Metabolism Is Required for the Expression of Ecstasy-Induced Cardiotoxicity in Vitro
Chemical Research in Toxicology April 27, 2004 Márcia Carvalho, Fernando Remião, Nuno Milhazes et al. 77 citations
MDMA (ecstasy) and its major metabolite MDA did not directly damage heart cells from adult rats in the lab, but two further metabolites, N-Me-alpha-MeDA and alpha-MeDA, caused significant toxicity. These catechol metabolites triggered a loss of normal cell shape, depletion of the antioxidant glutathione, sustained increases in intracellular calcium, drops in ATP, and reduced activity of antioxidant enzymes. N-Me-alpha-MeDA was the most toxic. The findings suggest that MDMA must be metabolized into these catechol compounds for cardiotoxicity to occur in isolated heart cells.