Document Detail

In vivo pharmacology of MDMA and its enantiomers in rhesus monkeys.
MedLine Citation:
PMID:  18266547     Owner:  NLM     Status:  MEDLINE    
The chiral nature of the MDMA molecule gives rise to two enantiomers, each of which is biologically active. This review attempts to cover the author's research into the in vivo effects of MDMA and its enantiomers, as well as other relevant publications which pertain to this topic. No particular differences between the capacities of racemic MDMA and its enantiomers to maintain behavior were noted, but antagonism of the 5-HT2A receptor produces a parallel rightward shift in the dose-effect function for the S(+)-enantiomer, but insurmountably reduces the reinforcing effects of R(-)-MDMA. Long-term self-administration of MDMA may lead to the development of chronic tolerance to the reinforcing effects of MDMA, but S(+)-MDMA is somewhat less susceptible to this effect than the racemate or the R(-)-enantiomer. Using PET neuroimaging, negligible occupancy at the dopamine transporter (DAT) was observed following administration of R(-)-MDMA, but reasonable DAT interaction was quantified following injection of S(+)-MDMA. The non-human primate studies reviewed herein caution that any results obtained in vivo with the MDMA enantiomers may not be particularly informative with regards to the racemate and vice versa.
William E Fantegrossi
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural    
Journal Detail:
Title:  Experimental and clinical psychopharmacology     Volume:  16     ISSN:  1064-1297     ISO Abbreviation:  Exp Clin Psychopharmacol     Publication Date:  2008 Feb 
Date Detail:
Created Date:  2008-02-12     Completed Date:  2008-03-06     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9419066     Medline TA:  Exp Clin Psychopharmacol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1-12     Citation Subset:  IM    
Copyright Information:
2008 APA
Department of Pharmacology and Toxicology, College of Medicine, University of Arkansas for Medical Sciences, Little Rock, AR 72205-7199, USA.
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MeSH Terms
Dopamine Plasma Membrane Transport Proteins / analysis,  drug effects
Dose-Response Relationship, Drug
Fluorobenzenes / pharmacology
Macaca mulatta
N-Methyl-3,4-methylenedioxyamphetamine / administration & dosage,  pharmacology*
Piperidines / pharmacology
Positron-Emission Tomography
Reinforcement (Psychology)
Self Administration
Serotonin Antagonists / pharmacology
Grant Support
Reg. No./Substance:
0/Dopamine Plasma Membrane Transport Proteins; 0/Fluorobenzenes; 0/Piperidines; 0/Serotonin Antagonists; 139290-65-6/MDL 100907; 42542-10-9/N-Methyl-3,4-methylenedioxyamphetamine

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