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-hydroxytryptamine (5-HT) for 10 s. ALEPH-2 is a partial agonist on the 5-HT2A 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 microM 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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Anxiety Agents / chemistry
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Anti-Anxiety Agents / pharmacology*
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DOM 2,5-Dimethoxy-4-Methylamphetamine / analogs & derivatives*
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DOM 2,5-Dimethoxy-4-Methylamphetamine / chemistry
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DOM 2,5-Dimethoxy-4-Methylamphetamine / pharmacology*
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Hallucinogens / chemistry
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Hallucinogens / pharmacology*
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Oocytes
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Propylamines / chemistry
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Propylamines / pharmacology*
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Receptor, Serotonin, 5-HT2A
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Receptor, Serotonin, 5-HT2C
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Receptors, Serotonin / metabolism*
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Serotonin / pharmacology
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Serotonin Receptor Agonists / pharmacology*
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Xenopus laevis
Substances
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Anti-Anxiety Agents
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Hallucinogens
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Propylamines
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Receptor, Serotonin, 5-HT2A
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Receptor, Serotonin, 5-HT2C
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Receptors, Serotonin
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Serotonin Receptor Agonists
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DOM 2,5-Dimethoxy-4-Methylamphetamine
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Serotonin
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1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane