Granisetron
格拉司琼
Catalog No.
A3443
血清素5-HT3受体拮抗剂
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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
Storage | Store at -20°C |
M.Wt | 312.41 |
Cas No. | 109889-09-0 |
Formula | C18H24N4O |
Solubility | Soluble in DMSO |
Chemical Name | 1-methyl-N-[(1S,5R)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | CN1C2CCCC1CC(C2)NC(=O)C3=NN(C4=CC=CC=C43)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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