| Acute administration of methylenedioxymethamphetamine: comparison with the neurochemical effects of its N-desmethyl and N-ethyl analogs. | |
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MedLine Citation:
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PMID: 2885204 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The acute and long-term neurochemical effects of three methylenedioxyamphetamine analogs were examined in the serotonergic system of the rat brain. Methylenedioxymethamphetamine as well as its N-desmethyl and N-ethyl derivatives depleted cortical serotonin (5HT) concentrations to less than 30% of control 3 h after drug administration. All three compounds were also very similar in their effects on [3H]5HT release from superfused rat striatal slices. Increasing the size of the N-alkyl substituent did appear to reduce the potency of the agent for inducing [3H]dopamine release. One week following drug administration cortical 5HT concentrations had returned to control levels in animals treated with the N-ethyl derivative while the other two analogs produced persistent depletions in transmitter concentrations. The effects of the latter two drugs were correlated with a significant decrease in whole brain synaptosomal [3H]5HT uptake indicating serotonergic nerve terminal damage. N-ethyl-methylenedioxyamphetamine had no effect on synaptosomal 5HT uptake at one week. The (+) stereoisomer of methylenedioxyamphetamine was slightly more potent than the (-) enantiomer at producing the long-term 5HT depletion as previously shown for its N-methyl derivative suggesting similar mechanisms may be responsible for their neurotoxic effects. |
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Authors:
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C J Schmidt |
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Publication Detail:
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Type: Comparative Study; Journal Article |
Journal Detail:
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Title: European journal of pharmacology Volume: 136 ISSN: 0014-2999 ISO Abbreviation: Eur. J. Pharmacol. Publication Date: 1987 Apr |
Date Detail:
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Created Date: 1987-07-24 Completed Date: 1987-07-24 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 1254354 Medline TA: Eur J Pharmacol Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 81-8 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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3,4-Methylenedioxyamphetamine
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analogs & derivatives,
pharmacology* Amphetamines / pharmacology* Animals Brain Chemistry / drug effects* Cerebral Cortex / drug effects, metabolism Male N-Methyl-3,4-methylenedioxyamphetamine Rats Rats, Inbred Strains Serotonin / metabolism* Stereoisomerism Synaptosomes / drug effects, metabolism |
| Chemical | |
Reg. No./Substance:
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0/Amphetamines; 42542-10-9/N-Methyl-3,4-methylenedioxyamphetamine; 4764-17-4/3,4-Methylenedioxyamphetamine; 50-67-9/Serotonin; 82801-81-8/3,4-methylenedioxyethamphetamine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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