Effects of enflurane on 5-hydroxytryptamine transport in synaptosomes from rat brain

Dan C Martin, Robert J. Adams, Robert S. Aronstam

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

The administration of volatile anesthetics to laboratory animals has been reported to alter brain 5-hydroxytryptamine (serotonin, 5-HT) homeostasis. To examine a potential anesthetic action that could account for these observations, the effect of enflurane on 5-HT accumulation by rat brain synaptosomes was examined. Established techniques were used to prepare synaptosomes and perform uptake assays using [3H]5-hydroxytryptamine as substrate. Exposure of the synaptosomes to enflurane 0resulted in a concentration-dependent inhibition of serotonin uptake; the apparent I50 was 1.4 ± 0.3 mM enflurane. Maximum inhibition was observed between enflurane concentrations of 2.6 and 4.3 mM, which inhibited uptake between 62 and 70%. The inhibition was rapid and reversible, and kinetic analysis of the inhibition was consistent with competitive inhibition by enflurane of 5-HT uptake with an apparent K1 of 1.61 ± 0.07 mM. In summary, exposure of synaptosomes to clinically relevant concentrations of enflurane resulted in a rapid, concentration-dependent, and reversible inhibition of 5-HT accumulation. These observations could represent a molecular interaction contributing to the anesthetic properties of enflurane and other volatile anesthetics.

Original languageEnglish (US)
Pages (from-to)187-192
Number of pages6
JournalBiochemical Pharmacology
Volume40
Issue number2
DOIs
StatePublished - Jul 15 1990

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Enflurane
Synaptosomes
Rats
Brain
Serotonin
Anesthetics
Molecular interactions
Laboratory Animals
Action Potentials
Assays
Animals
Homeostasis
Kinetics
Substrates

ASJC Scopus subject areas

  • Biochemistry
  • Pharmacology

Cite this

Effects of enflurane on 5-hydroxytryptamine transport in synaptosomes from rat brain. / Martin, Dan C; Adams, Robert J.; Aronstam, Robert S.

In: Biochemical Pharmacology, Vol. 40, No. 2, 15.07.1990, p. 187-192.

Research output: Contribution to journalArticle

Martin, Dan C ; Adams, Robert J. ; Aronstam, Robert S. / Effects of enflurane on 5-hydroxytryptamine transport in synaptosomes from rat brain. In: Biochemical Pharmacology. 1990 ; Vol. 40, No. 2. pp. 187-192.
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