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The substituted amphetamines 3,4-methylenedioxymethamphetamine, methamphetamine, p-chloroamphetamine and fenfluramine induce 5-hydroxytryptamine release via a common mechanism blocked by fluoxetine and cocaine.
Eur J Pharmacol. 1992 May 14; 215(2-3):153-60.EJ

Abstract

The abilities of the substituted amphetamines 3,4-methylenedioxymethamphetamine (MDMA), methamphetamine, p-chloroamphetamine (PCA) and fenfluramine to induce synaptosomal [3H]serotonin (5-HT) release were compared using a novel microassay system. The rank order of release potencies was found to be (+/-)PCA congruent to (+)-fenfluramine greater than (+)-MDMA much greater than (+)-methamphetamine. Combination of two drugs at their EC50 did not cause more release than either drug alone at an equivalent concentration. In addition, the 5-HT uptake blockers fluoxetine and cocaine inhibited the release induced by MDMA, methamphetamine, PCA and fenfluramine to the same percentage. However, threshold concentrations of the substituted amphetamines known to inhibit uptake did not attenuate the release caused by higher concentrations of these compounds. These results suggests that MDMA, methamphetamine, PCA and fenfluramine cause 5-HT release via a common mechanism. Furthermore, these results indicate that the 5-HT uptake blockade induced by these substituted amphetamines in vitro is different from that induced by either fluoxetine or cocaine.

Authors+Show Affiliations

Department of Biology, New York University, NY 10003.No affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

1356787

Citation

Berger, U V., et al. "The Substituted Amphetamines 3,4-methylenedioxymethamphetamine, Methamphetamine, P-chloroamphetamine and Fenfluramine Induce 5-hydroxytryptamine Release Via a Common Mechanism Blocked By Fluoxetine and Cocaine." European Journal of Pharmacology, vol. 215, no. 2-3, 1992, pp. 153-60.
Berger UV, Gu XF, Azmitia EC. The substituted amphetamines 3,4-methylenedioxymethamphetamine, methamphetamine, p-chloroamphetamine and fenfluramine induce 5-hydroxytryptamine release via a common mechanism blocked by fluoxetine and cocaine. Eur J Pharmacol. 1992;215(2-3):153-60.
Berger, U. V., Gu, X. F., & Azmitia, E. C. (1992). The substituted amphetamines 3,4-methylenedioxymethamphetamine, methamphetamine, p-chloroamphetamine and fenfluramine induce 5-hydroxytryptamine release via a common mechanism blocked by fluoxetine and cocaine. European Journal of Pharmacology, 215(2-3), 153-60.
Berger UV, Gu XF, Azmitia EC. The Substituted Amphetamines 3,4-methylenedioxymethamphetamine, Methamphetamine, P-chloroamphetamine and Fenfluramine Induce 5-hydroxytryptamine Release Via a Common Mechanism Blocked By Fluoxetine and Cocaine. Eur J Pharmacol. 1992 May 14;215(2-3):153-60. PubMed PMID: 1356787.
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TY - JOUR T1 - The substituted amphetamines 3,4-methylenedioxymethamphetamine, methamphetamine, p-chloroamphetamine and fenfluramine induce 5-hydroxytryptamine release via a common mechanism blocked by fluoxetine and cocaine. AU - Berger,U V, AU - Gu,X F, AU - Azmitia,E C, PY - 1992/5/14/pubmed PY - 1992/5/14/medline PY - 1992/5/14/entrez SP - 153 EP - 60 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 215 IS - 2-3 N2 - The abilities of the substituted amphetamines 3,4-methylenedioxymethamphetamine (MDMA), methamphetamine, p-chloroamphetamine (PCA) and fenfluramine to induce synaptosomal [3H]serotonin (5-HT) release were compared using a novel microassay system. The rank order of release potencies was found to be (+/-)PCA congruent to (+)-fenfluramine greater than (+)-MDMA much greater than (+)-methamphetamine. Combination of two drugs at their EC50 did not cause more release than either drug alone at an equivalent concentration. In addition, the 5-HT uptake blockers fluoxetine and cocaine inhibited the release induced by MDMA, methamphetamine, PCA and fenfluramine to the same percentage. However, threshold concentrations of the substituted amphetamines known to inhibit uptake did not attenuate the release caused by higher concentrations of these compounds. These results suggests that MDMA, methamphetamine, PCA and fenfluramine cause 5-HT release via a common mechanism. Furthermore, these results indicate that the 5-HT uptake blockade induced by these substituted amphetamines in vitro is different from that induced by either fluoxetine or cocaine. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/1356787/The_substituted_amphetamines_34_methylenedioxymethamphetamine_methamphetamine_p_chloroamphetamine_and_fenfluramine_induce_5_hydroxytryptamine_release_via_a_common_mechanism_blocked_by_fluoxetine_and_cocaine_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0014-2999(92)90023-W DB - PRIME DP - Unbound Medicine ER -