SAR of psilocybin analogs:: Discovery of a selective 5-HT2C agonist

被引：58

作者：

Sard, H

Kumaran, G

Morency, C

Roth, BL

Toth, BA

He, P

Shuster, L

机构：

[1] Organix Inc, Woburn, MA 01801 USA

[2] Case Western Reserve Univ, Sch Med, Cleveland, OH 44106 USA

[3] Tufts Univ, Sch Med, Boston, MA 02111 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 20期

关键词：

D O I：

10.1016/j.bmcl.2005.06.104

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An SAR study of psilocybin and psilocin derivatives reveals that 1-methylpsilocin is a selective agonist at the h5-HT2C receptor. The corresponding phosphate derivative, 1-methylpsilocybin, shows efficacy in an animal model for obsessive-compulsive disorder, as does 4-fluoro-N,N-dimethyltryptamine. These results suggest a new area for development of novel 5-HT2C agonists with applications for drug discovery. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4555 / 4559

页数：5

共 24 条

[21] Molecular determinants for the interaction of the valvulopathic anorexigen norfenfluramine with the 5-HT2B receptor [J].