Akuzawa S, Ito H, Yamaguchi T
Neuroscience Research, Pharmacology Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd., Tsukuba, Ibaraki, Japan.
Jpn J Pharmacol. 1998 Nov;78(3):381-4. doi: 10.1254/jjp.78.381.
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.
研究了[3H]雷莫司琼与克隆的人5-羟色胺3（5-HT3）受体结合的特性，并将其与[3H]格拉司琼的结合特性进行了直接比较。饱和研究表明，与[3H]格拉司琼（Kd = 1.17 +/- 0.25 nM，Bmax = 427 +/- 43 fmol/mg蛋白质）相比，[3H]雷莫司琼标记的高亲和力位点更多（Kd = 0.15 +/- 0.01 nM，Bmax = 653 +/- 30 fmol/mg蛋白质）。动力学研究表明，[3H]雷莫司琼的解离比[3H]格拉司琼慢。这些结果表明雷莫司琼是一种高效的5-HT3受体拮抗剂。
