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New aporphinoid 5-HT(2A) and alpha(1A) antagonists via structural manipulations of nantenine

Chaudhary, S., Ponnala, S., LeGendre, O., Gonzales, JA., Navarro, H., & Harding, WW. (2011). New aporphinoid 5-HT(2A) and alpha(1A) antagonists via structural manipulations of nantenine. Bioorganic and Medicinal Chemistry, 19(19), 5861-5868.

Abstract

A series of Cl, C2, C3 and N6 analogs of nantenine (2) was synthesized and evaluated in 5-HT(2A) and alpha(1A) receptor functional assays. Alkyl substitution of the Cl and N6 methyl groups of nantenine provided selective 5-HT(2A) and alpha 1A antagonists, respectively. The C2 alkyloxy analogs studied were generally selective for alpha(1A) versus 5-HT(2A). The C3 bromo analog 15 is one of the most potent aporphinoid 5-HT(2A) antagonists known presently. (C) 2011 Elsevier Ltd. All rights reserved

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