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仪器信息网试剂标物生化试剂常用生化试剂盐酸格拉司琼

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盐酸格拉司琼

价格：￥ 1

品牌：AMRESCO

供货周期：现货

货号：hz120176

规格：g/mg

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详细信息

详细信息

盐酸格拉司琼

98%

Product Name: Granisetron hydrochloride

CAS号:	107007-99-8
分子式:	C₁₈H₂₄N₄O·HCl
分子量:	348.87
MDL号:	MFCD01747034

盐酸格拉司琼

熔点:

284.0-290.0 °C

生化和生理学机理:

Description:
IC50 Value: 17uM (GR reduced 5-HT-evoked contractions) [1]
Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
in 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

盐酸格拉司琼

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