Elsevier

Life Sciences

Volume 18, Issue 12, 15 June 1976, Pages 1459-1465
Life Sciences

Selective inhibition of serotonin uptake by trazodone, a new antidepressant agent

https://doi.org/10.1016/0024-3205(76)90364-7Get rights and content

Abstract

The inhibitory effect of trazodone, a non tricyclic antidepressant, on 5-HT and catecholamine uptake into the synaptosomal preparation from the rat brain was compared with that of chlorimipramine. The inhibition of 5-HT uptake by trazodone is competitive with a Ki of 1.6 × 10−6 M. Trazodone inhibits 3H-5-HT, 3H-NE and 3H-DA uptake with an IC50 of 1.4 × 10−6, 3.1 × 10−4 and 5.2 × 10−4 M, respectively. Therefore trazodone is 220 and 370 times more potent in inhibiting 5-HT than NE and DA uptake, respectively. The respective IC50 values of chlorimipramine were 0.9 × 10−7, 3.6 × 10−6 and 4.0 × 10−6 M for 3H-5-HT, 3H-NE and 3H-DA.

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