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

[摘要] References(15)Cited-By(8)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 (Kd=0.15±0.01 nM, Bmax=653±30 fmol/mg protein) than [3H]granisetron (Kd=1.17±0.25 nM, Bmax=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.

[学科分类] 药理学

[关键词] Ramosetron;Granisetron;5-HT3 receptor