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

The Japanese Journal of Pharmacology

Hiroyuki Ito¹  Shinobu Akuzawa¹  Tokio Yamaguchi¹ 

[1] Neuroscience Research, Pharmacology Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

关键词: Ramosetron;    Granisetron;    5-HT3 receptor;   

DOI  :  10.1254/jjp.78.381

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 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.

【 授权许可】

Unknown