Systematic Structure-Activity Studies on Selected 2-, 3-, and 4-Monosubstituted Synthetic Methcathinone Analogs as Monoamine Transporter Releasing Agents.

ABSTRACT: Methcathinone analogs are appearing on the clandestine market at a rate nearly out-pacing the ability of investigators to examine them on an individual basis. To formulate structure-activity relationship (SAR) generalities, we examined the releasing ability of several simple methcathinone analogs at the three monoamine transporters (i.e., the dopamine, norepinephrine, and serotonin transporters, DAT, NET, and SERT, respectively) using in vitro assay methods. The analogs included methcathinone and 14 other compounds monosubstituted at the 2-, 3-, or 4-position. In general, (a) the 2-substituted analogs were less potent than either the 3- or 4-substituted analogs, (b) the 3- and 4-substituted analogs were relatively similar in potency, (c) methcathinone was the most selective as a DAT-releas

SUBMITTER: Walther D 

PROVIDER: S-EPMC8269283 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature