TRYPTOLINE INHIBITION OF SEROTONIN UPTAKE IN RAT FOREBRAIN HOMOGENATES

  • 1 January 1976
    • journal article
    • research article
    • Vol. 198  (3) , 619-625
Abstract
The effects of 6 tryptolines (tetrahydro-.beta.-carbolines) were studied on 5-hydroxytryptamine [5-HT serotonin] uptake into rat forebrain homogenates. All 6 were competitive inhibitors of 5-HT uptake. 5-Hydroxytryptoline, the most potent inhibitor, had an inhibitor constant (Ki) of 0.3 .mu.M. Both 5-hydroxytryptoline and 5-hydroxymethtryptoline were also relatively selective against 5-HT uptake, being 20 times less potent against norepinephrine uptake and 40 times less potent against dopamine. Since it is possible that tryptolines might be formed as a result of alcohol consumption, it is important to examine the possibilities that such compounds mediate some of the effects of alcohol upon serotonergic pathways.