Buckholtz1977
Inhibition by β-carbolines of monoamine uptake into a synaptosomal preparation: Structure-activity relationships. Buckholtz, N. S., Boggan, W. O. 1977. Life Sciences, 20(12), 2093–2100. 10.1016/0024-3205(77)90190-4 Charleston, S.C. 29401 (Received in final form May 23, 1977) The potency of a series of β-carboline compounds to inhibit ³H-serotonin (³H-5-HT) uptake into a synaptosomal suspension from mouse brain was studied. The in vitro structure-activity study showed the tetrahydro-β-carbolines to be the most potent inhibitors compared to unsaturated β-carbolines. In vitro inhibition of ³H-norepinephrine (³H-NE) and ³H-dopamine (³H-DA) uptake was determined for some tetrahydro-β-carbolines, and the degree of inhibition of uptake of these amines was less than that for ³H-5-HT. EC50s being 5-13 times those for ³H-5-HT. The tetrahydro-β-carbolines were also found to effectively inhibit ³H-5-HT but not ³H-NE or ³H-DA uptake ...