109889-09-0
109889-09-0 structure
- Name: Granisetron
- Chemical Name: granisetron
- CAS Number: 109889-09-0
- Molecular Formula: C18H24N4O
- Molecular Weight: 312.41
- Catalog: API Digestive system medication Antiemetic emetic
- Create Date: 2018-10-02 19:27:45
- Modify Date: 2025-08-20 17:24:01
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Granisetron 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
| Name | granisetron |
|---|---|
| Synonyms |
1-(H)Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide
Kevatril BIDD:GT0272 Sancuso [3H]-Granisetron UNII-WZG3J2MCOL 1-methyl-N-[(1S,5R)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide HMS2089P14 granisetron hydrochloride 1H-Indazole-3-carboxamide, 1-(methyl-d)-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]- |
| Description | Granisetron 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 |
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| Related Catalog | |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 532.0±40.0 °C at 760 mmHg |
| Molecular Formula | C18H24N4O |
| Molecular Weight | 312.41 |
| Flash Point | 275.6±27.3 °C |
| PSA | 50.16000 |
| LogP | 1.47 |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.690 |
| Storage condition | -20℃ |
| HS Code | 2934999090 |
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109889-09-0 |
| Literature: Journal of Medicinal Chemistry, , vol. 33, # 7 p. 1924 - 1929 |
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109889-09-0 |
| Literature: Journal of Medicinal Chemistry, , vol. 33, # 7 p. 1924 - 1929 |
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109889-09-0 |
| Literature: US2008/242696 A1, ; Page/Page column 3 ; |
| Precursor 4 | |
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| DownStream 1 | |
| HS Code | 2934999090 |
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| Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |