Selective inhibition of serotonin uptake by trazodone,a new antidepressant agent |
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| Authors: | Ennio Stefanini Fabio Fadda Lucio Medda Gian Luigi Gessa |
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| Institution: | 1. Institute of Pharmacology, University of Cagliari, 09100 Cagliari, Italy;1. Institute of Physiology, University of Cagliari, 09100 Cagliari, Italy |
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| 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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