Comparative Study of [3H]Ramosetron and [3H]Granisetron Binding in the Cloned Human 5-Hydroxytryptamine3 Receptors

Shinobu Akuzawa; Hiroyuki Ito; Tokio Yamaguchi

doi:10.1254/jjp.78.381

Short Communications

Comparative Study of [³H]Ramosetron and [³H]Granisetron Binding in the Cloned Human 5-Hydroxytryptamine₃ Receptors

Shinobu Akuzawa, Hiroyuki Ito, Tokio Yamaguchi

著者情報

キーワード: Ramosetron, Granisetron, 5-HT₃ receptor

ジャーナルフリー

1998 年 78 巻 3 号 p. 381-384

DOI https://doi.org/10.1254/jjp.78.381

詳細

抄録

Characteristics of the binding of [³H]ramosetron to cloned human 5-hydroxytryptamine₃ (5-HT₃) receptors were investigated and directly compared to those of [³H]granisetron binding. Saturation studies revealed that [³H]ramosetron labeled more sites with high affinity (K_d=0.15±0.01 nM, B_max=653±30 fmol/mg protein) than [³H]granisetron (K_d=1.17±0.25 nM, B_max=427±43 fmol/mg protein). Kinetic studies revealed that dissociation of [³H]ramosetron was slower than that of [³H]granisetron. These results suggest that ramosetron is a highly potent 5-HT₃-receptor antagonist.

責任著者(Corresponding author)

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