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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.
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.
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.
N-Desalkylquetiapine, a Potent Norepinephrine Reuptake Inhibitor and Partial 5-HT1A Agonist, as a Putative Mediator of Quetiapine's Antidepressant Activity
- Niels H. Jensen, R. Rodriguiz, M. Caron, W. Wetsel, R. Rothman, B. Roth
- Psychology, BiologyNeuropsychopharmacology
- 1 September 2008
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.
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 of…
Salvinorin A: A potent naturally occurring nonnitrogenous κ opioid selective agonist
Salvinorin A is the first naturally occurring nonnitrogenous opioid-receptor subtype-selective agonist for κ opioid receptors and may represent novel psychotherapeutic compounds for diseases manifested by perceptual distortions (e.g., schizophrenia, dementia, and bipolar disorders).
A proposal for the classification of sigma binding sites.
Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist.
- B. Roth, K. Baner, R. Rothman
- Biology, PsychologyProceedings of the National Academy of Sciences…
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).
Depressive-Like Effects of the κ-Opioid Receptor Agonist Salvinorin A on Behavior and Neurochemistry in Rats
- W. Carlezon, C. Béguin, B. Cohen
- Biology, PsychologyJournal of Pharmacology and Experimental…
- 1 January 2006
SalvA data provide additional support for the hypothesis that stimulation of brain κ-opioid receptors triggers depressive-like signs in rats and raise the possibility that decreases in extracellular concentrations of DA within the NAc contribute to these effects.
Evidence for the Involvement of Dopamine Transporters in Behavioral Stimulant Effects of Modafinil
- D. Żółkowska, R. Jain, M. Baumann
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 May 2009
The data show that modafinil interacts with DAT sites in rat brain, a property shared with agonist medications under investigation for treating cocaine dependence, and suggest that modAFinil should be tested as an adjunct for treating METH addiction.