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Methcathinone: A Study on the Impact of Stereoselectivity on Pharmacokinetics and Pharmacodynamics
Monday, March 08, 2021: 1:50 PM - 2:10 PM
Speaker(s)
Description
The United States is currently in the midst of a drug epidemic, with overdoses and drug-related deaths increasing annually. Often, the legal consequences of drug use incentivize individuals who abuse drugs to seek “legal highs” in the form of new psychoactive substances (NPS). NPS are usually closely related but poorly studied analogs of traditional drugs of abuse. Methcathinone is the beta-keto analog of the abused psychostimulant methamphetamine, and a chiral molecule that exhibits stereoselectivity. Intracranial self-stimulation (ICSS) was used to examine these stereoselective differences in rats. ICSS is an operant procedure in which subjects can respond upon a lever to receive electrical stimulation of brain reward areas, and it has been well characterized at preclinical assessment of the abuse potential of drugs. Thirteen (13) adult male Sprague-Dawley rats were anesthetized and surgically implanted with bipolar stainless-steel electrodes targeting the medial forebrain bundle. Animals were trained to respond upon a lever to receive electrical brain stimulation in one-minute frequency trials ranging from 56-158 Hz. Once stable responding was established, a range of doses of racemic methcathinone (0.10-1.0 mg/kg), R(+)-methcathinone (0.10-3.2 mg/kg), and S(-)-methcathinone (0.10-1.0 mg/kg) were administered by intraperitoneal injection, and the modulation of ICSS responding was compared. All three enantiomeric compositions of methcathinone facilitated ICSS responding in a manner consistent with other highly abused drugs. S(-)-methcathinone exhibited a 2.4-fold difference in potency to facilitate ICSS compared to R(+)-methcathinone. S(-)-methcathinone and R(+)-methcathinone had different times to peak effect. These stereoselective differences highlight the importance of bioanalytical methods that resolve individual enantiomers of chiral compounds in order to study drugs and their metabolites for forensic toxicological purposes.
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Clinical/Toxicology
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