4,3-a] quinoxalin-1-one; -85.3+/-5.2%) and to a lesser extent by the selective BKCa (large-conductance calcium- and voltage-activated potassium channel) inhibitor iberiotoxin (-59.3%), the selective IKCa (intermediate-conductance calcium-activated potassium channel) inhibitor TRAM-34 (1-[(2-chlorophenyl) diphenylmethyl]-1H-pyrazole; -50.7%) and the voltage-gated potassium channel inhibitor 4-aminopyridine (-40.8%).
32(0,1,1,2) Details
15893634 Zhu W, Pan ZZ: Mu-opioid-mediated inhibition of glutamate synaptic transmission in rat central amygdala neurons. Neuroscience. 2005;133(1):97-103.

Furthermore, the mu-opioid inhibition of the EPSC was blocked by 4-aminopyridine (4AP; 100 microM), a voltage-dependent potassium channel blocker, and by phospholipase A (2) inhibitors AACOCF (3) (10 microM) and quinacrine (10 microM).
32(0,1,1,2) Details
16432512 Gonczi M, Szentandrassy N, Johnson IT, Heagerty AM, Weston AH: Investigation of the role of TASK-2 channels in rat pulmonary arteries; pharmacological and functional studies following RNA interference procedures. Br J Pharmacol. 2006 Mar;147(5):496-505.

The application of levcromakalim (10 microM), NS1619 (33 microM) and a potassium channel inhibitor cocktail (5 mM 4-aminopyridine, 10 mM tetraethylammonium chloride, 30 microM Ba2+ and 10 microM glibenclamide) had similar effects in control and in siRNA-transfected vessels.
32(0,1,1,2) Details
17703356 Akar F, Manavbasi Y, Parlar AI, Ulus AT, Katircioglu SF: The gender differences in the relaxation to levosimendan of human internal mammary artery. Cardiovasc Drugs Ther. 2007 Oct;21(5):331-8.

The relaxations to levosimendan were also assessed in the presence of glibenclamide (10 microM), an adenosine triphosphate-sensitive potassium channel (K (ATP)) blocker, or charybdotoxin (100 nM), a calcium-activated potassium channel (K (Ca)) blocker, or 4-aminopyridine (1 mM), a voltage-sensitive potassium channel (K (v)) inhibitor.
32(0,1,1,2) Details
12712959 Abraham H, Losonczy A, Czeh G, Lazar GY: Potassium channel blockers tetraethylammonium and 4-aminopyridine fail to prevent microglial activation induced by elevated potassium concentration. Acta Biol Hung. 2003;54(1):63-78.

The effect of potassium channel blocker tetraethylammonium and 4-aminopyridine was examined on the elevated K+ concentration-induced microglial activation on rat hippocampal slice preparations.
32(0,1,1,2) Details
15719131 Liu SQ, Zang WJ, Li ZL, Sun Q, Yu XJ, Luo HL, Zhu SM: [Voltage-activated potassium channel blockers inhibit anisodamine-induced relaxation of rabbit aortic smooth muscles precontracted with noradrenaline]. Sheng Li Xue Bao. 2005 Feb 25;57(1):21-6.

In a 8-min period, 1, 3 and 10 micromol/L of anisodamine, significantly relaxed the 0.01 micromol/L NA precontracted aortic ring by (19.1+/-3.1)%, (30.1+/-3.8)% and (38.3+/-4.2)%, respectively, compared with the controls [by (4.8+/-2.4)%, (5.1+/-1.8)% and (5.6+/-2.5)%, respectively] (P <0.01). 10 mmol/L of CsCl (a non-selective potassium channel blocker), 1 mmol/L of 4-aminopyridine [a selective voltage-activated potassium channel (K (V)) blocker], 10 mumol/L BaCl2 (a selective inwardly-rectifying potassium channel blocker), 10 micromol/L of glibenclamide (a selective ATP-sensitive potassium channel blocker), 3 micromol/L of charybdotoxin (a large- and intermediate-conductance Ca (2+)-activated potassium channels blocker) and 3 micromol/L of apamin (a selective small conductance Ca (2+)-activated potassium channel blocker) significantly increased the NA-induced contraction by (14.4+/-3.2)%, (16.3+/-5.8)%, (12.7+/-4.2)%, (13.6+/-2.0)%, (11.1+/-5.5)% and (13.4+/-4.3)%, respectively, compared with the control [by (5.6 +/-1.2)%] (P <0.01).
85(1,1,1,5) Details
15242826 Rezaie-Majd S, Murar J, Nelson DP, Kelly RF, Hong Z, Lang IM, Varghese A, Weir EK: Increased release of serotonin from rat ileum due to dexfenfluramine. . Am J Physiol Regul Integr Comp Physiol. 2004 Nov;287(5):R1209-13. Epub 2004 Jul 8.

In an isolated loop of rat ileum perfused with a physiological salt solution, the administration of dexfenfluramine, its major metabolite D-norfenfluramine, the potassium channel blocker 4-aminopyridine (5 mM), and caffeine (30 mM) increased serotonin levels in the venous effluent.
31(0,1,1,1) Details
10978056 Iida Y, Katusic ZS: Mechanisms of cerebral arterial relaxations to hydrogen peroxide. Stroke. 2000 Sep;31(9):2224-30.

In the presence of a nonselective potassium channel inhibitor, BaCl (2) (10 (-4) mol/L), a delayed rectifier potassium channel inhibitor, 4-aminopyridine (10 (-3) mol/L), or a calcium-activated potassium channel inhibitor, charybdotoxin (3 x 10 (-8) mol/L), the relaxations to hydrogen peroxide were also significantly reduced.
31(0,1,1,1) Details
11586111 Dumont RJ, Verma S, Okonkwo DO, Hurlbert RJ, Boulos PT, Ellegala DB, Dumont AS: Acute spinal cord injury, part II: contemporary pharmacotherapy. Clin Neuropharmacol. 2001 Sep-Oct;24(5):265-79.

Myriad treatment modalities, including corticosteroids, 21-aminosteroids, opioid receptor antagonists, gangliosides, thyrotropin-releasing hormone (TRH) and TRH analogs, antioxidants and free radical scavengers, calcium channel blockers, magnesium replacement therapy, sodium channel blockers, N -methyl-D-aspartate receptor antagonists, alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid-kainate receptor antagonists, modulators of arachadonic acid metabolism, neurotrophic growth factors, serotonin antagonists, antibodies against inhibitors of axonal regeneration, potassium channel blockers (4-aminopyridine), paclitaxel, clenbuterol, progesterone, gabexate mesylate, activated protein C, caspase inhibitors, tacrolimus, antibodies against adhesion molecules, and other immunomodulatory therapy have been studied to date.
31(0,1,1,1) Details
19268563 Crestani S, Rattmann YD, Cipriani TR, de Souza LM, Iacomini M, Kassuya CA, Marques MC, da Silva-Santos JE: A potent and nitric oxide-dependent hypotensive effect induced in rats by semi-purified fractions from Maytenus ilicifolia. Vascul Pharmacol. 2009 Jul;51(1):57-63. Epub 2009 Mar 4.

In addition, methylene blue and ODQ, as well as the potassium channel blockers tetraethylammonium,4-aminopyridine, and glibenclamide, impaired ESAE-induced hypotension.
The hypotension induced by EAF was circumvented by L-NAME, methylene blue andODQ, strongly reduced by tetraethylammonium and 4-aminopyridine (but not by glibenclamide), and abolished by association of these three potassium channel blockers.
1(0,0,0,1) Details
10789695 McAlexander MA, Undem BJ: Potassium channel blockade induces action potential generation in guinea-pig airway vagal afferent neurones. J Auton Nerv Syst. 2000 Jan 14;78(2-3):158-64.

Exposure of the mechanically sensitive receptive fields to 4-aminopyridine (100 microM-1 mM) caused pronounced action potential discharge in all fibres studied.
1(0,0,0,1) Details
12753410 Uhrenholt TR, Nedergaard OA: Calcium channels involved in noradrenaline release from sympathetic neurones in rabbit carotid artery. Pharmacol Toxicol. 2003 May;92(5):226-33.

The potassium channel blocking agent 4-aminopyridine (10-5-10-3 M) enhanced the stimulation-evoked 3H overflow up to 5 times. 4-Aminopyridine (10 (-4) M) did not alter the inhibitory effect of omega-conotoxin GVIA (3 x 10 (-8) M).
Potassium channel blockade increases Ca (2+) entry into sympathetic neurones.
1(0,0,0,1) Details
11605936 Liu R, Ueda M, Okazaki N, Ishibe Y: Role of potassium channels in isoflurane- and sevoflurane-induced attenuation of hypoxic pulmonary vasoconstriction in isolated perfused rabbit lungs. Anesthesiology. 2001 Oct;95(4):939-46.

