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格拉司琼

规格或纯度: ≥98.0%
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货号 (SKU) 包装规格 是否现货 价格 数量
G127257-5mg
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G127257-25mg
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G127257-100mg
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G127257-250mg
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5-HT3A Antagonist

基本描述

英文别名 granisetron|109889-09-0|Sancuso|Sustol|Kevatril|Granisetronum|APF530|Kytril|BRL-43694|1-methyl-N-[(1S,5R)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide|CHEBI:5537|BRL 43694|APF 530|WZG3J2MCOL|1-methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.
规格或纯度 ≥98.0%
英文名称 Granisetron
生化机理

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
 

储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.


Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.


名称和标识符

IUPAC Name 1-methyl-N-[(1R,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide
INCHI InChI=1S/C18H24N4O/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23)/t12?,13-,14+
InChi Key MFWNKCLOYSRHCJ-AGUYFDCRSA-N
Canonical SMILES CN1C2CCCC1CC(C2)NC(=O)C3=NN(C4=CC=CC=C43)C
Isomeric SMILES CN1[C@@H]2CCC[C@H]1CC(C2)NC(=O)C3=NN(C4=CC=CC=C43)C
PubChem CID 5284566
分子量 312.41

化学和物理性质

溶解性 DMSO:11 mg/mL

安全和危险性(GHS)

象形图
ghs07

Harmful

信号词 Warning
危险声明 H319: Causes serious eye irritation
H412: Harmful to aquatic life with long lasting effects
H302: Harmful if swallowed
预防措施声明 P305+P351+P338,P273,P280,P501,P264,P270,P330,P264+P265,P301+P317,P337+P317

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