Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release |
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| Authors: | Crooks Peter A Ayers Joshua T Xu Rui Sumithran Sangeetha P Grinevich Vladimir P Wilkins Lincoln H Deaciuc A Gabriela Allen David D Dwoskin Linda P |
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| Affiliation: | Division of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082, USA. pcrooks@uky.edu |
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| 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. |
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