Browsing by Author "Scorza, C"

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    Aleph2, a Suspected Anxiolytic and Putative Hallucinogenic Phenylisopropylamine Derivative, Is a 5-Ht2a and 5-Ht2c Receptor Agonist
    (2000) Acuña-Castillo, C; Scorza, C; Reyes-Parada, M; Cassels, BK; Huidobro-Toro, JP
    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.