CAS Number107007-99-8
SynonymsGranisetron hydrochloride; 1-méthyl-N-[(3-endo)-9-méthyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide chlorhydrate; MFCD01747034; Granisetron HCl; 1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide hydrochloride; 1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide; 1-methyl-N-[(1S,5R)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide,hydrochloride; 1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazol-3-carboxamidhydrochlorid; Granisetron (Hydrochloride)
Molecular FormulaC18H25ClN4O
Molecular Weight348.87
Purity98%
Density1.33g/cm3
Boiling Point532ºC at 760mmHg
Melting Point290-292°C
AppearanceWhite to off-white crystalline solid
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 107007-99-8 |
| Catalog No. | 2A-9007907 |
| Chinese Name | 盐酸格拉司琼 |
| Synonyms | Granisetron hydrochloride; 1-méthyl-N-[(3-endo)-9-méthyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide chlorhydrate; MFCD01747034; Granisetron HCl; 1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide hydrochloride; 1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide; 1-methyl-N-[(1S,5R)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide,hydrochloride; 1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazol-3-carboxamidhydrochlorid; Granisetron (Hydrochloride) |
| Molecular Formula | C18H25ClN4O |
| Molecular Weight | 348.87 |
| Purity | 98 |
| Density | 1.33g/cm3 |
| Boiling Point | 532ºC at 760mmHg |
| Melting Point | 290-292°C |
| Appearance | White to off-white crystalline solid |
| Storage Condition | Room temp |
| Application | Granisetron (BRL 43694A) hydrochloride is a 5-HT3 receptor antagonist and can be used as an antiemetic after chemotherapy. |
| HTC | 2933990090 |
| PubChem ID | 329823512 |
| MDL Number | MFCD01747034 |
| SMILES | Cl.CN1[C@H]2CCC[C@@H]1C[C@@H](C2)NC(=O)c3nn(C)c4ccccc34 |
| InChI | 1S/C18H24N4O.ClH/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);1H/t12-,13+,14-; |
| InChI Key | QYZRTBKYBJRGJB-WQTKJZBYSA-N |
| NACRES Code | NA.24 |
| UNSPSC | 41116107 |
| MSDS | msds/7907_1_107007_99_8.pdf |
| Bioactivity | 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 Related Catalog Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Neurological Disease 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 & Physical Properties Density 1.33g/cm3 Boiling Point 532ºC at 760mmHg Melting Point 290-292°C Molecular Formula C18H25ClN4O Molecular Weight 348.870 Flash Point 275.6ºC Exact Mass 348.171692 PSA 50.16000 LogP 3.44920 Vapour Pressure 0mmHg at 25°C Index of Refraction 1.69 InChIKey QYZRTBKYBJRGJB-UHFFFAOYSA-N SMILES CN1C2CCCC1CC(NC(=O)c1nn(C)c3ccccc13)C2.Cl Storage condition Room temp |
| Use of | Properties Articles28 Name Granisetron hydrochloride Synonym More Synonyms Granisetron hydrochloride Biological Activity Related Catalog Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Neurological Disease 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 & Physical Properties Exact Mass 348.171692 PSA 50.16000 LogP 3.44920 Index of Refraction 1.69 InChIKey QYZRTBKYBJRGJB-UHFFFAOYSA-N Storage condition Room temp |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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