Inhibition of synaptosomal serotonin uptake by Ketalar
Martin, D.C.; Adams, R.J.; Watkins, C.A.
Research Communications in Chemical Pathology and Pharmacology 62(1): 129-132
1988
ISSN/ISBN: 0034-5164 PMID: 3205973 Document Number: 319970
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 microM) 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 microM ketamine. This action may represent a mechanism involved in ketamine anesthesia.