Granisetron HCl

Catalog No.S1345

Granisetron HCl Chemical Structure

Molecular Weight(MW): 348.87

Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.

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Biological Activity

Description Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.
Targets
5-HT3 [1]
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]

Protocol

Solubility (25°C)

In vitro Water 69 mg/mL (197.78 mM)
DMSO 1 mg/mL (2.86 mM)
Ethanol 1 mg/mL (2.86 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 348.87
Formula

C18H24N4O.HCl

CAS No. 107007-99-8
Storage powder
in solvent
Synonyms N/A

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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

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID