In vitro neuronal and vascular responses to 5-hydroxytryptamine: modulation by 4-methylthioamphetamine, 4-methylthiomethamphetamine and 3,4-methylenedioxymethamphetamine

Murphy, James E.; Flynn, James; Cannon, Dara M.; Guiry, Patrick J.; McCormack, P. D.; Baird, Alan W.; McBean, Gethin J.; Keenan, A. K.

doi:10.1016/s0014-2999(02)01586-8

Cited by 12 publications

(5 citation statements)

References 26 publications

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“…Data suggest that MDMA may competitively block the noradrenaline transporter (Al-Sahli et al, 2001). In contrast, MDMA does not appear to significantly alter 5-HT-induced aortic contraction (Cannon et al, 2001;Murphy et al, 2002). However both 4-methylthioamphetamine and 4-methylthiomethamphetamine are potent inhibitors of 5-HT-mediated vascular contraction (Murphy et al, 2002).…”

Section: Neuroendocrine and Immunementioning

confidence: 93%

The Pharmacology and Clinical Pharmacology of 3,4-Methylenedioxymethamphetamine (MDMA, “Ecstasy”)

et al. 2003

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Section: Neuroendocrine and Immunementioning

confidence: 93%

The Pharmacology and Clinical Pharmacology of 3,4-Methylenedioxymethamphetamine (MDMA, “Ecstasy”)

et al. 2003

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“…To some extent, similarities to the effects of MDMA were found, however, lacking the amphetaminergic character of MDMA [26]. 4-MTA is a very selective serotonergic agent, showing increase in the release of serotonin, inhibition of serotonin reuptake, inhibition of MAO A and only low affinity for noradrenaline and dopamine uptake sites and monoamine receptors [59][60][61][62][63]. Due to its pharmacological properties, the induction of a serotonin syndrome is very likely and could be shown in rats [60].…”

Section: R S-4-methylthioamphetamine (4-mta)mentioning

confidence: 99%

Metabolism of Designer Drugs of Abuse

Staack

Maurer

2005

CDM

106

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Abuse of designer drugs is widespread among young people, especially in the so-called "dance club scene" or "rave scene", worldwide. Severe and even fatal poisonings have been attributed to the consumption of such drugs of abuse. However, in contrast to new medicaments, which are extensively studied in controlled clinical studies concerning metabolism, including cytochrome P450 isoenzyme differentiation, and further pharmacokinetics, designer drugs are consumed without any safety testing. This paper reviews the metabolism of new designer drugs of abuse that have emerged on the black market during the last years. Para-methoxyamphetamine (PMA), para-methoxymethamphetamine (PMMA) and 4-methylthioamphetamine (4-MTA), were taken into consideration as new "classical" amphetamine-derived designer drugs. Furthermore, N-benzylpiperazine (BZP), 1-(3, 4-methylenedioxybenzyl)piperazine (MDBP), 1-(3-trifluoromethylphenyl)piperazine (TFMPP), 1-(3-chlorophenyl)piperazine (mCPP) and 1-(4-methoxyphenyl)piperazine (MeOPP) were taken into consideration as derivatives of the class of piperazine-derived designer drugs, as well as alpha-pyr-rolidinopropiophenone (PPP), 4'-methoxy-alpha-pyrrolidinopropiophenone (MOPPP), 3', 4'-methylenedioxy-alpha-pyrrolidino-propiophenone (MDPPP), 4'-methyl-alpha-pyrrolidinopropiophenone (MPPP), and 4'-methyl-alpha-pyrrolidinoexanophenone (MPHP) as derivatives of the class of alpha-pyrrolidinophenone-derived designer drugs. Papers describing identification of in vivo or in vitro human or animal metabolites and cytochrome P450 isoenzyme dependent metabolism have been considered and summarized.

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“…Meanwhile, it has been scheduled in the lists of controlled substances of several countries. 4-MTA has been reported to be a nonneurotoxic serotonin releasing and reuptake inhibitory agent with monoamine oxidase-A inhibitory properties [6][7][8][9]. Its mode of action is similar to that of other designer drugs such as dimethoxymethylamphetamine (DOM) and of methylenedioxymethamphetamine (MDMA), but with a slower onset of the effects [9,10].…”

Section: Introductionmentioning

confidence: 99%

Studies on the metabolism and toxicological detection of the designer drug 4-methylthioamphetamine (4-MTA) in human urine using gas chromatography–mass spectrometry

Ewald¹,

Peters²,

Weise³

et al. 2005

Journal of Chromatography B

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In vitro neuronal and vascular responses to 5-hydroxytryptamine: modulation by 4-methylthioamphetamine, 4-methylthiomethamphetamine and 3,4-methylenedioxymethamphetamine

Cited by 12 publications

References 26 publications

The Pharmacology and Clinical Pharmacology of 3,4-Methylenedioxymethamphetamine (MDMA, “Ecstasy”)

The Pharmacology and Clinical Pharmacology of 3,4-Methylenedioxymethamphetamine (MDMA, “Ecstasy”)

Metabolism of Designer Drugs of Abuse

Studies on the metabolism and toxicological detection of the designer drug 4-methylthioamphetamine (4-MTA) in human urine using gas chromatography–mass spectrometry

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