Journal of medicinal chemistry

Novel and potent 6-chloro-3-pyridinyl ligands for the α4β2 neuronal nicotinic acetylcholine receptor

B Latli, K D'Amou, JE Casida

Index: Latli, Bachir; D'Amour, Kevin; Casida, John E. Journal of Medicinal Chemistry, 1999 , vol. 42, # 12 p. 2227 - 2234

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Citation Number: 54

Abstract

1-[(6-Chloro-3-pyridinyl) methyl]-2-imidazolidine (1), the N-desnitro metabolite of the major insecticide imidacloprid, is known to have similar potency to that of (-)-nicotine as an inhibitor of [3H](-)-nicotine binding at the rat recombinant α4β2 neuronal nicotinic acetylcholine receptor (nAChR); IC50 values in the present study are 3.8 nM for (-)-nicotine, 6.0 nM for 1, and 155 nM for imidacloprid. Synthesis of new analogues of 1, modified only ...