Jpn. J. Pharmacol. 71 (4), 291-298 (1996)

Effect of Fluvoxamine on 5-Hydroxytryptamine Uptake, Paroxetine Binding Sites and Ketanserin Binding Sites in the Japanese Monkey Brain and Platelets, In Vivo and In Vitro

Shinichiro Goto, Toru Egashira (*), Yuji Wada, Fusako Takayama and Yasumitsu Yamanaka

Department of Pharmacology, Oita Medical University,1-1, Idaigaoka, Hasama-machi, Oita 879-55, Japan (*) To whom correspondence should be addressed.

Abstract: We investigated the in vitro effects of fluvoxamine on 3H-paroxetine binding and 3H-monoamine uptake in monkey cerebral cortex in comparison with those of other antidepressants. Fluvoxamine selectively inhibited 3H-5-hydroxytryptamine (5-HT) uptake and 3H-paroxetine binding. However, it did not alter 3H-norepinephrine or 3H-dopamine uptake. In addition, we examined the effects of chronic treatment with fluvoxamine (5 mg/kg per day, p.o.) on 5-HT uptake sites that bind 3H-paroxetine and 5-HT2 receptors that bind 3H-ketanserin, in monkey brains and platelets. Chronic treatment with fluvoxamine affected neither the paroxetine binding sites nor the kentanserin binding sites of the brains and platelets. These results suggest that long-term treatment with fluvoxamine does not affect either the 5-HT uptake sites or 5-HT2-receptors of 5-HT neurons in monkey brain in spite of its strong inhibitory effect on 5-HT uptake in vitro.

Keywords: Fluvoxamine, 5-Hydroxytryptamine uptake, Paroxetine binding, Monkey brain, Monkey platelet

Copyright© The Japanese Pharmacological Society 1996

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