| CAS NO: | 107007-99-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| Molecular Weight (MW) | 348.87 |
|---|---|
| Formula | C18H24N4O.HCl |
| CAS No. | 107007-99-8 (HCl salt); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 70 mg/mL (200.6 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| SMILES Code | O=C(C1=NN(C)C2=C1C=CC=C2)N[C@H]3C[C@@](N4C)([H])CCC[C@@]4([H])C3.[H]Cl |
| Synonyms | BRL43694; BRL 43694; BRL43694A; BRL 43694A; BRL-43694; BRL-43694A; Granisetron Hydrochloride; Granisetron HCl; GRAN; US trade name: Kytril. |
| In Vitro | In vitro activity: Granisetron blocks the delayed rectifier current (IK) of feline isolated ventricular myocytes with a KD of 4.3 mM. Granisetron shows an intrinsic voltage-dependence as the block increases with depolarization. Granisetron blocks from the intracellular side at a binding site located 10% across the transmembrane electrical field. Granisetron (3 mM) prolongs the action potential duration (APD) by about 30% at 0.5 Hz in feline isolated ventricular myocytes. Granisetron but not Ondansetron, could prevent the activation of putative 5-H; autoreceptors, thus leading to a decrease in serotonin release by the enterochromaffin cells. Cell Assay: 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. |
|---|---|
| In Vivo | Granisetron provides a substantial benefit against cisplatin-induced emesis in the piglet, some animals being completely protected during both the acute and the delayed phases. Granisetron (1 mg/kg, i.m.) administered three times per day reduces significantly the retching+vomiting response induced by cisplatin on days 1 and 2 by 100.0% and 75.0%, respectively, in cats. Granisetron or dexamethasone significantly improves macroscopic and histologic scores, curtails myeloperoxidase activity and diminishes colonic levels of inflammatory cytokines and malondialdehyde in rats. Granisetron, not only prevents cholera toxin-induced jejunal net fluid secretion but also, and in proportion, inhibits 5-HT release into the intestinal lumen of mice. |
| Animal model | Piglet |
| Formulation & Dosage | 1 mg/kg, i.m. |
| References | Br J Pharmacol. 1994 Oct;113(2):527-35; J Pharmacol Exp Ther. 1996 Oct;279(1):255-61. |
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