Protein Information

Name Acetylcholinesterase
Synonyms ACHE; ACHE protein; AChE; ARACHE; AcChoEase; Acetylcholine acetylhydrolase; Acetylcholinesterase; Acetylcholinesterase isoform E4 E6 variant…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
10632067 Han YF, Li CP, Chow E, Wang H, Pang YP, Carlier PR: Dual-site binding of bivalent 4-aminopyridine- and 4-aminoquinoline-based AChE inhibitors: contribution of the hydrophobic alkylene tether to monomer and dimer affinities. Bioorg Med Chem. 1999 Nov;7(11):2569-75.
63(0,2,2,3) Details
15003280 Harrison PK, Tattersall JE, Clement RA: Periodic orbit analysis reveals subtle effects of atropine on epileptiform activity in the guinea-pig hippocampal slice. Neurosci Lett. 2004 Mar 11;357(3):183-6.

We have used a recently developed mathematical technique based on periodic orbit analysis to investigate the effect of atropine (a muscarinic antagonist) on epileptiform activity induced by soman (an irreversible acetylcholinesterase inhibitor), 4-aminopyridine (a K+ channel blocker) and 8-cyclopentyl-1,3-dipropylxanthine (an adenosine A1 receptor antagonist) in the guinea-pig hippocampal slice.
31(0,1,1,1) Details
11256231 Ogura H, Kosasa T, Kuriya Y, Yamanishi Y: Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro. Methods Find Exp Clin Pharmacol. 2000 Oct;22(8):609-13.

The carbamate derivatives showed moderate selectivity, while the 4-aminopyridine derivatives tacrine and ipidacrine showed no selectivity.
6(0,0,0,6) Details
15496314 Caricati-Neto A, D'angelo LC, Reuter H, Hyppolito Jurkiewicz N, Garcia AG, Jurkiewicz A: Enhancement of purinergic neurotransmission by galantamine and other acetylcholinesterase inhibitors in the rat vas deferens. Eur J Pharmacol. 2004 Oct 25;503(1-3):191-201.

A striking enhancement of twitches was also caused by charybdotoxin, a blocker of high-conductance Ca2+-activated K+ channels, and by 4-aminopyridine, a non-specific blocker of K+ channels; in addition, apamin, a blocker of small-conductance Ca2+-activated K+ channels, induced a lower potentiation.
5(0,0,0,5) Details
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.


While CMS patients have been reported worldwide, in Japan there have been only a few descriptions of adult CMS patients with acetylcholinesterase (AChE) deficiency and slow channel syndrome.
2(0,0,0,2) Details
19593127 Argov Z: Management of myasthenic conditions: nonimmune issues. Curr Opin Neurol. 2009 Oct;22(5):493-7.


RECENT FINDINGS: Antisense compound inhibiting acetylcholine esterase has positive therapeutic effects during short-term administration, but further studies are needed to confirm its chronic effects.
1(0,0,0,1) Details
16643949 Amato MP, Portaccio E, Zipoli V: Are there protective treatments for cognitive decline in MS? . J Neurol Sci. 2006 Jun 15;245(1-2):183-6. Epub 2006 Apr 27.

Small trials with amantadine, pemoline, 4-aminopyridine and 3-4 aminopyridine have provided mainly negative results.
Acetylcholinesterase inhibitors (AChEI) used to treat Alzheimer's disease (AD)-such as donepezil, rivastigmine, and galantamine-have recently been tested in other cognitive disorders, including MS.
1(0,0,0,1) Details
16805718 Verschuuren JJ, Wirtz PW, Titulaer MJ, Willems LN, van Gerven J: Available treatment options for the management of Lambert-Eaton myasthenic syndrome. Expert Opin Pharmacother. 2006 Jul;7(10):1323-36.


Several drugs are available for the symptomatic treatment of the disease, including guanidine, aminopyridines or acetylcholinesterase inhibitors.
1(0,0,0,1) Details
18023348 Scipione L, De Vita D, Musella A, Flammini L, Bertoni S, Barocelli E: 4-Aminopyridine derivatives with anticholinesterase and antiamnesic activity. Bioorg Med Chem Lett. 2008 Jan 1;18(1):309-12. Epub 2007 Nov 19.

Compound 4d showed the highest inhibitory effect blocking non-competitively acetylcholinesterase and competitively butyrylcholinesterase.
1(0,0,0,1) Details
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.


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.
0(0,0,0,0) Details