Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding

…, M Pigini, W Quaglia, MI Damaj, BR Martin…

Index: Ferretti; Dukat; Giannella; Piergentili; Pigini; Quaglia; Damaj; Martin; Glennon Journal of Medicinal Chemistry, 2002 , vol. 45, # 21 p. 4724 - 4731

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Citation Number: 18

Abstract

We have recently identified 3-[(1-methyl)-4, 5-dihydro-1H-imidazol-2-yl) methyl] pyridine (homoazanicotine, 8) as a novel nicotinic acetylcholinergic (nACh) receptor ligand. In the present investigation, after we determined that 8 binds selectively at nicotinic (K i= 7.8 nM) vs muscarinic (K i> 10 000 nM) acetylcholinergic receptors, we examined its structure-affinity relationships for nACh receptor binding. The features investigated included the influence ...