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

• Published in: Japanese Journal of Pharmacology Vol. 71; no. 4; pp. 291 - 298
• Main Authors: Goto, Shinichiro, Egashira, Toru, Wada, Yuji, Takayama, Fusako, Yamanaka, Yasumitsu
• Format: Journal Article
• Language: English
• Published: Japan The Japanese Pharmacological Society 1996
• Subjects: 5-Hydroxytryptamine uptake; Animals; Binding, Competitive - drug effects; Blood Platelets - metabolism; Brain - metabolism; Cerebral Cortex - metabolism; Fluvoxamine; Fluvoxamine - pharmacology; In Vitro Techniques; Ketanserin - metabolism; Macaca; Male; Monkey brain; Monkey platelet; Paroxetine - metabolism; Paroxetine binding; Receptors, Serotonin - drug effects; Receptors, Serotonin - metabolism; Serotonin - pharmacokinetics; Serotonin Uptake Inhibitors - pharmacology; Monkey platelet; Paroxetine binding; Fluvoxamine; Monkey brain; 5-Hydroxytryptamine uptake
• ISSN: 0021-5198; 1347-3506
• DOI: 10.1254/jjp.71.291

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.