| Name | AP 4 |
|---|---|
| Synonyms | AP 4; AP4; Activating enhancer binding protein 4; TFAP 4; TFAP4; Transcription factor AP 4; Transcription factor AP4; transcription factor AP 4 (activating enhancer binding protein 4)… |
| Name | 4-aminopyridine |
|---|---|
| CAS | 4-pyridinamine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 12617942 | Zheng F, Johnson SW: Metabotropic glutamate and muscarinic cholinergic receptor-mediated preferential inhibition of component of transmissions in rat ventral tegmental area. Neuroscience. 2003;116(4):1013-20. Intracellular voltage clamp recordings were made from neurons in rat ventral tegmental area in slice preparations. (+/-)-1-Aminocyclopentane-trans-1,3-dicarboxylic acid (agonist for groups I and II metabotropic glutamate receptors) and L (+)-2-amino-4-phosphonobutyric acid (L-AP4; agonist for group III metabotropic glutamate receptors) were significantly more potent for inhibiting N-methyl-D-aspartate receptor-mediated excitatory postsynaptic currents, as compared with inhibition of excitatory postsynaptic currents mediated by alpha-amino-3--5-methyl-4-isoxazolepropionic acid receptors. Interestingly, the release stimulator 4-aminopyridine (30 microM) and the uptake inhibitor L-anti-endo-3,4-methanopyrrolidine dicarboxylate (300 microM) preferentially increased the amplitude of excitatory postsynaptic currents.Thus, agonists for metabotropic and muscarinic cholinergic receptors act presynaptically to cause a preferential reduction in the component of excitatory synaptic transmissions. |
2(0,0,0,2) | 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 selective mGluR4 agonist L-AP4 (100 microM) also caused a transient decrease in the peak amplitude of the fluorescence transients evoked by parallel fibre stimulation. 4. |
2(0,0,0,2) | Details |
| 10733605 | Andreani A, Leoni A, Locatelli A, Morigi R, Rambaldi M, Pietra C, Villetti G: 4-Aminopyridine derivatives with antiamnesic activity. Eur J Med Chem. 2000 Jan;35(1):77-82. (Ach) enhancement, useful in the treatment of Alzheimer's disease (AD), may be obtained by means of ion channel modulators such as 4-aminopyridine (4-AP). 4-AP is also the central ring of tacrine, the first drug approved for the treatment of AD. |
6(0,0,1,1) | Details |
| 10852214 | Lefebvre C, Fisher K, Cahill CM, Coderre TJ: Evidence that -induced nociception depends on release from primary afferent C-fibres. Neuroreport. 2000 Jun 5;11(8):1631-5. Pretreatment with drugs that have been shown to inhibit release, including a group II metabotropic glutamate receptor (mGluR) agonist (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylate ((2R,4R)-APDC), a group III mGluR agonist L-2-amino-4-phosphonobutyrate (L-AP4), or the use-dependent sodium channel blockers 3,5-diamino-6-(2,3-diclorophenyl)-1,2,4-triazine and 2-amino-6-trifluoromethoxybenzothiazole (riluzole), produced dose-dependent reductions in (RS)--induced SNBs. We have also shown that incubation of rat lumbar spinal cord slices with (RS)- potentiates 4-aminopyridine-evoked (4-AP) release of |
1(0,0,0,1) | Details |
| 15803964 | Kucukhuseyin C, Bozan G: Modulation by 4-aminopyridine and on the effect of on isolated spontaneously beating rat atria. J Basic Clin Physiol Pharmacol. 2004;15(3-4):289-302. RESULTS: (0.3-100 microg/ml) dose-dependently depressed both the beating frequency and contractility, more powerfully on the latter. 4-AP (4 mM) and Ca2+ (3.6 mM or 400 microg/ml) respectively increased force of contraction (203.4% and 199.3%) and spontaneous beating frequency (104.9% and 111.3%). 4-AP and Ca2+ significantly antagonized the inhibitory actions of on cardiac processes, more strongly on contractility and with 4-AP more potent than Ca2+. |
1(0,0,0,1) | Details |
| 11682450 | Ghisdal P, Morel N: Cellular target of voltage and -dependent K (+) channel blockers involved in EDHF-mediated responses in rat superior mesenteric artery. Br J Pharmacol. 2001 Nov;134(5):1021-8. In arteries contracted with prostaglandin F (2 alpha) (2.5 - 10 microM), relaxation evoked by (0.01 - 3 microM) was abolished by a combination of charybdotoxin (ChTX, 0.1 microM) plus apamin (Apa, 0.1 microM) and was inhibited by 68+/-6% (n=6) by 4-aminopyridine (4-AP, 5 mM). 3. It was decreased by 66+/-5% (n=6) by 4-AP. 4. |
1(0,0,0,1) | Details |
| 11773238 | Hirasawa H, Shiells R, Yamada M: A metabotropic glutamate receptor regulates transmitter release from cone presynaptic terminals in carp retinal slices. J Gen Physiol. 2002 Jan;119(1):55-68. The selective agonist for group III mGluRs, l-2-amino-4-phosphonobutyrate (L-APB or L-AP4; 20 microM), reduced the sEPSC rate with a slight reduction in amplitude, which is consistent with a presynaptic action on cone synaptic terminals to reduce transmitter release. During L-APB application, recovery of sEPSC rate occurred with 500 microM (s)-2-methyl-2-amino-4-phosphonobutyrate (MAP4), a selective antagonist of group III mGluR, and with 200 microM 4-aminopyridine (4-AP), a blocker of voltage-dependent channels. |
1(0,0,0,1) | Details |
| 11906950 | Wittmann S, Frohlich D, Daniels S: Characterization of the human fMLP receptor in neutrophils and in Xenopus oocytes. Br J Pharmacol. 2002 Mar;135(6):1375-82. The slow current showed weak inward rectification, was Ca (2+)-dependent and blocked by Cd (2+), 4-AP (4-aminopyridine) and haloperidol, suggesting activation of a mixed population of cation channels. 4. |
1(0,0,0,1) | Details |
| 12740033 | Li Y, Ganta S, von Stein FB, Mason DE, Mitchell BM, Freeman LC: 4-aminopyridine decreases production by porcine granulosa cells. Reprod Biol Endocrinol. 2003 Apr 1;1:31. Addition of either 8-CPT-cAMP or estradiol 17beta to serum-supplemented primary cultures reduced the inhibitory effects of 4-AP. 4-AP treatment was also associated with increased cell size, increased intracellular concentration, and hyperpolarization of resting membrane potential. |
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 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- (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. Unlike 4-AP, 4-AP-3-MeOH can restore axonal conduction without changing axonal electrophysiological properties. |
1(0,0,0,1) | Details |
| 10930547 | Tiwari JK, Sikdar SK: The kinetics of a non-inactivating K (+) current in alphaT3-1 pituitary gonadotropes is not affected by holding potential. Brain Res. 2000 Aug 11;873(2):218-24. The activation kinetics of the whole-cell currents and the gating charge measured from holding potential (V (HOLD)) of -10 mV, V (HOLD)=-80 mV in presence of 4-AP (4-aminopyridine), and V (HOLD)=-10 mV with a hyperpolarizing prepulse to -80 mV were similar. |
1(0,0,0,1) | Details |
| 11155211 | Bal R, Janahmadi M, Green GG, Sanders DJ: Two kinds of transient outward currents, I (A) and I (Adepol), in F76 and D1 soma membranes of the subesophageal ganglia of Helix aspersa. J Membr Biol. 2001 Jan 1;179(1):71-8. The separation of these two current components was based on activation and steady-state inactivation curves, holding potentials and sensitivity to 4-aminopyridine (4-AP). It was found that I (Adepol) was more sensitive than I (A) to 4-AP. 4-AP at a concentration of 1 mm blocked I (Adepol) completely, whereas 5-6 mm 4-AP was needed to block I (A) completely. |
1(0,0,0,1) | Details |
| 19605735 | Straub SV, Girouard H, Doetsch PE, Hannah RM, Wilkerson MK, Nelson MT: Regulation of intracerebral arteriolar tone by K (v) channels: effects of glucose and PKC. Am J Physiol Cell Physiol. 2009 Sep;297(3):C788-96. Epub 2009 Jul 15. Isolated, pressurized parenchymal arterioles and arterioles in cortical brain slices exhibited robust constriction in the presence of the K (v) channel inhibitor 4-aminopyridine (4-AP). 4-AP also decreased the amplitude of K (v) currents recorded from SMCs. |
31(0,1,1,1) | Details |
| 15733086 | Larkman PM, Perkins EM: A TASK-like pH- and amine-sensitive 'leak' K+ conductance regulates neonatal rat facial motoneuron excitability in vitro. Eur J Neurosci. 2005 Feb;21(3):679-91. Ba2+, Cs+ and Rb+ blocked I (NA) and I (pH) voltage-dependently with maximal block at hyperpolarized potentials. 4-Aminopyridine (4-AP, 4 mM) voltage-independently blocked I (NA) and I (pH). |
31(0,1,1,1) | Details |
| 11801366 | Doi A, Ishibashi H, Jinno S, Kosaka T, Akaike N: Presynaptic inhibition of GABAergic miniature currents by metabotropic glutamate receptor in the rat CNS. Neuroscience. 2002;109(2):299-311. The application of K+ channel blockers such as 4-aminopyridine, Cs+, Ba2+ or tetraethylammonium increased the mIPSC frequency, but failed to inhibit the tACPD action on mIPSC. |
0(0,0,0,0) | Details |
| 19850918 | Wu ZZ, Li DP, Chen SR, Pan HL: Aminopyridines potentiate synaptic and neuromuscular transmission by targeting the voltage-activated calcium channel beta subunit. J Biol Chem. 2009 Dec 25;284(52):36453-61. Epub 2009 Oct 22. Aminopyridines such as 4-aminopyridine (4-AP) are widely used as voltage-activated K (+) (Kv) channel blockers and can improve neuromuscular function in patients with spinal cord injury, myasthenia gravis, or multiple sclerosis. |
0(0,0,0,0) | Details |
| 16815680 | Motamedi GK, Salazar P, Smith EL, Lesser RP, Webber WR, Ortinski PI, Vicini S, Rogawski MA: Termination of epileptiform activity by cooling in rat hippocampal slice epilepsy models. Epilepsy Res. 2006 Aug;70(2-3):200-10. Epub 2006 Jul 3. We induced spontaneous epileptiform activity in rat brain slices by exposure to 4-aminopyridine (4-AP), 4-AP plus bicuculline, and Mg (2+)-free artificial CSF (aCSF) at 28-34 degrees C. |
6(0,0,1,1) | Details |