Structural specificity for inhibition of [14C]-5-hydroxytryptamine uptake by cerebral slices

Abstract

Cerebral slices were prepared from mice pretreated with reserpine and nialamide. The slices were incubated for 40 min at 37° in a Krebs-Henseleit solution equilibrated with 5% carbon dioxide in oxygen and containing [14C]-5-hydroxytryptamine. An uptake, dependent on energy metabolism and temperature, was observed. The uptake was blocked by tricyclic antidepressants, the order of activity being chlorimipramine > imipramine > desipramine. For 50% inhibition 0.03 μg/ml of chlorimipramine was required, when added to the suspension medium, or 1 mg/kg, when injected intraperitoneally 20 min beforehand. Comparison with earlier experiments using different experimental techniques appears to justify the conclusion that the evidence obtained represents the uptake mechanism of cerebral 5-hydroxytryptamine neurons.