Inhibition of synaptosomal serotonin uptake by Ketalar.
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.
Martin
D C
DC
Department of Anesthesiology, Medical College of Georgia, Augusta 30912-2700.
Adams
R J
RJ
Watkins
C A
CA
D000818:Animals; D001558:Benzethonium / Q000494:pharmacology; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D007649:Ketamine / Q000494:pharmacology*; D007700:Kinetics; D051381:Rats; D011919:Rats, Inbred Strains; D012701:Serotonin / Q000378:metabolism*; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism*
D001558:Benzethonium; D012701:Serotonin; D007649:Ketamine