ALEPH-2, a suspected anxiolytic and putative hallucinogenic phenylisopropylamine derivative, is a 5-HT_2a and 5-HT_2c receptor agonist

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• 作者：Acuñ ; a-Castillo ; Claudio ; Scorza ; Cecilia ; Reyes-Parada ; Miguel ; Cassels ; Bruce K. ; et. al.
• 关键词：ALEPH-2 ; 5-hydroxytryptamine ; 5-HT_2A and 5-HT_2C receptors ; Phenylisopropylamine derivatives
• 刊名：Life Sciences
• 出版年：2000
• 期刊代码：62_00243205
• 类别：imm
• 出版时间：November 17, 2000
• 卷：67
• 期：2
• 页码：3241-3247
• 文件大小：86.3 K

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-HT_2A or the 5-HT_2C receptor. Concentration-response curves were obtained following the exposure of the oocytes to varying concentrations of either ALEPH-2 or 5-hydroxytryptamine (5-HT) for 10 s. ALEPH-2 is a partial agonist on the 5-HT_2A receptor with a similar potency to 5-HT. In contrast, ALEPH-2 is a full 5-HT_2C receptor agonist and is about 15-fold less potent than 5-HT. Pre-application of 1 μM ritanserin antagonized the responses induced by 5-HT and ALEPH-2 to the same extent; however, the 5-HT_2A receptor is more sensitive to ritanserin blockade than the 5-HT_2C receptor.