The current study tested if the HPV-inhibitory effect of isoflurane and sevoflurane can be affected by changing the potassium-channel opening status with specific potassium-channel inhibitors in isolated rabbit lungs.
METHODS: Isolated rabbit lungs were divided into eight groups (n = 6 each in isoflurane groups and n = 8 in sevoflurane groups): those receiving no inhibitor treatment = control-isoflurane and control-sevoflurane groups; those treated with an adenosine triphosphate-sensitive potassium (K (ATP))-channel inhibitor, glibenclamide = glibenclamide-isoflurane and glibenclamide-sevoflurane groups; those treated with a high-conductance calcium-activated potassium (K (Ca))-channel inhibitor, iberiotoxin = iberiotoxin-isoflurane and iberiotoxin-sevoflurane groups; and those treated with a voltage-sensitive potassium (Kv)-channel inhibitor, 4-aminopyridine = 4-aminopyridine-isoflurane and 4-aminopyridine-sevoflurane groups.
1(0,0,0,1) Details
10604974 Gillis AM, Mathison HJ, Kulisz E, Lester WM: Dispersion of ventricular repolarization and ventricular fibrillation in left ventricular hypertrophy: influence of selective potassium channel blockers. J Pharmacol Exp Ther. 2000 Jan;292(1):381-6.

The magnitude of APD prolongation induced by the I (to) blocker 4-aminopyridine (4-AP) and combination 4-AP and the I (Kr) blocker dofetilide was greater in the hypertrophied hearts than in the normal hearts (P <.01).
1(0,0,0,1) Details
10611131 Smith KJ, Felts PA, John GR: Effects of 4-aminopyridine on demyelinated axons, synapses and muscle tension. Brain. 2000 Jan;123 ( Pt 1):171-84.

Several clinical trials have demonstrated that 4-amino-pyridine (4-AP), a potassium channel-blocking agent, improves symptoms in some patients with multiple sclerosis.
1(0,0,0,1) Details
18565276 Li L, Ma KT, Zhao L, Si JQ, Zhang ZS, Zhu H, Li J: Niflumic acid hyperpolarizes smooth muscle cells via calcium-activated potassium channel in spiral modiolar artery of guinea pigs. Acta Pharmacol Sin. 2008 Jul;29(7):789-99.

The NFA-induced response was almost completely blocked by charybdotoxin, iberiotoxin, tetraethylammonium, 1,2-bis (2- aminophenoxy) ethane-N,N,N',N'-tetraacetic acid tetrakis acetoxymethyl ester, but not by 4-aminopyridine, barium, glipizide, apamin, ouabain, and CdCl2.
1(0,0,0,1) Details
20083165 Henderson Z, Lu CB, Janzso G, Matto N, McKinley CE, Yanagawa Y, Halasy K: Distribution and role of Kv3.1b in neurons in the medial septum diagonal band complex. Neuroscience. 2010 Mar 31;166(3):952-69. Epub 2010 Jan 18.

The Kv3.1 potassium channel is a delayed rectifier channel that plays a major role in fast spiking neurons in the CNS, and has previously been localized in the MS/DB.
The results for the MS/DB were as follows: (1) cholinergic cells did not express GFP in either GAD67-GFP or VGluT2-GFP mice, and there was GAD67 immunoreactivity in GFP-positive neurons in GAD67-GFP mice and in a small proportion (6%) of GFP-positive neurons in VGluT2-GFP mice. (2) Kv3.1b immunofluorescence was associated with the somata of GABAergic neurons, especially those that contained parvalbumin, and with a minority of glutamatergic neurons, but not with cholinergic neurons, and with GABAergic axonal terminal-like processes around certain GABAergic neurons. (3) Both Kv3.1b-positive and -negative GABAergic neurons were septo-hippocampal, and there was a minor projection to hippocampus from VGluT2-GFP neurons. (4) Kainate-induced theta oscillations in the MS/DB slice were potentiated rather than inhibited by the Kv3.1 blocker 4-aminopyridine, and this agent on its own produced theta frequency oscillations in MS/DB slices that were reduced by ionotropic glutamate and GABA receptor antagonists and abolished by low extracellular calcium.
1(0,0,0,1) Details
11521164 Sampson LJ, Plane F, Garland CJ: Involvement of cyclic GMP and potassium channels in relaxation evoked by the nitric oxide donor, diethylamine NONOate, in the rat small isolated mesenteric artery. Naunyn Schmiedebergs Arch Pharmacol. 2001 Sep;364(3):220-5.

The contribution from cGMP-dependent signalling pathways was examined by exposing arteries to 1H-[1,2,4] oxadiazolo [4,3-a] quinoxalin-1-one (ODQ), a selective inhibitor of soluble guanylyl cyclase, while the contribution through potassium channels was assessed with different sub-type-selective potassium channel blockers.
The selective inhibitor of BK (Ca) channels, iberiotoxin (IbTX; 30 nM), and 4-aminopyridine (4-AP; 1 mM), an inhibitor of voltage-gated potassium channels (Kv), failed to modify DEA NONOate-evoked relaxation.
1(0,0,0,1) Details
11484102 Wohlrab D, Wohlrab J, Reichel H, Hein W: Is the proliferation of human chondrocytes regulated by ionic channels? . J Orthop Sci. 2001;6(2):155-9.

An association between potassium channel activity and cell proliferation has been detected in different human cell systems, whereas proof of an association between ion channel activity in human chondrocytes and their proliferation has yet to be established.
In this study, we investigated the concentration-dependent influence of the ion channel modulators tetraethylammonium (TEA), 4-aminopyridine (4-AP), 4',4'diisothiocyanato-stilbene-2,2'-disulfonic acid (DIDS), 4-acetamido-4'-isothiocyano-2,2'-disulfonic acid (SITS), and verapamil (vp) on the membrane potential and the proliferation of human chondrocytes, using flow cytometry.
1(0,0,0,1) Details
11117848 Hempelmann RG, Seebeck J, Ziegler A, Mehdorn HM: Effects of potassium channel inhibitors on the relaxation induced by the nitric oxide donor diethylamine nitric oxide in isolated human cerebral arteries. J Neurosurg. 2000 Dec;93(6):1048-54.

Different K+ channel inhibitors (tetraethylammonium [TEA], 10 (-3) M; charybdotoxin, 10 (-7) M; glibenclamide, 10 (-6) M; 4-aminopyridine [4-AP], 10 (-3) M; BaCl2, 5 x 10 (-5) M; and apamin, 10 (-6) M) alone failed to affect the responses to DEA/NO.
1(0,0,0,1) Details
10627587 Southan AP, Robertson B: Electrophysiological characterization of voltage-gated K (+) currents in cerebellar basket and purkinje cells: Kv1 and Kv3 channel subfamilies are present in basket cell nerve terminals. J Neurosci. 2000 Jan 1;20(1):114-22.


Dendrotoxin-sensitive potassium channel subunits are highly concentrated in cerebellar basket cell nerve terminals, and we have previously shown that they are responsible for a significant fraction of the voltage-gated potassium current in this region.
1(0,0,0,1) Details
15319384 Yeung CH, Barfield JP, Anapolski M, Cooper TG: Volume regulation of mature and immature spermatozoa in a primate model, and possible ion channels involved. Hum Reprod. 2004 Nov;19(11):2587-93. Epub 2004 Aug 19.


RVD of ejaculated spermatozoa was inhibited by the K+ channel blockers quinine and 4-aminopyridine (4-AP) but not by tetraethylammonium, Ba2+ or Gd3+, or the specific potassium channel blockers charybdotoxin, margatoxin, dendrotoxin, apamin, glybenclamide or clofilium.
0(0,0,0,0) Details
11313447 Alcon S, Morales S, Camello PJ, Hemming JM, Jennings L, Mawe GM, Pozo MJ: A redox-based mechanism for the contractile and relaxing effects of NO in the guinea-pig gall bladder. J Physiol. 2001 May 1;532(Pt 3):793-810.


These relaxations were sensitive to the guanylyl cyclase inhibitor 1H-[1,2,4] oxidiazolo [4,3-a] quinoxaline-1-one (ODQ, 2 microM) but they were not altered by treatment with the potassium channel blockers tetraethylammoniun (TEA, 5 mM) and 4-aminopyridine (4-AP, 5 mM).
0(0,0,0,0) Details
10832600 Terluk MR, da Silva-Santos JE, Assreuy J: Involvement of soluble guanylate cyclase and calcium-activated potassium channels in the long-lasting hyporesponsiveness to phenylephrine induced by nitric oxide in rat aorta. Naunyn Schmiedebergs Arch Pharmacol. 2000 May;361(5):477-83.


In contrast, 4-aminopyridine (1 mM) and glibenclamide (10 microM) had no effect.
0(0,0,0,0) Details
10990534 Yue L, Wang Z, Rindt H, Nattel S: Molecular evidence for a role of Shaw (Kv3) potassium channel subunits in potassium currents of dog atrium. J Physiol. 2000 Sep 15;527 Pt 3:467-78.

Like IKur,d, dKv3.1 was found to be highly sensitive to extracellular 4-aminopyridine (4-AP) and tetraethylammonium (TEA).
1(0,0,0,1) Details
16474412 Romano MR, Lograno MD: Cannabinoid agonists induce relaxation in the bovine ophthalmic artery: evidences for CB1 receptors, nitric oxide and potassium channels. Br J Pharmacol. 2006 Apr;147(8):917-25.

