Tetrakis-azaaromatic quaternary ammonium salts: novel subtype-selective 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: | Department of Pharmaceutical Sciences, University of Kentucky, Lexington, KY 40536-0082, USA. |
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Abstract: | A series of tetrakis-azaaromatic quaternary ammonium salts was synthesized to identify compounds with higher affinity and selectivity as antagonists at neuronal nicotinic receptor subtypes (nAChR) that mediate nicotine-evoked DA release. A high hit rate was achieved in identifying potent analogs that inhibit these nAChRs. Three tetrakis analogs, 11j, 11f, and 11g, were identified as potent (IC(50)=3, 28 and 56nM, respectively) antagonists at these receptors. These compounds represent a novel structural class of nicotinic receptor antagonists. |
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