4-Bromo-2,5-dimethoxyphenethylamine (2C-B) and structurally related phenylethylamines are potent 5-HT2A receptor antagonists in Xenopus laevis oocytes.
British journal of pharmacology April 1, 2004 Claudio A Villalobos, Paulina Bull, Patricio Sáez et al. 50 citations
Certain phenylethylamines (PEAs), including 2C-I, 2C-B, 2C-D, and 2C-H, block serotonin 5-HT2A receptors but not 5-HT2C receptors, showing subtype selectivity. In experiments with frog oocytes engineered to carry rat receptor clones, these compounds inhibited serotonin-induced currents at the 5-HT2A receptor, requiring a two-minute preincubation for maximum effect. The blocking potency depended on the chemical substituent at the fourth carbon position, with 2C-I being the most potent, followed by 2C-B, 2C-D, and 2C-H. The findings suggest that the psychoactive effects of these compounds may not rely solely on activating 5-HT2A receptors, as previously thought.