For research use only.
CAS No. 107007-99-8
Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.
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|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|
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