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Effects of MDMA and related analogs on plasma 5-HT: relevance to 5-HT transporters in blood and brain

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dc.contributor.author Yubero Lahoz, Samanta, 1985-
dc.contributor.author Ayestas, Mario A.
dc.contributor.author Blough, Bruce E.
dc.contributor.author Partilla, John S.
dc.contributor.author Rothman, Richard B.
dc.contributor.author Torre Fornell, Rafael de la
dc.contributor.author Baumann, Michael H.
dc.date.accessioned 2019-02-11T08:44:27Z
dc.date.available 2019-02-11T08:44:27Z
dc.date.issued 2012
dc.identifier.citation Yubero-Lahoz S, Ayestas MA Jr, Blough BE, Partilla JS, Rothman RB, de la Torre R, Baumann MH. Effects of MDMA and related analogs on plasma 5-HT: relevance to 5-HT transporters in blood and brain. Eur J Pharmacol. 2012; 674(2-3):337-44. DOI 10.1016/j.ejphar.2011.10.033
dc.identifier.issn 0014-2999
dc.identifier.uri http://hdl.handle.net/10230/36542
dc.description.abstract (±)-3,4-Methylenedioxymethamphetamine (MDMA) is an illicit drug that evokes transporter-mediated release of serotonin (5-HT) in the brain. 5-HT transporter (SERT) proteins are also expressed in non-neural tissues (e.g., blood), and evidence suggests that MDMA targets platelet SERT to increase plasma 5-HT. Here we tested two hypotheses related to the effects of MDMA on circulating 5-HT. First, to determine if MDMA metabolites might contribute to actions of the drug in vivo, we used in vitro microdialysis in rat blood specimens to examine the effects of MDMA and its metabolites on plasma 5-HT. Second, to determine whether effects of MDMA on plasma 5-HT might be used as an index of central SERT activity, we carried out in vivo microdialysis in blood and brain after intravenous MDMA administration. The in vitro results show that test drugs evoke dose-related increases in plasma 5-HT ranging from two- to sevenfold above baseline, with MDMA and its metabolite, (±)-3,4-methylenedioxyamphetamine (MDA), producing the largest effects. The ability of MDMA and related analogs to elevate plasma 5-HT is correlated with their potency as SERT substrates in rat brain synaptosomes. The in vivo results reveal that MDMA causes concurrent increases in extracellular 5-HT in blood and brain, but there are substantial individual differences in responsiveness to the drug. Collectively, our findings indicate that MDMA and its metabolites increase plasma 5-HT by a SERT-dependent mechanism, and suggest the possibility that measures of evoked 5-HT release in blood may reflect central SERT activity.
dc.format.mimetype application/pdf
dc.language.iso eng
dc.publisher Elsevier
dc.relation.ispartof Eur J Pharmacol. 2012; 674(2-3):337-44
dc.rights © Elsevier http://dx.doi.org/10.1016/j.ejphar.2011.10.033
dc.title Effects of MDMA and related analogs on plasma 5-HT: relevance to 5-HT transporters in blood and brain
dc.type info:eu-repo/semantics/article
dc.identifier.doi http://dx.doi.org/10.1016/j.ejphar.2011.10.033
dc.subject.keyword Blood
dc.subject.keyword Brain
dc.subject.keyword MDMA
dc.subject.keyword Microdialysis
dc.subject.keyword Platelet
dc.subject.keyword 5-HT (serotonin)
dc.subject.keyword SERT (serotonin transporter)
dc.rights.accessRights info:eu-repo/semantics/openAccess
dc.type.version info:eu-repo/semantics/acceptedVersion

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