TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors

M Bencherif, AJ Bane, CH Miller, GM Dull…

Index: Bencherif, Merouane; Bane, Andrew J; Miller, Craig H; Dull, Gary M; Gatto, Gregory J European Journal of Pharmacology, 2000 , vol. 409, # 1 p. 45 - 55

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Citation Number: 43

Abstract

TC-2559 [(E)-N-Methyl-4-[3-(5-ethoxypyridin) yl]-3-buten-1-amine] is a novel nicotinic agonist markedly more selective than recently reported novel nicotinic receptor ligands (selectivity ratio for central nervous system (CNS) to peripheral nervous system (PNS)> 4000). TC-2559 competes effectively with [3H]-nicotine binding (Ki= 5 nM) but not with [125I]- bungarotoxin (> 50,000 nM). Dopamine release from striatal synaptosomes and ion flux ...