Granisetron,109889-09-0

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产品名称：Granisetron

产品别名：格拉司琼

英文别名：BRL 43694

靶点：5-HT3 receptor

CAS：109889-09-0

纯度：≥98%

外观：白色或类白色固体

保存方法：Store at -20° C

描述：

Granisetron is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.

溶解性：DMSO ：11 mg/mL (35.21 mM)

体外研究：

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.

体内研究：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. 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.

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