They also cause endothelium-independent relaxation by involving potassium channel opening.
Relaxations to anandamide and WIN55212-2 were inhibited by iberiotoxin (IbTX, 200 nM), a blocker of large conductance, Ca2+-activated K+ channel (BK (Ca)), and by 4-aminopyridine (4-AP; 1 mM), a blocker of delayed rectifier K+ channel, whereas the blockade of K (ATP) channels by glibenclamide (5 microM) and of small conductance Ca2+-activated K+ channels (SK (Ca)) by apamin (100 nM) did not produce any effects.
1(0,0,0,1) Details
12775263 Liu XS, Xu YJ, Zhang ZX, Li CQ, Yang DL: [The role of delayed rectifier potassium channels in the regulation of bronchial smooth muscle tension in asthmatic rats]. Zhonghua Jie He He Hu Xi Za Zhi. 2003 Jan;26(1):18-21.

METHODS: By using a specific potassium channel blocker, the bronchial contraction induced by spasmogens was observed in normal and asthmatic rats with the isometric tension recording technique.
RESULTS: (1) K (V) blocker 4-aminopyridine (4-AP) caused concentration-dependent bronchial contraction in vitro.
1(0,0,0,1) Details
11307870 Michelakis ED, Weir EK: Anorectic drugs and pulmonary hypertension from the bedside to the bench. Am J Med Sci. 2001 Apr;321(4):292-9.

The pathogenesis of PPH in patients treated with these agents is uncertain, but recent evidence suggests that potassium channel abnormalities and vasoactive and proliferative properties of 5-HT may play a role.
There is increasing experimental evidence suggesting that aminorex, fenfluramine and dexfenfluramine inhibit 4-aminopyridine-sensitive currents in potassium channels resulting in vasoconstriction in pulmonary resistance vessels and perhaps smooth muscle cell proliferation. 5-HT causes pulmonary artery vasoconstriction and smooth muscle cell proliferation.
1(0,0,0,1) Details
18992811 Engelmann J, van den Burg E, Bacelo J, de Ruijters M, Kuwana S, Sugawara Y, Grant K: Dendritic backpropagation and synaptic plasticity in the mormyrid electrosensory lobe. J Physiol Paris. 2008 Jul-Nov;102(4-6):233-45. Epub 2008 Oct 17.


Potassium channel labelling was sparse, being most abundant in the deep fibre layer and the nucleus of the electrosensory lobe.
1(0,0,0,1) Details
19923250 Sun W, Smith D, Fu Y, Cheng JX, Bryn S, Borgens R, Shi R: Novel potassium channel blocker, 4-AP-3-MeOH, inhibits fast potassium channels and restores axonal conduction in injured guinea pig spinal cord white matter. J Neurophysiol. 2010 Jan;103(1):469-78. Epub 2009 Nov 18.

We have demonstrated that 4-aminopyridine-3-methanol (4-AP-3-MeOH), a 4-aminopyridine derivative, significantly restores axonal conduction in stretched spinal cord white-matter strips and shows no preference in restoring large and small axons.
1(0,0,0,1) Details
11602697 Cogolludo AL, Perez-Vizcaino F, Lopez-Lopez G, Ibarra M, Zaragoza-Arnaez F, Tamargo J: Propafenone modulates potassium channel activities of vascular smooth muscle from rat portal veins. J Pharmacol Exp Ther. 2001 Nov;299(2):801-10.

In whole veins, propafenone behaved as the K (V) inhibitor 4-aminopyridine, increasing the amplitude and duration of spontaneous contractions.
1(0,0,0,1) Details
16214530 Gao YJ, Zeng ZH, Teoh K, Sharma AM, Abouzahr L, Cybulsky I, Lamy A, Semelhago L, Lee RM: Perivascular adipose tissue modulates vascular function in the human internal thoracic artery. J Thorac Cardiovasc Surg. 2005 Oct;130(4):1130-6.


The relaxation of the recipient artery induced by the transfer of incubation solution from the donor (artery with intact perivascular adipose tissue or perivascular adipose tissue alone) was absent in vessels precontracted by KCl (60 mmol/L) and was prevented by calcium-dependent potassium channel blockers (tetraethylammonium chloride, 1 mmol/L; iberiotoxin, 100 nmol/L), but not by the voltage-dependent potassium channel blocker 4-aminopyridine (1 mmol/L) and the adenosine triphosphate-dependent potassium channel blocker glibenclamide (10 micromol/L).
0(0,0,0,0) Details
19585753 Bhaskar A, Subbanna PK, Arasan S, Rajapathy J, Rao JP, Subramani S: 4-aminopyridine-induced contracture in frog ventricle is due to calcium released from intracellular stores. Indian J Physiol Pharmacol. 2008 Oct-Dec;52(4):366-74.

0(0,0,0,0) Details
15802557 Mobasheri A, Gent TC, Womack MD, Carter SD, Clegg PD, Barrett-Jolley R: Quantitative analysis of voltage-gated potassium currents from primary equine (Equus caballus) and elephant (Loxodonta africana) articular chondrocytes. Am J Physiol Regul Integr Comp Physiol. 2005 Jul;289(1):R172-80. Epub 2005 Mar 31.


Pharmacological investigation of equine chondrocyte Kv currents showed them to be powerfully inhibited by the potassium channel blockers tetraethylammonium and 4-aminopyridine but not by dendrotoxin-I.
0(0,0,0,0) Details
11429390 Plane F, Sampson LJ, Smith JJ, Garland CJ: Relaxation to authentic nitric oxide and SIN-1 in rat isolated mesenteric arteries: variable role for smooth muscle hyperpolarization. Br J Pharmacol. 2001 Jul;133(5):665-72.


When the endothelium was intact, ChTX inhibited hyperpolarization and relaxation to SIN-1 (n=5), while iberiotoxin (IbTX; 50 nM) or 4-aminopyridine (4-AP; 500 microM) reduced relaxation by 40% and 20%, respectively and by 80% in combination (n=6 in each case).
0(0,0,0,0) Details
17203288 Calderone V, Martelli A, Testai L, Martinotti E, Breschi MC: Functional contribution of the endothelial component to the vasorelaxing effect of resveratrol and NS 1619, activators of the large-conductance calcium-activated potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 2007 Mar;375(1):73-80. Epub 2007 Jan 4.


Furthermore, the effects of high depolarisation of potassium channel blockers TEA (Tetraethylammonium), 4-AP ( 4-Aminopyridine) and IbTX (Iberiotoxin) and of inhibitors of NO-pathway (L-NAME and ODQ) have been evaluated.
0(0,0,0,0) Details
16554965 Ozdem SS, Yalcin O, Meiselman HJ, Baskurt OK, Usta C: The role of potassium channels in relaxant effect of levosimendan in rat small mesenteric arteries. Cardiovasc Drugs Ther. 2006 Apr;20(2):123-7.

Incubation of rat small mesenteric arterial segments with ATP-dependent potassium channel (KATP) blocker glibenclamide (GLI, 10 (-6) M) for 30 min significantly inhibited the relaxant responses to both levosimendan and CRO.
Neither the Ca (2+)-activated potassium channel (KCa) blocker iberiotoxin (10 (-7) M) nor the voltage-dependent potassium channel (KV) blocker 4-aminopyridine (5 mM) incubation for 30 min caused significant alterations in relaxant responses to levosimendan in KCl-precontracted small mesenteric arteries.
1(0,0,0,1) Details
12050569 Venkateswarlu K, Giraldi A, Zhao W, Wang HZ, Melman A, Spektor M, Christ GJ: Potassium channels and human corporeal smooth muscle cell tone: diabetes and relaxation of human corpus cavernosum smooth muscle by adenosine triphosphate sensitive potassium channel openers. J Urol. 2002 Jul;168(1):355-61.

Furthermore, relaxation responses elicited by pinacidil and levcromakalim were not affected by charybdotoxin or 4-aminopyridine but were completely reversed by KCl or tetraethylammonium chloride.
1(0,0,0,1) Details
15631089 Dong K, Tao QM, Xia Q, Shan QX, Pan GB: [Endothelium-independent vasorelaxant effect of puerarin on rat thoracic aorta]. Zhongguo Zhong Yao Za Zhi. 2004 Oct;29(10):981-4.


The relaxant effect of puerarin was significantly inhibited by pretreatment of endothelium-denuded aorta with potassium channel antagonists tetraethylammonium, 4-aminopyridine but not glibenclamide.
0(0,0,0,0) Details
12694876 Hammadi A, Ramiandrasoa F, Sinou V, Rogier C, Fusai T, Le Bras J, Parzy D, Kunesch G, Pradines B: Cellular uptake of a catechol iron chelator and chloroquine into Plasmodium falciparum infected erythrocytes. Biochem Pharmacol. 2003 Apr 15;65(8):1351-60.


