Effects of Hydroxylated Mephedrone Metabolites on Monoamine Transporter Activity <i>in vitro</i>.

ABSTRACT: Mephedrone is a largely abused psychostimulant. It elicits the release of monoamines via the high affinity transporters for dopamine (DAT), norepinephrine (NET) and serotonin (SERT). Stereoselective metabolic reactions are involved in the inactivation and the elimination of its chemical structure. However, during these processes, several structures are generated and some of them have been reported to be still pharmacologically active. In this study 1) we have newly synthetized several putative mephedrone metabolites, 2) compared their activity at monoamine transporters, 3) generated quantitative structure activity relationships, and 4) exploited the chemical structure of the putative metabolites to screen a urine sample from a drug user and dissect mephedrone metabolism. We have found that

SUBMITTER: Niello M 

PROVIDER: S-EPMC8063026 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature