ALEPH-2, a suspected anxiolytic and putative hallucinogenic phenylisopropylamine derivative, is a 5-HT2a and 5-HT2c receptor agonist

被引：4
|
作者：
Acuña-Castillo, C
Scorza, C
Reyes-Parada, M
Cassels, BK
Huidobro-Toro, JP
机构：
[1] Pontificia Univ Catolica Chile, Fac Ciencias Biol, Dept Fisiol,Ctr Regulac Celular & Patol, Inst Milenio Biol Fundamental & Aplicada, Santiago 1, Chile
[2] Inst Invest Biol Clemente Estable, Div Biol Celular, Montevideo, Uruguay
[3] Univ Santiago Chile, Fac Ciencias Med, Santiago, Chile
[4] Univ Chile, Fac Ciencias, Dept Quim, Inst Milenio Estudios Avanzados Biol Celular & Bi, Santiago, Chile
来源：
LIFE SCIENCES | 2000年 / 67卷 / 26期
关键词：
ALEPH-2; 5-hydroxytryptamine; 5-HT2A and 5-HT2C receptors; phenylisopropylamine derivatives;
D O I：
10.1016/S0024-3205(00)00906-1
中图分类号：
R-3 [医学研究方法]; R3 [基础医学];
学科分类号：
1001 ;
摘要：
To assess the pharmacodynamic profile of ALEPH-2, a phenylisopropylamine derivative with alleged anxiolytic and hallucinogenic properties,Xenopus laevis oocytes were microinjected with either of the rat cRNA for the 5-HT2A or the 5-HT2C receptor. Concentration-response curves were obtained following the exposure of the oocytes to varying concentrations of either ALEPH-2 or 5-hydroxy-tryptamine (5-HT) for 10 s. ALEPH-2 is a partial agonist on the 5-HT,,receptor with a similar potency to 5-HT. In contrast, ALEPH-2 is a full 5-HT2C receptor agonist and is about 15-fold less potent than 5-HT. Pre-application of 1 muM ritanserin antagonized the responses induced by 5-HT and ALEPH-2 to the same extent; however, the 5-HT2A receptor is more sensitive to ritanserin blockade than the 5-HT2C receptor. (C) 2000 Elsevier Science Inc. All rights reserved.
引用
收藏
页码：3241 / 3247
页数：7
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