Combinations of FR160 with verapamil, diltiazem, clotrimazole, amiloride, diazoxide, 4-aminopyridine, and picrotoxin should be avoided (antagonistic effects).
0(0,0,0,0) Details
17271112 Dong K, Tao QM, Shan QX, Jin HF, Pan GB, Chen JZ, Zhu JH, Xia Q: Endothelium-independent vasorelaxant effect of puerarin on rat thoracic aorta. Conf Proc IEEE Eng Med Biol Soc. 2004;5:3757-60.


The relaxant effect of puerarin was significantly inhibited by pretreatment of endothelium-denuded aorta with potassium channel antagonists tetraethylammonium and 4-aminopyridine, but not glibenclamide.
0(0,0,0,0) Details
12456838 Haddock RE, Hill CE: Differential activation of ion channels by inositol 1,4,5-trisphosphate (IP3)- and ryanodine-sensitive calcium stores in rat basilar artery vasomotion. J Physiol. 2002 Dec 1;545(Pt 2):615-27.


Ryanodine, charybdotoxin and TRAM-34, but not iberiotoxin, 4-aminopyridine or apamin, each depolarized SMCs and increased the frequency of rhythmical depolarizations and [Ca (2+)](i) oscillations.
0(0,0,0,0) Details
18612804 Xue W, Zhang M, Li J, Wu D, Niu L, Liang Y: Effects of taurine on aortic rings isolated from fructose-fed insulin resistance Sprague-Dawley rat are changed. Cardiovasc Drugs Ther. 2008 Dec;22(6):461-8. Epub 2008 Jul 10.


Iberiotoxin (100 nM) only augmented the contraction enhancement in IR rings. 4-Aminopyridine (1 mM), glibenclamide (10 microM) and indomethacin (10 muM) had no influence on the effect of taurine in both NC and IR rings.
0(0,0,0,0) Details
19903983 Wang Y, Zhang M, Liu Y, Li J, Song E, Niu L, Cheng N: Neither K+ channels nor PI3K/Akt mediates the vasodilative effect of nebivolol on different types of rat arteries. J Cardiovasc Pharmacol Ther. 2009 Dec;14(4):332-8.


During contraction by KCl (60 mmol/L) or phenylephrine (PE; 10 (-6) mol/L; femoral artery and renal artery were precontracted by 10 (-5) mol/L), the effect of nebivolol (10 (-7)-10 (- 5) mol/L) was obtained in the presence of different potassium channel, PI3K/Akt, or NOS inhibitors.
1(0,0,0,1) Details
16536905 Dimpfel W: Different anticonvulsive effects of hesperidin and its aglycone hesperetin on electrical activity in the rat hippocampus in-vitro. J Pharm Pharmacol. 2006 Mar;58(3):375-9.

Modulation of the pyramidal cell response in the presence of tetraethylammonium (TEA) and pentylentetrazol on one hand and 4-aminopyridine (4-AP) and bicuculline on the other was influenced in a different way.
Since the action of hesperidin was sensitive to the presence of iberiotoxin, the involvement of a large conductance calcium-dependent potassium channel might be assumed.
1(0,0,0,1) Details
18206237 Li G, Sang N: Delayed rectifier potassium channels are involved in SO2 derivative-induced hippocampal neuronal injury. Ecotoxicol Environ Saf. 2009 Jan;72(1):236-41. Epub 2008 Feb 21.


Interestingly, the neuronal death and DNA ladder formation, caused by SO (2) derivatives, could be attenuated by the delayed rectifier potassium channel blocker (tetraethylammonium, TEA), but not by the transient outward potassium channel blocker (4-aminopyridine, 4-AP).
0(0,0,0,0) Details
19445161 Li Z, Zhang M, Liang Y: [Endothelium-independent vasorelaxant effect of Taurine on rat aorta rings]. Zhongguo Zhong Yao Za Zhi. 2009 Feb;34(3):332-5.


The relaxant effect of taurine was significantly inhibited by pretreatment of endothelium-denuded aorta with potassium channel antagonists glibenclamide and tetraethylamine but not by BaCl2 or 4-aminopyridine.
0(0,0,0,0) Details
16424798 Lam FF, Yeung JH, Cheung JH, Or PM: Pharmacological evidence for calcium channel inhibition by danshen (Salvia miltiorrhiza) on rat isolated femoral artery. J Cardiovasc Pharmacol. 2006 Jan;47(1):139-45.


A 3.3-fold shift was produced on the concentration-response curve of danshen when the artery rings were pretreated with a mixture of 10 mM TEA, 1 mM 4-aminopyridine (K (V) blocker), 1 microM glibenclamide (K (ATP) blocker), 100 nM iberiotoxin (BK (Ca) blocker), and 100 microM barium chloride (K (IR) blocker).
0(0,0,0,0) Details
18780812 Korenke AR, Rivey MP, Allington DR: Sustained-release fampridine for symptomatic treatment of multiple sclerosis. Ann Pharmacother. 2008 Oct;42(10):1458-65. Epub 2008 Sep 9.

DATA SOURCES: An English-language human data search was done using PubMed/MEDLINE (1966-August 2008) to retrieve relevant material using the search terms fampridine-SR, 4-aminopyridine, and multiple sclerosis.
DATA SYNTHESIS: Fampridine-SR is a sustained-release, orally administered potassium-channel blocker acting in the central nervous system to enhance conduction in demyelinated axons.
1(0,0,0,1) Details
12620956 Liu R, Ishibe Y, Okazaki N, Ueda M, Hirosawa J: Volatile anesthetics regulate pulmonary vascular tension through different potassium channel subtypes in isolated rabbit lungs. Can J Anaesth. 2003 Mar;50(3):301-4.

METHODS: To investigate whether or not potassium channels play a role in the effect of volatile anesthetic on pulmonary vessels, isolated and perfused rabbit lungs were divided into four groups (n = 7 each): a control group without treatment, a glibenclamide (Glib) group treated with adenosine triphosphate-sensitive K (+) (K (ATP)) channel inhibitor, a 4-aminopyridine (4-AP) group treated with voltage-sensitive K (+) (K (V)) channel inhibitor, and an iberiotoxin (IbTX) group treated with high conductance calcium-activated K (+) (K (Ca)) channel inhibitor.
1(0,0,0,1) Details
16888071 Dombkowski RA, Doellman MM, Head SK, Olson KR: Hydrogen sulfide mediates hypoxia-induced relaxation of trout urinary bladder smooth muscle. J Exp Biol. 2006 Aug;209(Pt 16):3234-40.


However, H2S relaxation of bladders was not affected by the potassium channel inhibitors, apamin, charybdotoxin, 4-aminopyridine, and glybenclamide, or by chloride channel/exchange inhibitors 4,4'-Diisothiocyanatostilbene-2,2'-disulfonic acid disodium salt, tamoxifen and glybenclamide, or by the presence or absence of extracellular HCO3-.
0(0,0,0,0) Details
12020933 Testai L, Chericoni S, Calderone V, Nencioni G, Nieri P, Morelli I, Martinotti E: Cardiovascular effects of Urtica dioica L. (Urticaceae) roots extracts: in vitro and in vivo pharmacological studies. J Ethnopharmacol. 2002 Jun;81(1):105-9.


Furthermore, potassium channel blockers (TEA, 4-aminopyridine, quinine, but not glybenclamide) antagonized the vasodilator action of the purified fraction F1W of U. dioica.
0(0,0,0,0) Details
17525113 Abi-Char J, Maguy A, Coulombe A, Balse E, Ratajczak P, Samuel JL, Nattel S, Hatem SN: Membrane cholesterol modulates Kv1.5 potassium channel distribution and function in rat cardiomyocytes. J Physiol. 2007 Aug 1;582(Pt 3):1205-17. Epub 2007 May 24.

MCD-increased current was inhibited by low 4-aminopyridine concentration.
1(0,0,0,1) Details
15610163 Brooke RE, Moores TS, Morris NP, Parson SH, Deuchars J: Kv3 voltage-gated potassium channels regulate neurotransmitter release from mouse motor nerve terminals. Eur J Neurosci. 2004 Dec;20(12):3313-21.

Significantly, this effect of TEA was still observed in the presence of the large-conductance calcium-activated potassium channel blockers iberiotoxin (25-150 nM) and Penitrem A (100 nM), suggesting a selective action on Kv3 subunits.
Consistent with this, 15-microM 4-aminopyridine, which blocks Kv3 but not large-conductance calcium-activated potassium channels, enhanced evoked EPP amplitude.
1(0,0,0,1) Details
15843617 Weisz CJ, Raike RS, Soria-Jasso LE, Hess EJ: Potassium channel blockers inhibit the triggers of attacks in the calcium channel mouse mutant tottering. J Neurosci. 2005 Apr 20;25(16):4141-5.

These mutations predict reduced calcium currents, particularly in cerebellar Purkinje cells, where these channels are most abundant. 4-Aminopyridine (4-AP), a nonselective blocker of K (v) voltage-gated potassium channels, alleviates attacks of ataxia in EA2 patients.
1(0,0,0,1) Details
15589969 Lo YC, Tsou HH, Lin RJ, Wu DC, Wu BN, Lin YT, Chen IJ: Endothelium-dependent and -independent vasorelaxation by a theophylline derivative MCPT: roles of cyclic nucleotides, potassium channel opening and phosphodiesterase inhibition. Life Sci. 2005 Jan 7;76(8):931-44.

