Home Neuronal Signaling 5-HT Receptor antagonist Granisetron HCl

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Granisetron HCl 5-HT Receptor antagonist

Cat.No.S1345

Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.
Granisetron HCl 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 348.87

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Chemical Information, Storage & Stability

Molecular Weight 348.87 Formula

C18H24N4O.HCl

 Storage (From the date of receipt)
CAS No. 107007-99-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN1C2CCCC1CC(C2)NC(=O)C3=NN(C4=CC=CC=C43)C.Cl

Solubility

In vitro
Batch:

Water : 69 mg/mL

Ethanol : 21 mg/mL

DMSO : 17 mg/mL (48.72 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
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]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/20154102/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10882387/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04918862 Completed
1mg Vs 3 mg of Granisetron
Cairo University|Mohamed Yousry Mohamed|Tamer Fayez Safan|Tamer Mohamed Khair|Mohamed Ahmed A. M.D.|Islam Mohamed Sayed
 January 8 2021 Phase 3

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