Receptor Interaction Profiles of 4-Alkoxy-Substituted 2,5-Dimethoxyphenethylamines and Related Amphetamines.

ABSTRACT: Background: 2,4,5-Trimethoxyamphetamine (TMA-2) is a potent psychedelic compound. Structurally related 4-alkyloxy-substituted 2,5-dimethoxyamphetamines and phenethylamine congeners (2C-O derivatives) have been described but their pharmacology is mostly undefined. Therefore, we examined receptor binding and activation profiles of these derivatives at monoamine receptors and transporters. Methods: Receptor binding affinities were determined at the serotonergic 5-HT_1A, 5-HT_2A, and 5-HT_2C receptors, trace amine-associated receptor 1 (TAAR1), adrenergic α₁ and α₂ receptors, dopaminergic D₂ receptor, and at monoamine transporters, using target-transfected cells. Additionally, activation of 5-HT_2A and 5-HT<

SUBMITTER: Kolaczynska KE 

PROVIDER: S-EPMC6893898 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature