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4-Methylthioamphetamine Increases Dopamine in the Rat Striatum and has Rewarding Effects In Vivo

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Autor dc.contributor.author Sotomayor-Zarate R.
Autor dc.contributor.author Quiroz G.
Autor dc.contributor.author Araya K.A.
Autor dc.contributor.author Abarca J.
Autor dc.contributor.author Ibanez M.R.
Autor dc.contributor.author Montecinos A.
Autor dc.contributor.author Guajardo C.
Autor dc.contributor.author Nunez G.
Autor dc.contributor.author Fierro A.
Autor dc.contributor.author Moya P.R.
Autor dc.contributor.author Iturriaga-Vasquez P.
Autor dc.contributor.author Gomez-Molina C.
Autor dc.contributor.author Gysling K.
Autor dc.contributor.author Reyes-Parada M.
Fecha Ingreso dc.date.accessioned 2014-04-05T00:18:44Z
Fecha Disponible dc.date.available 2014-04-05T00:18:44Z
Fecha en Repositorio dc.date.issued 2014-04-04
dc.identifier 10.1111/j.1742-7843.2012.00926.x
dc.description.abstract 4-Methylthioamphetamine (MTA) is a phenylisopropylamine derivative whose use has been associated with severe intoxications. MTA is usually regarded as a selective serotonin-releasing agent. Nevertheless, previous data have suggested that its mechanism of action probably involves a catecholaminergic component. As little is known about dopaminergic effects of this drug, in this work the actions of MTA upon the dopamine (DA) transporter (DAT) were studied in vitro, in vivo and in silico. Also, the possible abuse liability of MTA was behaviourally assessed. MTA exhibited an in vitro affinity for the rat DAT in the low micromolar range (6.01 μM) and induced a significant, dose-dependent increase in striatal DA. MTA significantly increased c-Fos-positive cells in striatum and nucleus accumbens, induced conditioned place preference and increased locomotor activity. Docking experiments were performed in a homology model of the DAT. In conclusion, our results show that MTA is able to increase extracellular striatal DA levels and that its administration has rewarding properties. These effects were observed at concentrations or doses that can be relevant to its use in human beings. © 2012 Nordic Pharmacological Society. en_US
dc.source Basic and Clinical Pharmacology and Toxicology
Link Descarga dc.source.uri http://www.scopus.com/inward/record.url?eid=2-s2.0-84869202147&partnerID=40&md5=05c850e4b992f4f3bf2b482ab682ae03
Title dc.title 4-Methylthioamphetamine Increases Dopamine in the Rat Striatum and has Rewarding Effects In Vivo en_US
Tipo dc.type Article
dc.description.keywords 4 methylthioamphetamine; amphetamine derivative; dopamine; dopamine transporter; protein c fos; unclassified drug; animal experiment; animal tissue; article; controlled study; corpus striatum; dopamine brain level; dose response; drug protein binding; extracellular space; in vitro study; in vivo study; locomotion; male; molecular docking; nonhuman; nucleus accumbens; place preference; priority journal; radioassay; rat; reward; structural homology; Amphetamines; Animals; Chromatography, High Pressure Liquid; Corpus Striatum; Dopamine; Dopamine Plasma Membrane Transport Proteins; Male; Motor Activity; Nucleus Accumbens; Rats; Rats, Sprague-Dawley; Rattus en_US


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