Z3881312504 (also known as Z2504) is a substituted phenethylamine derivative which acts as a serotonin receptor modulator. It binds to the 5-HT2A, 5-HT2B and 5-HT2C receptors with fairly similar affinity, but while it is a reasonably potent partial agonist of 5-HT2A, its efficacy at the 5-HT2B and 5-HT2C receptors is negligible, making it a functional antagonist at these receptors. Study of the binding mode of Z2504 and how it achieves functional selectivity for 5-HT2A despite similar binding at all three subtypes has led to the subsequent development of compounds such as IHCH-2330 and IHCH-6122 which are more potent as both 5-HT2A agonists and 5-HT2B antagonists, and may have potential for clinical development as antidepressants.
See also Substituted phenethylamine 25-NB (psychedelics)
References