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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.
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.
N-Substituted Piperazines Abused by Humans Mimic the Molecular Mechanism of 3,4-Methylenedioxymethamphetamine (MDMA, or ‘Ecstasy’)
- M. Baumann, R. D. Clark, Allison G Budzynski, J. Partilla, B. Blough, R. Rothman
- Biology, ChemistryNeuropsychopharmacology
- 1 March 2005
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.
Monoamine transporters and psychostimulant drugs.
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.
Evidence for Possible Involvement of 5-HT2B Receptors in the Cardiac Valvulopathy Associated With Fenfluramine and Other Serotonergic Medications
It is suggested that all clinically available medications with serotonergic activity and their active metabolites be screened for agonist activity at 5-HT2B receptors and that clinicians should consider suspending their use of medications with significant activity at5-HT1B receptors.
3,4-Methylenedioxymethamphetamine (MDMA) neurotoxicity in rats: a reappraisal of past and present findings
MDMA-induced 5- HT depletions are not necessarily synonymous with neurotoxic damage, however, doses of MDMA which do not cause long-term 5-HT depletion can have protracted effects on behavior, suggesting even moderate doses of the drug may pose risks.
Relationship between the Serotonergic Activity and Reinforcing Effects of a Series of Amphetamine Analogs
- S. Wee, K. Anderson, M. Baumann, R. Rothman, B. Blough, W. Woolverton
- BiologyJournal of Pharmacology and Experimental…
- 1 May 2005
The results suggest that the mechanism for this effect involves a decrease in reinforcing potency and efficacy among monoamine releasing agents when 5-HT releasing potency is increased relative to DA.