New aporphinoid 5-HT2A and α1A antagonists via structural manipulations of nantenine
摘要:
A series of Cl, C2, C3 and N6 analogs of nantenine (2) was synthesized and evaluated in 5-HT2A and alpha(1A) receptor functional assays. Alkyl substitution of the Cl and N6 methyl groups of nantenine provided selective 5-HT2A and alpha 1A antagonists, respectively. The C2 alkyloxy analogs studied were generally selective for alpha(1A) versus 5-HT2A. The C3 bromo analog 15 is one of the most potent aporphinoid 5-HT2A antagonists known presently. (C) 2011 Elsevier Ltd. All rights reserved.
New aporphinoid 5-HT2A and α1A antagonists via structural manipulations of nantenine
摘要:
A series of Cl, C2, C3 and N6 analogs of nantenine (2) was synthesized and evaluated in 5-HT2A and alpha(1A) receptor functional assays. Alkyl substitution of the Cl and N6 methyl groups of nantenine provided selective 5-HT2A and alpha 1A antagonists, respectively. The C2 alkyloxy analogs studied were generally selective for alpha(1A) versus 5-HT2A. The C3 bromo analog 15 is one of the most potent aporphinoid 5-HT2A antagonists known presently. (C) 2011 Elsevier Ltd. All rights reserved.