Interspecies In Vitro Evaluation of Stereoselective Protein Binding for 3,4-Methylenedioxymethamphetamine

Wan Raihana Wan Aasim; Soo Choon Tan; Siew Hua Gan

doi:10.1155/2017/8103726

Interspecies In Vitro Evaluation of Stereoselective Protein Binding for 3,4-Methylenedioxymethamphetamine

Wan Raihana Wan Aasim, Soo Choon Tan, Siew Hua Gan

Journal of Chemistry 2017 DOI: 10.1155/2017/8103726 (opens in new tab)

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Study at a glance

AI-extracted from the abstract

Characteristics	In vitro laboratory study Peer reviewed
Population	Human plasma, rat serum, and mouse serum
Intervention	rac-MDMA
Dose	20 and 200 ng/mL
Topics	MDMA
Key points	No significant stereoselectivity in MDMA protein binding was observed in human plasma or rat serum, but significant stereoselective binding (p<0.05) occurred in mouse serum. The authors note that MDMA protein binding in mouse serum is considerably lower than in humans and rats, and caution against using mice for in vitro MDMA studies.

Abstract

Abuse of 3,4-methylenedioxymethamphetamine (MDMA) is becoming more common worldwide. To date, there is no information available on stereoselectivity of MDMA protein binding in humans, rats, and mice. Since stereoselectivity plays an important role in MDMA’s pharmacokinetics and pharmacodynamics, in this study we investigated its stereoselectivity in protein binding. The stereoselective protein binding ofrac-MDMA was investigated using two different concentrations (20 and 200 ng/mL) in human plasma and mouse and rat sera using an ultrafiltration technique. No significant stereoselectivity in protein binding was observed in both human plasma and rat serum; however, a significant stereoselective binding (p<0.05) was observed in mouse serum. Since the protein binding of MDMA in mouse serum is considerably lower than in humans and rats, caution should be exercised when using mice for in vitro studies involving MDMA.

Comparable studies

Other preclinical and animal studies on MDMA, most cited first.

Study	Year	Design
Neurotoxicity of the psychedelic amphetamine, methylenedioxymethamphetamine. Rats (implied by typical neurochemical study context)	1987	Experimental study
3,4-Methylenedioxymethamphetamine and 3,4-methylenedioxyamphetamine destroy serotonin terminals in rat brain: quantification of neurodegeneration by measurement of [3H]paroxetine-labeled serotonin uptake sites. Rat brain	1987	Animal experiment
Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs Human and mouse dopamine, norepinephrine, and serotonin transporters expressed in cells	2006	In vitro laboratory study
Small Changes in Ambient Temperature Cause Large Changes in 3,4-Methylenedioxymethamphetamine (MDMA)-Induced Serotonin Neurotoxicity and Core Body Temperature in the Rat Rats	1998	Experimental study
Altered Serotonin Innervation Patterns in the Forebrain of Monkeys Treated with (±)3,4-Methylenedioxymethamphetamine Seven Years Previously: Factors Influencing Abnormal Recovery Squirrel monkeys treated with MDMA	1999	Observational cohort

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