p‐Methylthioamphetamine and 1‐(m‐chlorophenyl)piperazine, two non‐neurotoxic 5‐HT releasers in vivo, differ from neurotoxic amphetamine derivatives in their mode of action at 5‐HT nerve endings in vitro

@article{Gobbi2002pMethylthioamphetamineA1,
  title={p‐Methylthioamphetamine and 1‐(m‐chlorophenyl)piperazine, two non‐neurotoxic 5‐HT releasers in vivo, differ from neurotoxic amphetamine derivatives in their mode of action at 5‐HT nerve endings in vitro},
  author={Marco Gobbi and M Moia and Lorenza Pirona and Ilaria Ceglia and Miguel Reyes-Parada and Cecilia Dagert de Scorza and Tiziana Mennini},
  journal={Journal of Neurochemistry},
  year={2002},
  volume={82}
}
The mechanism underlying the serotoninergic neurotoxicity of some amphetamine derivatives, such as p‐chloroamphetamine (pCA) and 3,4‐methylenedioxymethamphetamine (MDMA), is still debated. Their main acute effect, serotonin (5‐HT) release from nerve endings, involves their interaction with 5‐HT transporters (SERTs), as substrates. Although this interaction is required for the neurotoxic effects, 5‐HT release alone may not be sufficient to induce long‐term 5‐HT deficits. Some non‐neurotoxic… 
N,N‐dimethyl‐thioamphetamine and methyl‐thioamphetamine, two non‐neurotoxic substrates of 5‐HT transporters, have scant in vitro efficacy for the induction of transporter‐mediated 5‐HT release and currents
TLDR
It is confirmed that the neurotoxic properties of some amphetamine derivatives are independent of their 5‐HT‐releasing activity in vivo, and only those amphetamines with high efficiency in inducing 5‐ HT release and currents in vitro have neurot toxic properties.
4‐Methylthioamphetamine Increases Dopamine in the Rat Striatum and has Rewarding Effects In Vivo
TLDR
Results show that MTA is able to increase extracellular striatal DA levels and that its administration has rewarding properties and these effects were observed at concentrations or doses that can be relevant to its use in human beings.
Pharmacological Characterization of 4-Methylthioamphetamine Derivatives
TLDR
The results show that the pharmacological and safety profiles of MTA are modulated by changing the methyl-thio group or the methyl group of the aminoethyl chain.
Proof of a 1-(3-chlorophenyl)piperazine (mCPP) intake: use as adulterant of cocaine resulting in drug-drug interactions?
Synthesis of Fluoro Analogues of 3,4‐(Methylenedioxy)amphetamine (MDA) and Its Derivatives
TLDR
Six new 3,4‐(difluoromethylenedioxy) analogues of MDMA were prepared and characterized, and may help to verify the hypothesis that MDMA‐induced neurotoxicity is the result of the formation of metabolites lacking the methylenedioXY bridge.
Amphetamines take two to tango: an oligomer-based counter-transport model of neurotransmitter transport explores the amphetamine action.
TLDR
It is proposed that, in the presence of amphetamine analogs, monoamine transporters operate as counter-transporters; influx and efflux occur through separate but coupled moieties.
Effect fingerprinting of new psychoactive substances (NPS): What can we learn from in vitro data?
Endogenous 5-HT outflow from chicken aorta by 5-HT uptake inhibitors and amphetamine derivatives
TLDR
The results suggest that the 5-HT uptake system of5-HT-containing chemoreceptor cells in the chicken thoracic aorta has characteristics similar to those of 5- HT-containing neurons in the mammalian central nervous system (CNS).
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