| 常用名 | 盐酸格拉司琼 | CAS号 | 107007-99-8 |
|---|---|---|---|
| 价格 | ¥需询单/1kg | 纯度 | 99.0% |
| 备货期 | 需询单 | 库存 | 询单 |
| 产品详情(用途,包装等)
用途: Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.IC50 Value: 17uM (GR reduced 5-HT-evoked contractions) [1]Target: 5-HT3 receptorin vitro: In rat forestomach GR reduced 5-HT-evoked contractions at IC50 17 /- 6 uM. In isolated rabbit heart, GR 0.003-0.03 nM dose-dependently reduced s-HT tachycardia; at high levels GR reduced submaximal and maximal responses to 5-HT [1].in vivo: Leukocyte accumulation was dose-dependently inhibited by granisetron both at 6 and 72 h after induction of inflammation. Granisetron increased PGE(2) level at a lower dose (50 microg/pouch) but higher doses (100 and 200 microg/pouch) inhibited the release. At the same time, TNFalpha production was decreased by the lower dose and increased by higher doses of granisetron in a reciprocal fashion [2]. The GTDS displayed non-inferiority to oral granisetron: complete control was achieved by 60% of patients in the GTDS group, and 65% in the oral granisetron group (treatment difference, -5%; 95% confidence interval, -13-3). Both treatments were well tolerated, the most common adverse event being constipation [3].Clinical trial: Effect of External Heat on a Transdermal Granisetron Patch in Pharmacokinetics (PK) of Healthy Subjects. Phase 1 物理化学性质: CAS号:107007-99-8 常用中文名:盐酸格拉司琼 常用英文名:Granisetron hydrochloride 分子式:C18H25ClN4O 分子量:348.870 密度:1.33g/cm3 沸点:532ºC at 760mmHg 熔点:290-292°C 闪点:275.6ºC 储存条件:Room temp |