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

Acuna-Castillo, C; Scorza, C; Reyes-Parada, M; CASSELS, BK; Huidobro-Toro, JP

Abstract

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.

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Título según WOS: ALEPH-2, a suspected anxiolytic and putative hallucinogenic phenylisopropylamine derivative, is a 5-HT2a and 5-HT2c receptor agonist
Título de la Revista: LIFE SCIENCES
Volumen: 67
Número: 26
Editorial: PERGAMON-ELSEVIER SCIENCE LTD
Fecha de publicación: 2000
Página de inicio: 3241
Página final: 3247
Idioma: English
URL: http://linkinghub.elsevier.com/retrieve/pii/S0024320500009061
DOI:

10.1016/S0024-3205(00)00906-1

Notas: ISI