Release studies with rat brain cortical synaptosomes indicate that tramadol is a 5-hydroxytryptamine uptake blocker and not a 5-hydroxytryptamine releaser

Marco Gobbi, Tiziana Mennini

Research output: Contribution to journalArticle

Abstract

Tramadol is a centrally acting opioid analgesic whose mechanism of action could also involve an increase in central serotoninergic transmission. Thus, tramadol inhibits synaptosomal serotonin (5-hydroxytryptamine, 5-HT) reuptake and induces tritium release from [3H]5-HT-preloaded slices. We investigated the effect of (±)-tramadol in release studies with superfused rat brain cortex synaptosomes preloaded with [3H]5-HT. Tramadol had no releasing effect up to 30 μM, whereas at 10 μM tramadol significantly inhibited by 45% d-fenfluramine-induced [3H]5-HT release. At 100 μM, tramadol showed a slight releasing effect in the absence or in the presence of pargyline, which was not augmented in synaptosomes pre-exposed to Ro 04-1284 (2-ethyl-1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-2H-benzo [a]quinolizin-2-ol hydrochloride), a reserpine-like compound that enhances cytoplasmic 5-HT levels. In summary, (±)-tramadol behaved as a classical 5-HT uptake blocker (like citalopram) and not as a substrate of the 5-HT carrier with indirect 5-HT mimetic properties (like d-fenfluramine). Copyright (C) 1999 Elsevier Science B.V.

Original languageEnglish
Pages (from-to)23-26
Number of pages4
JournalEuropean Journal of Pharmacology
Volume370
Issue number1
DOIs
Publication statusPublished - Apr 1 1999

Keywords

  • (±)-Tramadol
  • 5-HT (5-hydroxytryptamine, serotonin) carrier
  • 5-HT (5-hydroxytryptamine, serotonin) release
  • Synaptosome

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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