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ALEPH-2, a suspected anxiolytic and putative hallucinogenic phenylisopropylamine derivative, is a 5-HT(2a) and 5-HT(2c) receptor agonist
Keywords: animals, serotonin, binding, 2a, laevis, agonist, receptor, agents, xenopus, agent, agonists, oocytes, pharmacodynamics, rna, drug, article, oocyte, psychopharmacology, concentration, anxiolytic, 4, 1, response, nonhuman, Anti-Anxiety, Receptors,, Complementary, 2, (2,5, dimethoxy, ethylthiophenyl), aminopropane, 2,5-Dimethoxy-4-Methylamphetamine, Receptor,, unclassified, microinjection, ritanserin, Serotonin,, psychedelic, 2C, Hallucinogens, Propylamines, 5-HT2A, 5-HT2C
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-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 ?M 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. (C) 2000 Elsevier Science Inc.
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| Título según SCOPUS: | ALEPH-2, a suspected anxiolytic and putative hallucinogenic phenylisopropylamine derivative, is a 5-HT(2a) and 5-HT(2c) 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://www.scopus.com/inward/record.url?eid=2-s2.0-0034680728&partnerID=q2rCbXpz |
| Notas: | SCOPUS |