Molecular Weight(MW): 348.87
Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.
Purity & Quality Control
Choose Selective 5-HT Receptor Inhibitors
|Description||Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.|
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. 
|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. |
-  de Lorenzi FG, et al. Br J Pharmacol,?994, 113(2), 527-535.
-  Gr閘ot L, et al. J Pharmacol Exp Ther,?996, 279(1), 255-261.
-  Rudd JA, et al. Eur J Pharmacol,?000, 391(1-2), 145-150.
|In vitro||Water||69 mg/mL (197.78 mM)|
|DMSO||1 mg/mL (2.86 mM)|
|Ethanol||1 mg/mL (2.86 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01416259||Completed||Drug: Withdraw treatment||Healthy||Heron Therapeutics||July 2011||--|
|NCT01073696||Completed||Drug: granisetron IV|Drug: granisetron patch||Healthy||Prostrakan Pharmaceuticals||March 2010||Phase 1|
|NCT00954291||Unknown status||--||Cancer|Vomiting||Taipei Medical University WanFang Hospital||July 2009||--|
|NCT00890565||Completed||Drug: granisetron||Healthy||Prostrakan Pharmaceuticals||May 2009||Phase 1|
|NCT00873197||Completed||Drug: granisetron||Healthy||Prostrakan Pharmaceuticals||April 2009||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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