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ID: ALA1147512

Journal: Bioorg Med Chem Lett

Title: Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.

Authors: Crooks PA, Ayers JT, Xu R, Sumithran SP, Grinevich VP, Wilkins LH, Deaciuc AG, Allen DD, Dwoskin LP.

Abstract: N-n-Alkylation of nicotine converts it from an agonist into an antagonist at neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogues exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.

CiteXplore: 15050618

DOI: 10.1016/j.bmcl.2003.10.074