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Assessment of the role of alpha-methylepinine in the neurotoxicity of MDMA.
Steele, T D; Brewster, W K; Johnson, M P; Nichols, D E; Yim, G K.
Afiliación
  • Steele TD; Department of Pharmacology and Toxicology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907.
Pharmacol Biochem Behav ; 38(2): 345-51, 1991 Feb.
Article en En | MEDLINE | ID: mdl-1676172
To assess the potential involvement of metabolism of 3,4-methylenedioxymethamphetamine (MDMA) to the catechol alpha-methylepinine in producing serotonergic neurotoxicity, we attempted to correlate aspects of this reaction with the neurotoxicity profile of MDMA. In contrast to the stereoselectivity of S-(+)-MDMA in causing persistent declines in rat brain 5-hydroxyindole levels, no stereochemical component to the metabolic reaction was apparent. Rat liver microsomes generated a significantly greater amount of alpha-methylepinine than did mouse microsomes, but similar amounts of metabolite were produced by brain microsomes from the two species. Formation of alpha-methylepinine by hepatic, but not brain, microsomes was inhibited by SKF 525A and induced by phenobarbital, possibly indicating a tissue specificity in cytochrome P-450-dependent metabolism of MDMA. To directly assess whether alpha-methylepine is a likely mediator of MDMA neurotoxicity, the compound was administered intracerebroventricularly. No persistent declines in biogenic amines or their metabolites were observed one week following treatment. These data suggest that alpha-methylepinine alone is not responsible for the neurotoxic effects of MDMA.
Asunto(s)
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Desoxiepinefrina / 3,4-Metilenodioxianfetamina / Enfermedades del Sistema Nervioso Límite: Animals Idioma: En Revista: Pharmacol Biochem Behav Año: 1991 Tipo del documento: Article Pais de publicación: Estados Unidos
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Desoxiepinefrina / 3,4-Metilenodioxianfetamina / Enfermedades del Sistema Nervioso Límite: Animals Idioma: En Revista: Pharmacol Biochem Behav Año: 1991 Tipo del documento: Article Pais de publicación: Estados Unidos