Trans-2-(2,5-dimethoxy-4-iodophenyl)cyclopropylamine and trans-2-(2,5-dimethoxy-4-bromophenyl)cyclopropylamine as potent agonists for the 5-HT 2 receptor family
UNC Libraries August 7, 2020 A. Pigott, X.-p. Huang, J.d. Mccorvy et al.
Replacing the ethylamine side chain of two psychedelic amphetamine derivatives, DOI and DOB, with a cyclopropylamine group produced new compounds that bind tightly to the 5-HT2 family of serotonin receptors. The most potent version had the (-)-(1R,2S)- configuration. However, these cyclopropane analogues also showed increased affinity for several other serotonin receptor subtypes beyond 5-HT2A and 5-HT2B. At appropriate doses, they may still be useful research tools for probing 5-HT2 receptor function, but their selectivity for 5-HT2A receptors is lower than that of the original compounds.