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Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $32 | In Stock | |
25 mg | $51 | In Stock | |
50 mg | $74 | In Stock | |
100 mg | $129 | In Stock | |
200 mg | $188 | In Stock | |
500 mg | $319 | In Stock | |
1 mL x 10 mM (in DMSO) | $81 | In Stock |
Description | Granisetron hydrochloride (Granisetron HCl) is a serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients. |
In vitro | 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. [1] 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. [2] |
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. [2] 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. [3] Granisetron or dexamethasone significantly improves macroscopic and histologic scores, curtails myeloperoxidase activity and diminishes colonic levels of inflammatory cytokines and malondialdehyde in rats. [4] 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. [5] |
Alias | BRL 43694A, Granisetron HCl |
Molecular Weight | 348.87 |
Formula | C18H25ClN4O |
Cas No. | 107007-99-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 3.49 mg/mL (10 mM), Sonication is recommended. ![]() | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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