Protein Information

Name acetylcholine receptor (protein family or complex)
Synonyms Acetylcholine receptor; Acetylcholine receptors

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
15145336 Burke G, Cossins J, Maxwell S, Robb S, Nicolle M, Vincent A, Newsom-Davis J, Palace J, Beeson D: Distinct phenotypes of congenital acetylcholine receptor deficiency. Neuromuscul Disord. 2004 Jun;14(6):356-64.

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14976404 Shi H, Wang H, Li D, Nattel S, Wang Z: Differential alterations of receptor densities of three muscarinic acetylcholine receptor subtypes and current densities of the corresponding K+ channels in canine atria with atrial fibrillation induced by experimental congestive heart failure. Cell Physiol Biochem. 2004;14(1-2):31-40.

Whole-patch-clamp recordings showed that the current densities of IKACh (induced by 1 mM acetylcholine) and IK4AP (induced by 1 mM 4-aminopyridine) were n45% and n55% lower, respectively, while that of IKM3 (induced by 10 mM choline) was n75% higher, at a plateau voltage of 0 mV in atrial myocytes from CHF than those from healthy hearts.
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19172815 Ishigaki K, Murakami T, Ito Y, Yanagisawa A, Kodaira K, Shishikura K, Suzuki H, Hirayama Y, Osawa M: [Treatment approach to congenital myasthenic syndrome in a patient with acetylcholine receptor deficiency]. No To Hattatsu. 2009 Jan;41(1):37-42.

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12213259 Wong JY, Ross SA, McColl C, Massalas JS, Powney E, Finkelstein DI, Clark M, Horne MK, Berkovic SF, Drago J: Proconvulsant-induced seizures in alpha (4) nicotinic acetylcholine receptor subunit knockout mice. Neuropharmacology. 2002 Jul;43(1):55-64.

We investigated the response of alpha (4) nAChR subunit knockout mice to the gamma-aminobutyric acid (GABA) receptor antagonists; pentylenetetrazole (PTZ) and bicuculline (BIC), the glutamate receptor agonist kainic acid (KA), the glycine receptor antagonist strychnine and the K (+) channel blocker 4-aminopyridine (4-AP).
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17206662 Sha SJ, Layzer RB: Myasthenia gravis and Lambert-Eaton myasthenic syndrome in the same patient. Muscle Nerve. 2007 Jul;36(1):115-7.


Antibodies to the acetylcholine receptor were found in her serum, but electrodiagnostic testing showed abnormalities typical of the Lambert-Eaton myasthenic syndrome (LEMS).
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15036330 Banwell BL, Ohno K, Sieb JP, Engel AG: Novel truncating RAPSN mutations causing congenital myasthenic syndrome responsive to 3,4-diaminopyridine. Neuromuscul Disord. 2004 Mar;14(3):202-7.


Rapsyn is essential for clustering the acetylcholine receptor at the postsynaptic membrane of the neuromuscular junction.
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12624181 Urbano FJ, Piedras-Renteria ES, Jun K, Shin HS, Uchitel OD, Tsien RW: Altered properties of quantal neurotransmitter release at endplates of mice lacking P/Q-type Ca2+ channels. Proc Natl Acad Sci U S A. 2003 Mar 18;100(6):3491-6. Epub 2003 Mar 6.


Changes in presynaptic function were also associated with a significant reduction in the size of postsynaptic acetylcholine receptor clusters.
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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.
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16338999 Bandyopadhyay S, Sutor B, Hablitz JJ: Endogenous acetylcholine enhances synchronized interneuron activity in rat neocortex. J Neurophysiol. 2006 Mar;95(3):1908-16. Epub 2005 Dec 7.

Application of 4-aminopyridine (4-AP) along with EAA) receptor antagonists produces gamma-aminobutyric acid (GABAA) receptor-dependent synchronized activity in interneurons.
Because interneurons in the neocortex are excited by nicotinic acetylcholine receptor (nAChR) agonists, ACh may influence synchronization of these local neocortical interneuronal networks.
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19166510 Grilli M, Zappettini S, Zoli M, Marchi M: Pre-synaptic nicotinic and D receptors functionally interact on dopaminergic nerve endings of rat and mouse nucleus accumbens. J Neurochem. 2009 Mar;108(6):1507-14. Epub 2009 Feb 16.

The aim of the present work was to investigate whether acetylcholine receptors (nAChRs) and dopamine (DA) autoreceptors, which are both able to modulate DA release, functionally interact on the same nerve endings.
Both nicotinic agonists and 4-aminopyridine (4-AP) provoked [(3) H] DA release which was inhibited by quinpirole and blocked by sulpiride and raclopride.
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10849677 Shirahata M, Ishizawa Y, Rudisill M, Sham JS, Schofield B, Fitzgerald RS: Acetylcholine sensitivity of cat petrosal ganglion neurons. . Adv Exp Med Biol. 2000;475:377-87.

We investigated if neuronal nicotinic acetylcholine receptors (nAChRs) are localized in chemoreceptor afferent neurons in the cat petrosal ganglion (PG) and if acetylcholine (ACh) excites chemoreceptor afferent neurons.
Outward current was blocked by 4-aminopyridine (4-AP) and sometimes by atropine.
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12649591 Shi H, Yang B, Xu D, Wang H, Wang Z: Electrophysiological characterization of cardiac muscarinic acetylcholine receptors: different subtypes mediate different potassium currents. Cell Physiol Biochem. 2003;13(2):59-74.

Tetramethylammonium (0.5 mM) activated a K+ conductance with delayed rectifying properties (I (KM3)) and the currents were highly sensitive to 4-diphenylacetoxy-N-methylpiperidine methiodide (2 nM, an M3 receptor inhibitor). 4-aminopyridine (1 mM) induced a delayed rectifier-like current (I (K4AP)) which was selectively suppressed by tropicamide (200 nM, an M4 receptor blocker).
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16135768 Wen H, Brehm P: Paired motor neuron-muscle recordings in zebrafish test the receptor blockade model for shaping synaptic current. J Neurosci. 2005 Aug 31;25(35):8104-11.

We used this preparation to test the recent proposal that open channel block of the acetylcholine receptor by acetylcholine modulates the kinetics and timing of transmission between nerve and muscle in larval zebrafish (Legendre et al., 2000).
In contrast, blockade of motor neuron K channels by 4-aminopyridine prolonged the action potential and introduced a significant delay and slowing of evoked synaptic currents, demonstrating our ability to measured altered transmitter release with this system.
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