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The Norepinephrine Transporter Inhibitor Reboxetine Reduces Stimulant Effects of MDMA (“Ecstasy”) in Humans
Author(s) -
Hysek CM,
Simmler LD,
Ineichen M,
Grouzmann E,
Hoener MC,
Brenneisen R,
Huwyler J,
Liechti ME
Publication year - 2011
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.2011.78
Subject(s) - mdma , reboxetine , ecstasy , stimulant , norepinephrine transporter , pharmacology , norepinephrine , chemistry , active metabolite , crossover study , transporter , placebo , catecholamine , pharmacokinetics , medicine , reuptake inhibitor , endocrinology , dopamine , biochemistry , serotonin , psychiatry , alternative medicine , pathology , gene , receptor
This study assessed the pharmacodynamic and pharmacokinetic effects of the interaction between the selective norepinephrine (NE) transporter inhibitor reboxetine and 3,4‐methylenedioxymethamphetamine (MDMA, “ecstasy”) in 16 healthy subjects. The study used a double‐blind, placebo‐controlled crossover design. Reboxetine reduced the effects of MDMA including elevations in plasma levels of NE, increases in blood pressure and heart rate, subjective drug high, stimulation, and emotional excitation. These effects were evident despite an increase in the concentrations of MDMA and its active metabolite 3,4‐methylenedioxyamphetamine (MDA) in plasma. The results demonstrate that transporter‐mediated NE release has a critical role in the cardiovascular and stimulant‐like effects of MDMA in humans. Clinical Pharmacology & Therapeutics (2011) 90 2, 246–255. doi: 10.1038/clpt.2011.78