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 Conditions Sponsor/Collaborators Start Date Phases
NCT03817970 Not yet recruiting Nephrotoxicity University of Colorado Denver|Memorial Sloan Kettering Cancer Center|Rutgers University|National Institute of General Medical Sciences (NIGMS) April 25 2019 Not Applicable
NCT03817970 Not yet recruiting Nephrotoxicity University of Colorado Denver|Memorial Sloan Kettering Cancer Center|Rutgers University|National Institute of General Medical Sciences (NIGMS) April 25 2019 Not Applicable
NCT01596426 Unknown status Chemotherapy Induced Nausea and Vomiting Kyowa Kirin Pharmaceutical Development Ltd July 2018 Phase 1
NCT01596426 Unknown status Chemotherapy Induced Nausea and Vomiting Kyowa Kirin Pharmaceutical Development Ltd July 2018 Phase 1
NCT03434340 Not yet recruiting Nausea and Vomiting Universiti Kebangsaan Malaysia Medical Centre June 2018 Not Applicable
NCT03434340 Not yet recruiting Nausea and Vomiting Universiti Kebangsaan Malaysia Medical Centre June 2018 Not Applicable

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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