ALEPH-2, a suspected anxiolytic and putative hallucinogenic phenylisopropylamine derivative, is a 5-HT2a and 5-HT2c receptor agonist

Life Sci. 2000 Nov 17;67(26):3241-7. doi: 10.1016/s0024-3205(00)00906-1.

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

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Anxiety Agents / chemistry
  • Anti-Anxiety Agents / pharmacology*
  • DOM 2,5-Dimethoxy-4-Methylamphetamine / analogs & derivatives*
  • DOM 2,5-Dimethoxy-4-Methylamphetamine / chemistry
  • DOM 2,5-Dimethoxy-4-Methylamphetamine / pharmacology*
  • Hallucinogens / chemistry
  • Hallucinogens / pharmacology*
  • Oocytes
  • Propylamines / chemistry
  • Propylamines / pharmacology*
  • Receptor, Serotonin, 5-HT2A
  • Receptor, Serotonin, 5-HT2C
  • Receptors, Serotonin / metabolism*
  • Serotonin / pharmacology
  • Serotonin Receptor Agonists / pharmacology*
  • Xenopus laevis

Substances

  • Anti-Anxiety Agents
  • Hallucinogens
  • Propylamines
  • Receptor, Serotonin, 5-HT2A
  • Receptor, Serotonin, 5-HT2C
  • Receptors, Serotonin
  • Serotonin Receptor Agonists
  • DOM 2,5-Dimethoxy-4-Methylamphetamine
  • Serotonin
  • 1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane