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Granisetron HCl Sale

(Synonyms: 盐酸格拉司琼; BRL 43694A) 目录号 : GC16029

A 5-HT3 receptor antagonist with antiemetic activity

Granisetron HCl Chemical Structure

Cas No.:107007-99-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥462.00
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5mg
¥378.00
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50mg
¥525.00
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100mg
¥893.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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

References:
[1]. Sanger GJ, Nelson DR. Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron). Eur J Pharmacol. 1989 Jan 10;159(2):113-24.
[2]. Maleki-Dizaji N, Eteraf-Oskouei T, Fakhrjou A, The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation. Int Immunopharmacol. 2010 Sep;10(9):1010-6.
[3]. Boccia RV, Gordan LN, Clark G, Efficacy and tolerability of transdermal granisetron for the control of chemotherapy-induced nausea and vomiting associated with moderately and highly emetogenic multi-day chemotherapy: a randomized, double-blind, phase III

Chemical Properties

Cas No. 107007-99-8 SDF
别名 盐酸格拉司琼; BRL 43694A
化学名 1-methyl-N-[(1S,5R)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide;hydrochloride
Canonical SMILES CN1C2CCCC1CC(C2)NC(=O)C3=NN(C4=CC=CC=C43)C.Cl
分子式 C18H24N4O.HCl 分子量 348.87
溶解度 ≥ 17.44mg/mL in DMSO with gentle warming, ≥ 17.44mg/mL in Water 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.8664 mL 14.332 mL 28.664 mL
5 mM 0.5733 mL 2.8664 mL 5.7328 mL
10 mM 0.2866 mL 1.4332 mL 2.8664 mL
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