| 常用名 | 格拉司琼 | CAS号 | 109889-09-0 |
|---|---|---|---|
| 价格 | ¥需询单/100kg ¥需询单/10kg ¥需询单/1kg ¥需询单/100g | 纯度 | 99.0% |
| 备货期 | 需询单 | 库存 | 现货 |
| 产品网页 | http://www.mic-pharma.com | ||
| 产品详情(用途,包装等)
用途: Granisetron 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 作用: 格拉司琼是一种止吐药,由葛兰素史克公司的前身英国史克必成医药公司在90年代初推出,用于防治化疗和放疗引起的恶心与呕吐,止吐效力是昂丹司琼的6~11倍 。作用机制是通过对上端小肠腹部向心神经纤维和孤束核或呕吐化学感受区的5-HT3受体的阻断作用,从而达到抑制抗肿瘤药物和放疗引起的恶心和呕吐的效果。 物理化学性质: CAS号:109889-09-0 常用中文名:格拉司琼 常用英文名:Granisetron 分子式:C18H24N4O 分子量:312.41 密度:1.3±0.1 g/cm3 沸点:532.0±40.0 °C at 760 mmHg 熔点:N/A 闪点:275.6±27.3 °C 储存条件:-20℃ |