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Hyperthermia Severely Affects the Vascular Effects of MDMA and Metabolites in the Human Internal Mammary Artery In Vitro

Fonseca, D. A. ; Guerra, A. F. ; Carvalho, F. ; Fernandes, E. ; Ferreira, L. M. ; Branco, P. S. ; Antunes, P. E. ; Antunes, M. J. ; Cotrim, M. D.

Cardiovascular toxicology, 2017-10, Vol.17 (4), p.405-416 [Periódico revisado por pares]

New York: Springer US

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Título:
Hyperthermia Severely Affects the Vascular Effects of MDMA and Metabolites in the Human Internal Mammary Artery In Vitro
Autor: Fonseca, D. A. ; Guerra, A. F. ; Carvalho, F. ; Fernandes, E. ; Ferreira, L. M. ; Branco, P. S. ; Antunes, P. E. ; Antunes, M. J. ; Cotrim, M. D.
Assuntos: Abuse ; Adult ; Aged ; Aged, 80 and over ; Antagonists ; Biomedical and Life Sciences ; Biomedicine ; Blood pressure ; Cardiac patients ; Cardiology ; Cardiovascular diseases ; Catechol ; Dose-Response Relationship, Drug ; Ecstasy ; Ecstasy (Drug) ; Female ; Fever ; Fever - metabolism ; Fever - pathology ; Health risks ; Heart diseases ; Heart rate ; Humans ; Hyperthermia ; Male ; Mammary Arteries - drug effects ; Mammary Arteries - metabolism ; Mammary Arteries - pathology ; MDMA ; Metabolites ; Middle Aged ; N-Methyl-3,4-methylenedioxyamphetamine - metabolism ; N-Methyl-3,4-methylenedioxyamphetamine - toxicity ; Organ Culture Techniques ; Original Paper ; Pharmacology/Toxicology ; Resveratrol ; Side effects ; Vasoconstriction ; Vasoconstriction - drug effects ; Vasoconstriction - physiology
É parte de: Cardiovascular toxicology, 2017-10, Vol.17 (4), p.405-416
Descrição: 3,4-Methylenedioxymethamphetamine (MDMA or “ecstasy”) is a recreational drug used worldwide for its distinctive psychotropic effects. Although important cardiovascular effects, such as increased blood pressure and heart rate, have also been described, the vascular effects of MDMA and metabolites and their correlation with hyperthermia (major side effect of MDMA) are not yet fully understood and have not been previously reported. This study aimed at evaluating the effects of MDMA and its main catechol metabolites, alpha-methyldopamine (α-MeDA), N -methyl-alpha-methyldopamine ( N -Me-α-MeDA), 5-(glutathion-S-yl)-alpha-methyldopamine [5-(GSH)-α-MeDA] and 5-(glutathion-S-yl)- N -methyl-alpha-methyldopamine [5-(GSH)- N -Me-α-MeDA], on the 5-HT-dependent vasoactivity in normothermia (37 °C) and hyperthermia (40 °C) of the human internal mammary artery (IMA) in vitro. The results showed the ability of MDMA, α-MeDA and N -Me-α-MeDA to exert vasoconstriction of the IMA which was considerably higher in hyperthermic conditions (about fourfold for MDMA and α-MeDA and twofold for N -Me-α-MeDA). The results also showed that all the compounds may influence the 5-HT-mediated concentration-dependent response of IMA, as MDMA, α-MeDA and N -Me-α-MeDA behaved as partial agonists and 5-(GSH)-α-MeDA and 5-(GSH)- N -Me-α-MeDA as antagonists. In conclusion, MDMA abuse may imply a higher cardiovascular risk associated both to MDMA and its metabolites that might be relevant in patients with underlying cardiovascular diseases, particularly in hyperthermia.
Editor: New York: Springer US
Idioma: Inglês

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Hyperthermia Severely Affects the Vascular Effects of MDMA and Metabolites in the Human Internal Mammary Artery In Vitro

Fonseca, D. A. ; Guerra, A. F. ; Carvalho, F. ; Fernandes, E. ; Ferreira, L. M. ; Branco, P. S. ; Antunes, P. E. ; Antunes, M. J. ; Cotrim, M. D.

New York: Springer US

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