Novel bis-, tris-, and tetrakis-tertiary amino analogs as antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release |
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Authors: | Zhang Zhenfa Zheng Guangrong Pivavarchyk Marharyta Deaciuc A Gabriela Dwoskin Linda P Crooks Peter A |
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Affiliation: | College of Pharmacy, Department of Pharmaceutical Sciences, University of Kentucky, Lexington, KY 40536-0082, USA |
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Abstract: | A series of tertiary amine analogs derived from lead azaaromatic quaternary ammonium salts has been designed and synthesized. The preliminary structure-activity relationships of these new analogs suggest that such tertiary amine analogs, which potently inhibit nicotine-evoked dopamine release from rat striatum, represent drug-like inhibitors of α6-containing nicotinic acetylcholine receptors. The bis-tertiary amine analog 7 exhibited an IC50 of 0.95 nM, while the tris-tertiary amine analog 19 had an IC50 of 0.35 nM at nAChRs mediating nicotine-evoked dopamine release. |
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Keywords: | nAChR antagonists Smoking cessation Tobacco dependency |
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