title: 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.
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.
authors.affiliation: Department of Pharmacology, Oita Medical University, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Goto
authors.forename: T
authors.initials: T
authors.lastname: Egashira
authors.forename: Y
authors.initials: Y
authors.lastname: Wada
authors.forename: F
authors.initials: F
authors.lastname: Takayama
authors.forename: Y
authors.initials: Y
authors.lastname: Yamanaka
mesh_terms: D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001792:Blood Platelets / Q000378:metabolism*; D001921:Brain / Q000378:metabolism*; D002540:Cerebral Cortex / Q000378:metabolism*; D016666:Fluvoxamine / Q000494:pharmacology*; D066298:In Vitro Techniques; D007650:Ketanserin / Q000378:metabolism*; D008251:Macaca; D008297:Male; D017374:Paroxetine / Q000378:metabolism*; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism; D012701:Serotonin / Q000493:pharmacokinetics*; D017367:Selective Serotonin Reuptake Inhibitors / Q000494:pharmacology*
chemical_list: D016666:Fluvoxamine; D007650:Ketanserin; D017374:Paroxetine; D011985:Receptors, Serotonin; D012701:Serotonin; D017367:Selective Serotonin Reuptake Inhibitors