| 产品描述: | 5-HT3 选择性抑制剂 | 激动剂 | 拮抗剂 | 调节剂;5-HT3 Selective Inhibitors | Agonists | Antagonists | Modulators;产品说明:Lerisetron (F 0930, F 0930RS) 是一种 5-HT3 receptor 拮抗剂,IC50为0.81μM。;InformationLerisetron (F 0930, F 0930RS) is a5-HT3 receptorantagonist with IC50 of 0.81μM.Targets5-HT3 receptor (Cell-free assay) 0.81 μM |
| 靶点: |
pKi: 9.2 (5-HT3) |
| 体内研究: |
Lerisetron (50-200 μg/kg; IV; single) exhibits CL of 0.004-0.005 L/min, Vds of 0.88-0.96 L, MRT0-LAST of 224-337.1 min and AUC∞ of 57.7-66.1 μg·min/L in rats. Lerisetron (2-10 μg/kg; IV; single) causes rapid recovery from bradycardia. Pharmacokinetic Parameters of Lerisetron in Sprague-Dawley rats. |
| 参考文献: |
1. Orjales A, Mosquera R, Labeaga L, Rodes R. New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation. J Med Chem. 1997;40(4):586-593.2. Jauregizar N, Calvo R, Suarez E, Quintana A, Raczka E, Lukas JC. Pharmacokinetics and pharmacological effect of lerisetron, a new 5-HT3 antagonist, in rats. J Pharm Sci. 2002;91(1):41-52. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.42 ml |
17.101 ml |
34.202 ml |
| 5 mM |
0.684 ml |
3.42 ml |
6.84 ml |
| 10 mM |
0.342 ml |
1.71 ml |
3.42 ml |
| 50 mM |
0.068 ml |
0.342 ml |
0.684 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |