Comparative metabolism of the designer drug 4-methylthioamphetamine by hepatocytes from man, monkey, dog, rabbit, rat and mouse

  title={Comparative metabolism of the designer drug 4-methylthioamphetamine by hepatocytes from man, monkey, dog, rabbit, rat and mouse},
  author={Helena Carmo and Jan G. Hengstler and Douwe de Boer and Michael T. Ringel and F{\'e}lix Carvalho and Eduarda Fernandes and Fernando Remi{\~a}o and Lesseps A. dos Reys and Franz Oesch and Maria Lourdes Bastos},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
Several cases of death associated with 4-methylthioamphetamine (4-MTA) have raised public concern about the abuse of this designer drug that is usually sold as “Ecstasy” or “Flatliners”. Since only very little is known about the metabolism of 4-MTA in humans we performed an in vitro study incubating racemic 4-MTA with primary hepatocytes isolated from three male human donors. Additionally, hepatocytes from male monkey (Cynomolgus), dog (Beagle), rabbit (Chinchilla), rat (Sprague-Dawley), and… 
Metabolic fate of desomorphine elucidated using rat urine, pooled human liver preparations, and human hepatocyte cultures as well as its detectability using standard urine screening approaches
Investigation of the metabolic fate of desomorphine in vivo and in vitro using pooled human liver microsomes and cytosol as well as human liver cell lines found HepaRG cells to be the most suitable tool for prediction of human hepatic phase I and II metabolism of drugs of abuse.
Studies on the metabolism and toxicological detection of the designer drug 2,5‐dimethoxy‐4‐methyl‐β‐ phenethylamine (2C‐D) in rat urine using gas chromatographic/mass spectrometric techniques
The authors' systematic toxicological analysis (STA) procedure allowed the detection of an intake of a dose of 2C-D in rat urine that corresponds to a common drug user's dose, and should be suitable for proof of a intake of 1,5-dimethoxy-4-methyl-β-phenethylamine in human urine.


Excretion Profile of 4‐Methylthioamphetamine in Dogs
4-Methylthioamphetamine is detectable by immunoassay at 1 μgmL−1 and can be detected in dogs up to 23 h after administration and EMIT positive screens can be checked using GC-MS incorporating derivatization to confirm the presence of 4-MTA.
Fatal poisoning with a new phenylethylamine: 4-methylthioamphetamine (4-MTA).
  • S. Elliott
  • Chemistry, Biology
    Journal of analytical toxicology
  • 2000
Analysis of postmortem blood and urine specimens in a case implicating 3,4-methylenedioxymethamphetamine revealed the presence of 4-MTA at a concentration of 4.6 mg/L in femoral blood and 87.2 mg/l in the urine.
The hyperthermic and neurotoxic effects of ‘Ecstasy’ (MDMA) and 3,4 methylenedioxyamphetamine (MDA) in the Dark Agouti (DA) rat, a model of the CYP2D6 poor metabolizer phenotype
These data demonstrate that female DA rats are more susceptible to the acute hyperthermic effects of MDMA, probably because of impaired N‐demethylation and indicate that in human subjects acute MDMA‐induced toxicity may be exacerbated in poor metabolizer phenotypes.
Para‐methylthioamphetamine, a new amphetamine designer drug of abuse
Toxicological analysis proved that the 'S‐5 tablet' contained para‐methylthioamphetamine (MTA), mainly, which is a relative unknown amphetamine designer drug, which has only been studied as a model compound in some structure‐activity relationship studies.
Neuroendocrine pharmacology of three serotonin releasers: 1-(1,3-benzodioxol-5-yl)-2-(methylamino)butane (MBDB), 5-methoxy-6-methyl-2-aminoindan (MMAi) and p-methylthioamphetamine (MTA).
The results suggest that MBDB, MMAI and MTA can increase the secretion of several hormones, at least in part, through stimulation of serotonergic neurotransmission, however, these three 5-HT releasers seem to have effects on other mechanisms that can stimulate the release of some hormones.
One fatal and seven non-fatal cases of 4-methylthioamphetamine (4-MTA) intoxication: clinico-pathological findings
This report proves once again that the new amphetamine designer drugs are not without danger, as is thought by many young people, and the medico-legal implications of new, as yet unregistered drugs are discussed.