Granisetron hydrochloride

SKU: orb1309961

Description

Granisetron HCl is a selective 5-HT3 receptor antagonist used to prevent nausea and vomiting. It is widely applied in cancer therapy research and has been utilized in both in vitro binding assays and in vivo models to study antiemetic efficacy and receptor pharmacology.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 107007-99-8
• MW: 348.87
• Purity: 99.93%
• Formula: C₁₈H₂₅ClN₄O
• SMILES: Cl.CN1C2CCCC1CC(C2)NC(=O)c1nn(C)c2ccccc12
• Target: 5-HT Receptor
• Solubility: DMSO:3.49 mg/mL (10 mM)

Bioactivity

• Target IC50:
  5-HT3:17μM
• 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.
• 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. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Serotonin Receptor, BRL 43694A, 5-HT, 5-hydroxytryptamine Receptor, 5HTReceptor, 5HT Receptor, 5-HT Receptor, inhibit, Granisetron, Granisetron HCl, Granisetron hydrochloride, Granisetron Hydrochloride, Inhibitor

Compound Identifiers

PubChem CID

65264