查看文章

Methcathinone (MCAT) is a potent monoamine releaser and parent compound to emerging drugs of abuse including mephedrone (4‐CH₃ MCAT), the para‐methyl analogue of MCAT. This study examined quantitative structure–activity relationships (QSAR) for MCAT and six para‐substituted MCAT analogues on (a) in vitro potency to promote monoamine release via dopamine and serotonin transporters (DAT and SERT, respectively), and (b) in vivo modulation of intracranial self‐stimulation (ICSS), a behavioural procedure used to evaluate abuse potential. Neurochemical and behavioural effects were correlated with steric (E_s), electronic (σ_p) and lipophilic (π_p) parameters of the para substituents.

For neurochemical studies, drug effects on monoamine release through DAT and SERT were evaluated in rat brain synaptosomes. For behavioural studies, drug effects …