This relaxation was also reduced by the presence of nitric oxide synthase inhibitor Nomega-nitro-L-arginine methylester (L-NAME, 100 microM), soluble guanylyl cyclase (sGC) inhibitors methylene blue (10 microM), 1 H-[1,2,4] oxidazolol [4,3-a] quinoxalin-1-one (ODQ, 1 microM), adenylyl cyclase (AC) blocker SQ 22536 (100 microM), ATP-sensitive K+ channel blocker (KATP) glibenclamide (1 microM), a Ca2+ activated K+ channels blocker tetraethylammonium (TEA, 10 mM) and a voltage-dependent potassium channels blocker 4-aminopyridine (4-AP, 100 microM).
1(0,0,0,1) Details
17380036 Seyrek M, Yildiz O, Ulusoy HB, Yildirim V: Testosterone relaxes isolated human radial artery by potassium channel opening action. J Pharmacol Sci. 2007 Mar;103(3):309-16.

Testosterone-induced relaxations were tested in the presence of the cyclooxygenase inhibitor indomethacin (10 microM), nitric oxide synthase inhibitor N (omega)-nitro-L-arginine methyl ester (L-NAME, 100 microM), non-selective large conductance Ca (2+)-activated and voltage-sensitive K (+) channel inhibitor tetraethylammonium (TEA, 1 mM), ATP-sensitive K (+) channel inhibitor glibenclamide (GLI, 10 microM), and voltage-sensitive K (+) channel inhibitor 4-aminopyridine (4-AP, 1 mM).
1(0,0,0,1) Details
17997400 Niu LG, Zhang MS, Liu Y, Xue WX, Liu DB, Zhang J, Liang YQ: Vasorelaxant effect of taurine is diminished by tetraethylammonium in rat isolated arteries. Eur J Pharmacol. 2008 Feb 2;580(1-2):169-74. Epub 2007 Oct 25.

The relaxation was not affected by 0.1 mM NG-nitro-L-arginine methylester ester (a nitric oxide synthetase inhibitor), 10 microM indomethacin (a cyclooxygenase inhibitor), 1 mM 4-aminopyridine (a K (V) blocker), 10 muM glibenclamide (a K (ATP) blocker), 1 mM barium chloride (BaCl (2), a K (IR) blocker), and 100 nM iberiotoxin (a BK (Ca) blocker), but was nearly abolished by 10 mM tetraethylammonium (TEA, a non-selective potassium channel blocker).
Present experiments show that taurine relaxes contracted rat aorta and inhibits the phenylephrine-induced contraction of renal and mesenteric arteries, and suggest that a mechanism related to potassium channel opening may be involved in the action of taurine.
1(0,0,0,1) Details
11566512 Deuchars SA, Brooke RE, Frater B, Deuchars J: Properties of interneurones in the intermediolateral cell column of the rat spinal cord: role of the potassium channel subunit Kv3.1. Neuroscience. 2001;106(2):433-46.

Low concentrations of tetraethylammonium chloride (TEA) (0.5 mM) or 4-aminopyridine (4-AP) (30 microM) affected interneurones but not sympathetic preganglionic neurones by prolonging the action potential repolarisation as well as decreasing both the afterhypolarisation amplitude and firing frequency.
1(0,0,0,1) Details
14638386 Schweizer T, Birthelmer A, Lazaris A, Cassel JC, Jackisch R: 3,4-DAP-evoked transmitter release in hippocampal slices of aged rats with impaired memory. Brain Res Bull. 2003 Dec 15;62(2):129-36.


Young adults (3-5 months) were used as controls. 3,4-diaminopyridine (3,4-DAP), a potassium channel antagonist which increases neuronal excitability, was used to evoke the overflow of the three neurotransmitters.
1(0,0,0,1) Details
18313857 Correia MJ, Weng T, Prusak D, Wood TG: Kvbeta1.1 associates with Kvalpha1.4 in Chinese hamster ovary cells and pigeon type II vestibular hair cells and enhances the amplitude, inactivation and negatively shifts the steady-state inactivation range. Neuroscience. 2008 Mar 27;152(3):809-20. Epub 2008 Jan 25.

In the native hair cells, the A-type current was identified by its pharmacological (4-aminopyridine (4-AP); IC (50)=11 microM) and voltage dependent inactivation properties.
To examine other possibilities, we cloned alpha and beta subunits that comprise the A-type potassium channel complex in adult and embryonic pigeon brain, cochlea and labyrinth.
1(0,0,0,1) Details
10800632 Barcenilla A, Alamo C, Carvajal A, Garcia-Pozo J, Velasco A: Effect of nicorandil upon different guinea-pig and rat isolated organ preparations in vitro. Arzneimittelforschung. 2000 Apr;50(4):341-4.

A study of the effect of nicorandil (N-2-(hydroxyethyl) nicotinamide nitrate, CAS 65141-46-0), a potassium channel and guanylatecyclase activator, upon preparations of rat was deferens and uterus, and guinea pig ileum was performed.
The drug exerts a non-competitive antagonist effect upon rat isolated uterus response to serotonin, histamine, oxytocin, and, at high concentrations, inhibits guinea-pig isolated ileum responses to acetylcholine, histamine, 4-aminopyridine and potassium.
1(0,0,0,1) Details
11007070 Mukerji MS, Leathard HL, Huddart H: The effects of potassium channel blockers on progesterone-induced suppression of rat portal vein contractility. J Pharm Pharmacol. 2000 Aug;52(8):983-90.

Incubation with barium chloride (20 and 100 microM), 4-aminopyridine (1 mM), tetraethylammonium chloride (1 mM), glibenclamide (1 microM) or apamin (1 microM) did not, however, have the same antagonistic effect.
1(0,0,0,1) Details
12142548 Mao BQ, MacLeish PR, Victor JD: Relation between potassium-channel kinetics and the intrinsic dynamics in isolated retinal bipolar cells. J Comput Neurosci. 2002 May-Jun;12(3):147-63.

1(0,0,0,1) Details
14526233 Lindauer U, Vogt J, Schuh-Hofer S, Dreier JP, Dirnagl U: Cerebrovascular vasodilation to extraluminal acidosis occurs via combined activation of ATP-sensitive and Ca2+-activated potassium channels. J Cereb Blood Flow Metab. 2003 Oct;23(10):1227-38.

Activity of one of these potassium channel families is sufficient for vasodilation to acidosis, and only combined inhibition completely abolishes vasodilation.
In separate experiments, ATP-sensitive potassium channels (KATP) were blocked by extraluminal application of glibenclamide (Glib), Ca2+-activated potassium channels (KCa) by tetraethylammonium (TEA), voltage-gated potassium channels (Kv) by 4-aminopyridine, and inward rectifier potassium channels (KIR) by BaCl2.
1(0,0,0,1) Details
18045622 Wang Y, Shi JG, Wang MZ, Che CT, Yeung JH: Mechanisms of the vasorelaxant effect of 1, 5-dihydroxy-2, 3-dimethoxy-xanthone, an active metabolite of 1-hydroxy-2, 3, 5-trimethoxy-xanthone isolated from a Tibetan herb, Halenia elliptica, on rat coronary artery. Life Sci. 2008 Jan 2;82(1-2):91-8. Epub 2007 Nov 1.

The vasorelaxant effect of HM-5 was mediated through opening of potassium channel (4-AP) and altering intracellular calcium by partial inhibition of Ca2+ influx through L-type voltage-operated Ca2+ channels and intracellular Ca2+ stores.
In endothelium-denuded coronary artery rings, the vasorelaxant effect of HM-5 was inhibited by a potassium channel blocker, TEA (10 mM), and 4-aminopyridine (4-AP, a K (v) blocker; 1 mM) but not by other K+ channel blockers such as iberiotoxin (100 nM), barium chloride (100 microM) and glibenclamide (10 microM).
1(0,0,0,1) Details
14976323 Erdos B, Simandle SA, Snipes JA, Miller AW, Busija DW: Potassium channel dysfunction in cerebral arteries of insulin-resistant rats is mediated by reactive oxygen species. Stroke. 2004 Apr;35(4):964-9. Epub 2004 Feb 19.

Blockade of the K (ir) and K (v) channels with Ba2+ and 4-aminopyridine, respectively, constricted the MCAs in both experimental groups with no significant difference.
1(0,0,0,1) Details
19272127 Shih HC, Hsu CS, Yang LL: In vitro study of the tocolytic effect of oroxylin A from Scutellaria baicalensis root. J Biomed Sci. 2009 Mar 4;16:27.

Contractions of the uterus were induced with acetylcholine (Ach) (1 microM), PGF2alpha (0.1 microM), oxytocin (10-3 U/ml), KCl (56.3 mM), tetraethylammonium (TEA; 1 and 10 mM), 4-aminopyridine (4-AP; 5 mM), glipizide (30 microM), a nitric oxide synthase (NOS) inhibitor (LNNA; 10-3M), a beta-receptor blocker (propranolol; 10 microM), and a cyclooxygenase inhibitor (indomethacin; 60 microM).
Otherwise, oroxylin A-mediated relaxation of the rat uterus might occur through opening of uterine calcium-dependent potassium channels or adenosine triphosphate potassium channel activation.
1(0,0,0,1) Details
19680683 Schilling T, Eder C: Lysophosphatidylcholine- and MCP-1-induced chemotaxis of monocytes requires potassium channel activity. Pflugers Arch. 2009 Nov;459(1):71-7. Epub 2009 Aug 14.

Inhibition of voltage-gated K+ channels with 4-aminopyridine or margatoxin partially inhibited MCP-1- and LPC-stimulated migration of monocytes.
1(0,0,0,1) Details
11588124 Matsumoto S, Nishikawa T, Yoshida S, Ikeda M, Tanimoto T, Saiki C, Takeda M: Effects of potassium channel and Na+-Ca2+ exchange blockers on the responses of slowly adapting pulmonary stretch receptors to hyperinflation in flecainide-treated rats. Br J Pharmacol. 2001 Oct;134(3):682-90.

The effects of K (+) channel blockers, such as 4-aminopyridine (4-AP) and tetraethylammonium (TEA), and a reverse-mode Na (+)-Ca (2+) exchange blocker, 2-[2-[4-(4-nitrobenzyloxyl) phenyl] ethyl] isothiourea methanesulphonate (KB-R7943), on the responses of slowly adapting pulmonary stretch receptor activity to hyperinflation (inflation volume=3 tidal volumes) were investigated in anaesthetized, artificially ventilated, unilaterally vagotomized rats after pretreatment with a Na (+) channel blocker flecainide.
1(0,0,0,1) Details
18930118 Su T, Cong WD, Long YS, Luo AH, Sun WW, Deng WY, Liao WP: Altered expression of voltage-gated potassium channel 4.2 and voltage-gated potassium channel 4-interacting protein, and changes in intracellular calcium levels following lithium-pilocarpine-induced status epilepticus. Neuroscience. 2008 Dec 2;157(3):566-76. Epub 2008 Sep 27.

In this study, we investigated whether the expression of the Kv4.2 channel and of its major modulator, voltage-dependent potassium channel-interacting protein (KChIP1), is altered following lithium-pilocarpine induced status epilepticus (SE) and the chronic-epilepsy phase in the rat model.
We compared the difference in 4-aminopyridine (4-AP)-induced intracellular calcium ([Ca (2+)] i) elevation between model and control brain slices.
1(0,0,0,1) Details
12168055 Abdul M, Hoosein N: Voltage-gated potassium ion channels in colon cancer. . Oncol Rep. 2002 Sep-Oct;9(5):961-4.

Potassium channel (PC) openers, minoxidil and diazoxide (5-50 microg/ml), increased growth of SW1116, LoVo, Colo320DM and LS174t human colon cancer cell lines by 20-40%.
PC-blockers such as glibenclamide inhibited cellular proliferation at concentrations above 50 microg/ml while tetraethylammonium and 4-aminopyridine (up to 100 microg/ml) did not have significant growth-suppressive effects.
1(0,0,0,1) Details
14504065 Williams BA, Buckler KJ: Biophysical properties and metabolic regulation of a TASK-like potassium channel in rat carotid body type 1 cells. Am J Physiol Lung Cell Mol Physiol. 2004 Jan;286(1):L221-30. Epub 2003 Sep 22.

1(0,0,0,1) Details
12223577 Bailey TW, Jin YH, Doyle MW, Andresen MC: Vanilloid-sensitive afferents activate neurons with prominent A-type potassium currents in nucleus tractus solitarius. J Neurosci. 2002 Sep 15;22(18):8230-7.

Our results suggest that the potassium-channel differences of second-order NTS neurons contribute to the differential processing of A- and C-type cranial visceral afferents beginning as early as this first central neuron.
Steady-state currents were similar in both groups. 4-Aminopyridine or depolarized conditioning blocked the TOC, but tetraethylammonium had no effect.
1(0,0,0,1) Details
18365869 Rampino T, Gregorini M, Guidetti C, Broggini M, Marchini S, Bonomi R, Maggio M, Roscini E, Soccio G, Tiboldo R, Dal Canton A: KCNA1 and TRPC6 ion channels and NHE1 exchanger operate the biological outcome of HGF/scatter factor in renal tubular cells. Growth Factors. 2007 Dec;25(6):382-91.

In previous study, we found that HGF upregulated in epithelial tubular cell line (HK2) 3 genes: potassium channel KCNA1, calcium channel (transient receptor potential channel, subfamily C, member 6, TRPC6) and Na (+)/H (+) exchanger-1 (NHE1).
To investigate whether KCNA1, TRPC6, NHE1 mediate the changes induced by HGF in HK2, we studied the effects of their inhibitors: 4-aminopyridine, charybdotoxin, dendrotoxin K inhibitors of KCNA1, lanthanum, N-(p-amylcinnamoyl) anthranilic acid inhibitors of TRPC6, 5-(N-ethyl-N-isopropyl) amiloride, cariporide inhibitors of NHE1.
1(0,0,0,1) Details
11531164 Nevala R, Paukku K, Korpela R, Vapaatalo H: Calcium-sensitive potassium channel inhibitors antagonize genistein- and daidzein-induced arterial relaxation in vitro. Life Sci. 2001 Aug 10;69(12):1407-17.

The antagonists of voltage-dependent K+-channels (K (V)) (4-aminopyridine), ATP-sensitive K+-channels (K (ATP)) (glibenclamide), or inward rectifier K+-channels (KIR) (barium) had no effect on the relaxation responses of any of the compounds studied.
1(0,0,0,1) Details
15644941 Salapatek AM, Ji J, Muinuddin A, Diamant NE: Potassium channel diversity within the muscular components of the feline lower esophageal sphincter. Can J Physiol Pharmacol. 2004 Nov;82(11):1006-17.

There was a large reduction in outward current with 4-aminopyridine (4-AP) in sling muscle, while BKCa blockers had a limited effect on the voltage-activated outward current in sling muscle.
1(0,0,0,1) Details
10743627 Wohlrab D, Hein W: [Effect of ion channel modulators on the membrane potential of human chondrocytes]. Orthopade. 2000 Feb;29(2):80-4.


A connection between the potassium channel activity and the proliferation has been detected in different human cell systems.
1(0,0,0,1) Details
11744755 Daniel H, Crepel F: Control of Ca (2+) influx by cannabinoid and metabotropic glutamate receptors in rat cerebellar cortex requires K (+) channels. J Physiol. 2001 Dec 15;537(Pt 3):793-800.


Bath application of the potassium channel blocker 4-AP (1 mM) totally prevented both the WIN55,212-2- and the L-AP4-induced inhibition of peak fluorescence transients evoked by parallel fibre stimulation. 5.
1(0,0,0,1) Details
12840158 van Lunteren E, Moyer M: Sternohyoid muscle fatigue properties of dy/dy dystrophic mice, an animal model of merosin-deficient congenital muscular dystrophy. Pediatr Res. 2003 Oct;54(4):547-53. Epub 2003 Jul 2.


The potassium-channel blocker, 3,4-diaminopyridine, increased force of dy/dy sternohyoid muscle during twitch and 25-Hz contractions by 148 +/- 20% (p < 0.00001) and 109 +/- 18% (p < 0.00002), respectively.
1(0,0,0,1) Details
11341793 Gosche JR: Oxygen dilation in fetal pulmonary arterioles: role of K (+) channels. J Surg Res. 2001 May 15;97(2):159-63.

We have examined the effect of potassium channel blockers on oxygen-induced vasodilation in isolated pulmonary arterioles from fetal rats at term.
Responses were recorded in the absence of blockers (controls) or in the presence of a voltage-gated K (+) channel (K (v)) blocker, 4-aminopyridine; an ATP-sensitive K (+) channel (K (ATP)) blocker, glibenclamide; a Ca (2+)-activated K (+) channel (K (Ca)) blocker, charybdotoxin; or a nonspecific K (+) channel blocker, tetraethylammonium.
1(0,0,0,1) Details
15157623 Glover CN, Bury NR, Hogstrand C: Intestinal zinc uptake in freshwater rainbow trout: evidence for apical pathways associated with potassium efflux and modified by calcium. Biochim Biophys Acta. 2004 May 27;1663(1-2):214-21.


The potassium channel blocker, tetraethylammonium chloride inhibited zinc uptake at this relatively high zinc concentration, suggesting the presence of a low affinity zinc uptake pathway linked to potassium efflux.
1(0,0,0,1) Details
11691539 Tahara S, Fukuda K, Kodama H, Kato T, Miyoshi S, Ogawa S: Potassium channel blocker activates extracellular signal-regulated kinases through Pyk2 and epidermal growth factor receptor in rat cardiomyocytes. J Am Coll Cardiol. 2001 Nov 1;38(5):1554-63.

METHODS: Primary cultured rat cardiomyocytes were stimulated with four different KBs-4-aminopyridine (4-AP), E-4031, tetra-ethylammonium and quinidine-and phosphorylation of ERK, proline-rich tyrosine kinase 2 (Pyk2) and epidermal growth factor receptor (EGFR) was detected.
1(0,0,0,1) Details
14614103 Ishikawa T, Nakamura Y, Saitoh N, Li WB, Iwasaki S, Takahashi T: Distinct roles of Kv1 and Kv3 potassium channels at the calyx of Held presynaptic terminal. J Neurosci. 2003 Nov 12;23(32):10445-53.

Despite identification of > 100 potassium channel subunits, relatively little is known about their roles in synaptic transmission.
IPK was composed of a 4-aminopyridine (4-AP)-sensitive component and a smaller 4-AP-insensitive component composed of an iberiotoxin-sensitive current and an unidentified slowly activating potassium current.
1(0,0,0,1) Details
14622907 Namba H, Takei N, Nawa H: Transforming growth factor-alpha changes firing properties of developing neocortical GABAergic neurons by down-regulation of voltage-gated potassium currents. Neuroscience. 2003;122(3):637-46.


Reverse transcription-polymerase chain reaction analysis of potassium channel mRNA in the bipolar neurons revealed that the reduction in the IK current density was caused by Kv2.2 mRNA down-regulation.
1(0,0,0,1) Details
19362348 Yildiz O, Seyrek M, Irkilata HC, Yildirim I, Tahmaz L, Dayanc M: Testosterone might cause relaxation of human corpus cavernosum by potassium channel opening action. Urology. 2009 Jul;74(1):229-32. Epub 2009 Apr 10.

Testosterone-induced responses were tested in the presence of nonselective, large, conductance Ca (2+)-activated and voltage-sensitive K (+) channel inhibitor tetraethylammonium (1 mM), adenosine triphosphate-sensitive K (+) channel inhibitor glibenclamide (10 microM), voltage-dependent inward rectifier K (+) channel inhibitor barium chloride (30 microM) and voltage-sensitive K (+) channel inhibitor 4-aminopyridine (1 mM).
1(0,0,0,1) Details
11811894 Matsumoto S, Yoshida S, Ikeda M, Nishikawa T, Saiki C, Takeda M: Effects of potassium channel blockers on hyperinflation-induced rapidly adapting pulmonary stretch receptor stimulation in the rabbit. Life Sci. 2001 Dec 21;70(5):491-501.

1(0,0,0,1) Details
18495797 Troncoso Brindeiro CM, Fallet RW, Lane PH, Carmines PK: Potassium channel contributions to afferent arteriolar tone in normal and diabetic rat kidney. Am J Physiol Renal Physiol. 2008 Jul;295(1):F171-8. Epub 2008 May 21.

The in vitro blood-perfused juxtamedullary nephron technique was utilized to quantify afferent arteriolar lumen diameter responses to K+ channel blockers: 0.1-3.0 mM 4-aminopyridine (4-AP; KV channels), 10-100 microM barium (KIR channels), 1-100 nM tertiapin-Q (TPQ; Kir1.1 and Kir3.x subfamilies of KIR channels), 100 nM apamin (SKCa channels), and 1 mM tetraethylammonium (TEA; BKCa channels).
1(0,0,0,1) Details
11483700 Cheong A, Dedman AM, Beech DJ: Expression and function of native potassium channel [K (V) alpha1] subunits in terminal arterioles of rabbit. J Physiol. 2001 Aug 1;534(Pt 3):691-700.

Current activated on depolarisation positive of about -45 mV and a large fraction of this current was blocked by 3,4-diaminopyridine (3,4-DAP) or 4-aminopyridine (4-AP), inhibitors of K (V) channels.
1(0,0,0,1) Details
10583910 Hendriks R, Morest DK, Kaczmarek LK: Shaw-like potassium currents in the auditory rhombencephalon throughout embryogenesis. J Neurosci Res. 1999 Dec 15;58(6):791-804.

The Shaw subfamily of potassium channel genes, including Kv3.1, are highly expressed within the auditory nuclei of the brainstem, where they have been implicated in the characteristic response properties of particular types of neurons.
Potassium currents carried by Kv3.1 are voltage-dependent, have a high activation threshold, are slow to inactivate, and are very sensitive to 4-aminopyridine (4-AP) and tetraethylammonium (TEA).
1(0,0,0,1) Details
14994186 Wong KL, Yang HY, Chan P, Cheng TH, Liu JC, Hsu FL, Liu IM, Cheng YW, Cheng JT: Isosteviol as a potassium channel opener to lower intracellular calcium concentrations in cultured aortic smooth muscle cells. Planta Med. 2004 Feb;70(2):108-12.

The attenuation by isosteviol of the vasopressin- and phenylephrine-induced increase in [Ca (2+)] i was inhibited by glibenclamide, apamin and 4-aminopyridine but not by charybdotoxin.
1(0,0,0,1) Details
19527707 Pagan RM, Martinez AC, Martinez MP, Hernandez M, Garcia-Sacristan A, Correa C, Prieto D, Benedito S: Endothelial and potassium channel dependent modulation of noradrenergic vasoconstriction in the pig radial artery. Eur J Pharmacol. 2009 Aug 15;616(1-3):166-74. Epub 2009 Jun 13.

Pre-incubation with tetraethylammonium and 4-aminopyridine, but not glibenclamide, enhanced these neurogenic responses.
1(0,0,0,1) Details
16472864 Judge SI, Bever CT Jr: Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment. Pharmacol Ther. 2006 Jul;111(1):224-59. Epub 2006 Feb 9.

To date, only 2 broad-spectrum K (+) channel blockers, 4-aminopyridine (4-AP) and 3,4-diaminopyridine (3,4-DAP), have been tested in MS patients.
1(0,0,0,1) Details
10716759 Yang Q, Kaji R, Hirota N, Kojima Y, Takagi T, Kohara N, Kimura J, Shibasaki H, Bostock H: Effect of maturation on nerve excitability in an experimental model of threshold electrotonus. Muscle Nerve. 2000 Apr;23(4):498-506.

These findings indicate that mature rats (> 400 g) may provide a useful experimental model for interpreting abnormal TE responses in humans, and provide evidence for nonlinear maturation of potassium channel function in myelinated axons.
In contrast, TEd (10-20) gradually decreased up to 330 g, and then jumped to a higher level, which was maintained for animals of > 400 g. 4-Aminopyridine, a blocker of fast potassium channels, selectively increased TEd (10-20) only in the immature or young (<330 g) rats.
1(0,0,0,1) Details
15879679 Matsuda T, Takeda K, Ito M, Yamagishi R, Tamura M, Nakamura H, Tsuruoka N, Saito T, Masumiya H, Suzuki T, Iida-Tanaka N, Itokawa-Matsuda M, Yamashita T, Tsuruzoe N, Tanaka H, Shigenobu K: Atria selective prolongation by NIP-142, an antiarrhythmic agent, of refractory period and action potential duration in guinea pig myocardium. J Pharmacol Sci. 2005 May;98(1):33-40. Epub 2005 May 7.

In the present study, we examined the effects of NIP-142 on isolated guinea pig myocardium and on the G-protein-coupled inwardly rectifying potassium channel current (acetylcholine-activated potassium current; I (KACh)) expressed in Xenopus oocytes.
E-4031 and 4-aminopyridine prolonged action potential duration in both left atrium and right ventricle.
1(0,0,0,1) Details
12388256 Hampl V, Bibova J, Stranak Z, Wu X, Michelakis ED, Hashimoto K, Archer SL: Hypoxic fetoplacental vasoconstriction in humans is mediated by potassium channel inhibition. Am J Physiol Heart Circ Physiol. 2002 Dec;283(6):H2440-9. Epub 2002 Aug 22.

HFPV and 4-aminopyridine, an inhibitor of voltage-dependent K (+) (K (v)) channels, increased pressure in a nonadditive manner, suggesting they act via a common mechanism.
1(0,0,0,1) Details
17659475 Mathie A, Veale EL: Therapeutic potential of neuronal two-pore domain potassium-channel modulators. Curr Opin Investig Drugs. 2007 Jul;8(7):555-62.

Although not inhibited by classical potassium channel-blocking drugs, such as tetraethylammonium and 4-aminopyridine, K2P channels are regulated by a diverse array of pharmacological mediators.
1(0,0,0,1) Details
12072589 Bardou M, Goirand F, Bernard A, Guerard P, Gatinet M, Devillier P, Dumas JP, Morcillo EJ, Rochette L, Dumas M: Relaxant effects of selective phosphodiesterase inhibitors on U46619 precontracted human intralobar pulmonary arteries and role of potassium channels. J Cardiovasc Pharmacol. 2002 Jul;40(1):153-61.

