Inhibition of synaptosomal serotonin uptake by Ketalar

Dan C Martin, R. J. Adams, C. A. Watkins

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

The effects of the clinical preparation of ketamine, Ketalar and its preservative, benzethonium chloride on [3H]5-hydroxytryptamine uptake were studied using rat brain synaptosomes. Ketalar caused a concentration-dependent inhibition of substrate uptake by the high affinity transport site (I50 = 20.2 ± 2.75 μM) while benzethonium chloride had no effect. Kinetic analysis indicated the inhibition to be competitive with serotonin; the apparent k(m) (54 nM) was increased nearly two-fold at 10 μM ketamine. This action may represent a mechanism involved in ketamine anesthesia.

Original languageEnglish (US)
Pages (from-to)129-132
Number of pages4
JournalResearch Communications in Chemical Pathology and Pharmacology
Volume62
Issue number1
StatePublished - Jan 1 1988

ASJC Scopus subject areas

  • Pathology and Forensic Medicine
  • Toxicology
  • Pharmacology
  • Pharmacology, Toxicology and Pharmaceutics(all)

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