ALEPH-2, a suspected anxiolytic and putative hallucinogenic phenylisopropylamine derivative, is a 5-HT2a and 5-HT2c receptor agonist.
C Acuña-castillo, C Scorza, M Reyes-Parada, B K Cassels, J P Huidobro-Toro
Life sciences November 17, 2000 DOI: 10.1016/s0024-3205(00)00906-1 via PubMed
Summary
AI-generated from the abstractALEPH-2, a phenylisopropylamine derivative with claimed anxiolytic and hallucinogenic effects, acts as a partial agonist on the 5-HT2A receptor with potency similar to serotonin, but as a full agonist on the 5-HT2C receptor, where it is about 15-fold less potent than serotonin. The antagonist ritanserin blocks responses to both serotonin and ALEPH-2 equally, though the 5-HT2A receptor is more sensitive to ritanserin than the 5-HT2C receptor.
Study at a glance
| Characteristics | Laboratory experiment Peer reviewed |
|---|---|
| Population | Xenopus laevis oocytes microinjected with rat cRNA for 5-HT2A or 5-HT2C receptors |
| Interventions | ALEPH-2 5-hydroxytryptamine (5-HT) ritanserin |
| Citations | 3 |
| Key finding | ALEPH-2 is a partial agonist on the 5-HT2A receptor with potency similar to serotonin and a full agonist on the 5-HT2C receptor with about 15-fold lower potency than serotonin. |
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.