The heterocyclic substituted pyridine derivative (±)-2-(-3-pyridinyl)-1-azabicyclo [2.2. 2] octane (RJR-2429): a selective ligand at nicotinic acetylcholine receptors

M Bencherif, JD Schmitt, BS Bhatti, P Crooks…

Index: Bencherif; Schmitt; Bhatti; Crooks; Caldwell; Lovette; Fowler; Reeves; Lippiello Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 284, # 3 p. 886 - 894

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Citation Number: 55

Abstract

Abstract The present report describes in vitro studies demonstrating that the heterocyclic substituted pyridine compound (±)-2-(3-pyridinyl)-1-azabicyclo [2.2. 2] octane (RJR-2429) is extremely potent in activating human muscle nicotine ACh receptor (nAChR)(EC 50= 59±17 nM; E max= 110±09% vs. nicotine). RJR-2429 is markedly less potent in activating nAChRs in the clonal cell line PC12, with EC 50= 1100±230 nM andE max= 85±20% when ...