Differences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5-HT(2A) and 5-HT(2C) receptors.
British journal of pharmacology June 1, 2002 Claudio Acuña-Castillo, Claudio Villalobos, Pablo R Moya et al.
A series of phenylisopropylamines and phenylethylamines were tested on rat serotonin 5-HT2A and 5-HT2C receptors expressed in frog eggs. All compounds acted as full agonists at 5-HT2C receptors, while at 5-HT2A receptors they were partial agonists, with relative efficacy ranging from 22% to 58% of serotonin's effect. The phenylethylamines had lower or undetectable efficacy at 5-HT2A receptors. DOI was a full agonist at 5-HT2C, while 2C-N acted as an antagonist at both receptors, competitive at 5-HT2A but non-competitive at 5-HT2C. The alpha-methyl group on the drugs determined their efficacy at both receptor subtypes.