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The Designer Methcathinone Analogs, Mephedrone and Methylone, are Substrates for Monoamine Transporters in Brain Tissue
In vitro and in vivo methods demonstrate that designer methcathinone analogs are substrates for monoamine transporters, with a profile of transmitter-releasing activity comparable to MDMA. Expand
Amphetamine‐type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin
In vitro methods determined the neurochemical mechanism of action of amphetamine, 3,4‐methylenedioxymethamphetamine (MDMA), (+)‐methamphetamine, ephedrine, phentermine, and aminorex, and demonstrated that the most potent effect of these stimulants is to release NE. Expand
Powerful Cocaine-Like Actions of 3,4-Methylenedioxypyrovalerone (MDPV), a Principal Constituent of Psychoactive ‘Bath Salts’ Products
The data show that MDPV is a monoamine transporter blocker with increased potency and selectivity for catecholamines when compared with cocaine, and may provide a mechanism to explain the adverse effects observed in humans taking high doses of ‘bath salts’ preparations. Expand
N-Desalkylquetiapine, a Potent Norepinephrine Reuptake Inhibitor and Partial 5-HT1A Agonist, as a Putative Mediator of Quetiapine's Antidepressant Activity
The data strongly suggest that the antidepressant activity of quetiapine is mediated, at least in part, by its metabolite N-DesalkylquetiAPine through NET inhibition and partial 5-HT1A agonism. Expand
Salvinorin A: A potent naturally occurring nonnitrogenous κ opioid selective agonist
Salvia divinorum, whose main active ingredient is the neoclerodane diterpene Salvinorin A, is a hallucinogenic plant in the mint family that has been used in traditional spiritual practices for itsExpand
N-Substituted Piperazines Abused by Humans Mimic the Molecular Mechanism of 3,4-Methylenedioxymethamphetamine (MDMA, or ‘Ecstasy’)
The results show that BZP/TFMPP and MDMA share the ability to evoke monoamine release, but dangerous drug–drug synergism may occur when piperazines are coadministered at high doses. Expand
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.
Salvinorin A is the first naturally occurring nonnitrogenous opioid-receptor subtype-selective agonist for kappa opioid receptors, and may represent novel psychotherapeutic compounds for diseases manifested by perceptual distortions (e.g., schizophrenia, dementia, and bipolar disorders). Expand
SNC 80, a selective, nonpeptidic and systemically active opioid delta agonist.
The present study has investigated the pharmacology of SNC 80, a nonpeptidic ligand proposed to be a selective delta agonist in vitro and in vivo. SNC 80 was potent in producing inhibition ofExpand
Monoamine transporters and psychostimulant drugs.
The brain contains high abundance nonclassical binding sites for cocaine-like drugs that have micromolar affinity for cocaine and that none of the clinically available amphetamine-type appetite suppressants are equipotent substrates for dopamine transporter (DAT) and serotonin transporter (SERT) proteins. Expand
A proposal for the classification of sigma binding sites.