All PDEI tested induced a concentration-dependent relaxation with theophylline being significantly (p < 0.05) more efficient and rolipram more potent than PDE5I and PDE3I (Emax values, expressed as a percentage of maximal relaxation by papaverine 10 (-4) M, were 92% +/- 2%, 84% +/- 8%, 90% +/- 4% and 99% +/- 1%, and pD2 values were 7.30 +/- 0.35, 6.14 +/- 0.25, 5.86 +/- 0.17, and 4.85 +/- 0.47 for rolipram, siguazodan, zaprinast and theophylline, respectively). 4-Aminopyridine (4-AP, Kv, voltage dependent channel blocker, 1 mM) induced a significant increase (+17% p < 0.05) of U46619-induced vasoconstriction whereas the other K+-channels blockers, glibenclamide (KATP channels, 1 microM) charybdotoxin (predominant BKCa, large conductance Ca2+-sensitive K+ channels, 0.1 microM) and apamine (SKCa, small conductance, 0.3 microM) were without effect.
None of the potassium channel blockers displaced the CRC for zaprinast and theophylline.
1(0,0,0,1) Details
16769957 Lorenz D, Hagen K, Ufer M, Cascorbi I, Deuschl G, Volkmann J: No benefit of 3,4-diaminopyridine in essential tremor: a placebo-controlled crossover study. Neurology. 2006 Jun 13;66(11):1753-5.


3,4-Diaminopyridine (3,4-DAP) is a potassium channel blocker that has recently demonstrated an antioscillatory effect in humans by significantly reducing downbeat nystagmus.
1(0,0,0,1) Details
10634895 Vyshedskiy A, Lin JW: Presynaptic Ca (2+) influx at the inhibitor of the crayfish neuromuscular junction: a photometric study at a high time resolution. J Neurophysiol. 2000 Jan;83(1):552-62.


Gradual changes in potassium channel block allowed us to estimate the calcium cooperativity of transmitter release over a 10-fold range in presynaptic calcium influx.
1(0,0,0,1) Details
12535634 Wu MM, Gao PJ, Jiao S, Zhu DL, Zang ZH, Mei YA: TGF-beta1 induces the expression of fast inactivating K+ (I (A)) channels in rat vascular myofibroblasts. Biochem Biophys Res Commun. 2003 Jan 31;301(1):17-23.

In myofibroblasts, induced by the treatment of fibroblasts with TGF-beta1, we report the emergence of an additional transient outward K (+) current The TGF-beta1-induced outward current is inhibited by 4-aminopyridine.
K (V2.1), the transcript for a non-inactivating potassium channel gene, was detected by quantitative RT-PCT in both cultured fibroblasts and myofibroblasts.
1(0,0,0,1) Details
16914430 Wareing M, Bai X, Seghier F, Turner CM, Greenwood SL, Baker PN, Taggart MJ, Fyfe GK: Expression and function of potassium channels in the human placental vasculature. Am J Physiol Regul Integr Comp Physiol. 2006 Aug;291(2):R437-46. Epub 2006 Mar 2.

The expression of voltage-gated (Kv) 2.1, KV9.3, large-conductance Ca2+-activated K channel (BKCa), inward-rectified K+ channel (KIR) 6.1, and two-pore domain inwardly rectifying potassium channel-related acid-sensitive K channels (TASK) 1 in chorionic plate arteries, veins, and placental homogenate was assessed by RT-PCR and Western blot analysis.
Functional activity of K channels was assessed pharmacologically in small chorionic plate arteries and veins by wire myography using 4-aminopyridine, iberiotoxin, pinacidil, and anandamide.
1(0,0,0,1) Details
17687001 Bai X, Ma J, Pan Z, Song YH, Freyberg S, Yan Y, Vykoukal D, Alt E: Electrophysiological properties of human adipose tissue-derived stem cells. Am J Physiol Cell Physiol. 2007 Nov;293(5):C1539-50. Epub 2007 Aug 8.

The I (KDR) was inhibited by tetraethyl ammonium (TEA) and 4-aminopyridine (4-AP), which significantly reduced the proliferation of hASCs in a dose-dependent manner (P < 0.05), as suggested by bromodeoxyurindine (BrdU) incorporation.
Other selective potassium channel blockers, including linopiridine, iberiotoxin, clotrimazole, and apamin also significantly inhibited I (KDR).
1(0,0,0,1) Details
10553805 Moon DG, Lee DS, Kim JJ: Altered contractile response of penis under hypoxia with metabolic acidosis. Int J Impot Res. 1999 Oct;11(5):265-71.


The changes of intracavernous pressure (ICP) to erectogenic agents (acetylcholine, L-arginine, prostaglandin E1: PGE1), erectolytic agents (epinephrine, thromboxane A2; TXA2), K channel-related drugs (pinacidil, 4-aminopyridine, tetraethylammonium; TEA, glibenclamide) and calcium ionophore were monitored at Set 1 (PO2 > 60 mmHg, pH > 7.25), Set 2 (PO2 < 30 mmHg, 7.25 > pH > 7.0), Set 3 (PO2 < 30 mmHg, pH < 7.0), and Set 4 (PO2 > 60 mmHg, pH < 7.0) in vivo.
0(0,0,0,0) Details
11374879 Denda M, Ashida Y, Inoue K, Kumazawa N: Skin surface electric potential induced by ion-flux through epidermal cell layers. Biochem Biophys Res Commun. 2001 Jun 1;284(1):112-7.


Skin surface barrier disruption reduced the potential and calcium and potassium channel blockers partially prevented the decrease.
1(0,0,0,1) Details
17076688 Novakovic A, Bukarica LG, Kanjuh V, Heinle H: Potassium channels-mediated vasorelaxation of rat aorta induced by resveratrol. Basic Clin Pharmacol Toxicol. 2006 Nov;99(5):360-4.


We used different potassium channel inhibitors to determine whether the K (+) channels mediated endothelium-independent relaxation of rat aorta induced by resveratrol.
1(0,0,0,1) Details
12296855 Qiu MR, Campbell TJ, Breit SN: A potassium ion channel is involved in cytokine production by activated human macrophages. Clin Exp Immunol. 2002 Oct;130(1):67-74.


We have previously implicated an outwardly rectifying potassium channel (Kor) in this process and for this reason we have investigated the role of potassium (K+) and K+ channels in the regulation of tumour necrosis factor-alpha (TNF-alpha) and interleukin (IL)-8 production by activated human culture-derived macrophages.
1(0,0,0,1) Details
10586958 Bringmann A, Francke M, Pannicke T, Biedermann B, Faude F, Enzmann V, Wiedemann P, Reichelt W, Reichenbach A: Human Muller glial cells: altered potassium channel activity in proliferative vitreoretinopathy. Invest Ophthalmol Vis Sci. 1999 Dec;40(13):3316-23.

1(0,0,0,1) Details
17510187 Bailey TW, Hermes SM, Whittier KL, Aicher SA, Andresen MC: A-type potassium channels differentially tune afferent pathways from rat solitary tract nucleus to caudal ventrolateral medulla or paraventricular hypothalamus. J Physiol. 2007 Jul 15;582(Pt 2):613-28. Epub 2007 May 17.

Since intrinsic properties impact information transmission, here we evaluated potassium channel expression and somatodendritic morphology of projection neurons and their relation to afferent information output directed to PVN or CVLM pathways.
However, only PVN-projecting NTS neurons displayed large transient, 4-aminopyridine-sensitive, A-type currents (IKA).
1(0,0,0,1) Details
16088387 Frieling H, Grundling M, Lauer KS, Wendt M, Hachenberg T, Lehmann C, Pavlovic D: Intraperitoneal instillation of polihexanide produces hypotension and vasodilation: in vivo and in vitro study in rats. Int J Colorectal Dis. 2006 May;21(4):373-80. Epub 2005 Oct 26.

The relaxing effect of polihexanide (aortae -endothelium) was not affected by K (+)-channel blocking agents charybdotoxin, tetraethylammoniumchloride, glibenclamide or 4-aminopyridine, while polihexanide had no effects on 40-mM KCl contractions.
CONCLUSION: This implies that polihexanide may promote nitric oxide liberation, potassium channel activation and vasodilation that may result in hypotension.
1(0,0,0,1) Details
11248242 Decher N, Maier M, Dittrich W, Gassenhuber J, Bruggemann A, Busch AE, Steinmeyer K: Characterization of TASK-4, a novel member of the pH-sensitive, two-pore domain potassium channel family. FEBS Lett. 2001 Mar 9;492(1-2):84-9.

TASK-4 currents were efficiently blocked by barium (83% inhibition at 2 mM), only weakly inhibited by 1 mM concentrations of quinine, bupivacaine and lidocaine, but not blocked by tetraethylammonium, 4-aminopyridine and Cs (+).
1(0,0,0,1) Details
11568792 Fulep EE, Vedernikov YP, Saade GR, Garfield RE: The role of endothelium-derived hyperpolarizing factor in the regulation of the uterine circulation in pregnant rats. Am J Obstet Gynecol. 2001 Sep;185(3):638-42.

RESULTS: The decrease in perfusion pressure induced by endothelium-derived hyperpolarizing factor was significantly attenuated by 4-aminopyridine and was abolished by a combination of 4-aminopyridine and tetraethylammonium.
CONCLUSION: In the pregnant rat uterine vascular beds, endothelium-derived hyperpolarizing factor release is activated by a delayed rectifier type of voltage-sensitive potassium channel.
1(0,0,0,1) Details