New aporphinoid 5-HT2A and α1A antagonists via structural manipulations of nantenine

Volume: 19, Issue: 19, Pages: 5861 - 5868
Published: Oct 1, 2011
Abstract
A series of C1, C2, C3 and N6 analogs of nantenine (2) was synthesized and evaluated in 5-HT(2A) and α(1A) receptor functional assays. Alkyl substitution of the C1 and N6 methyl groups of nantenine provided selective 5-HT(2A) and α(1A) antagonists, respectively. The C2 alkyloxy analogs studied were generally selective for α(1A) versus 5-HT(2A). The C3 bromo analog 15 is one of the most potent aporphinoid 5-HT(2A) antagonists known...
Paper Details
Title
New aporphinoid 5-HT2A and α1A antagonists via structural manipulations of nantenine
Published Date
Oct 1, 2011
Volume
19
Issue
19
Pages
5861 - 5868
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