INHIBITION OF SYNAPTOSOMAL SEROTONIN UPTAKE BY KETALAR

  • 1 October 1988
    • journal article
    • letter
    • Vol. 62  (1) , 129-132
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 (50 = 20.2 .+-. 2.75 .mu.M) while benzethonium chloride had no effect. Kinetic analysis indicated the inhibition to be competitive with serotonin; the apparent km (54 nM) was increased nearly two-fold at 10 .mu.M ketamine. This action may represent a mechanism involved in ketamine anesthesia.