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    Granisetron HCl (BRL 43694A)
    Granisetron HCl (BRL 43694A)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0976
    CAS #: 107007-99-8 Purity ≥98%

    Description: Granisetron HCl (BRL-43694; BRL43694; BRL-43694A; trade name: Kytril), an approved antiemetic drug, is a potent serotonin 5-HT3 receptor antagonist with antiemetic activity. It is 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. 

    References: Br J Pharmacol. 1994 Oct;113(2):527-35; J Pharmacol Exp Ther. 1996 Oct;279(1):255-61.

    Related CAS#: 109889-09-0 (free base) 

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    Molecular Weight (MW)348.87 
    FormulaC18H24N4O.HCl 
    CAS No.107007-99-8 (HCl salt);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 70 mg/mL (200.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL 
    SMILES CodeO=C(C1=NN(C)C2=C1C=CC=C2)N[[email protected]]3C[[email protected]@](N4C)([H])CCC[[email protected]@]4([H])C3.[H]Cl
    SynonymsBRL43694; BRL 43694; BRL43694A; BRL 43694A; BRL-43694; BRL-43694A; Granisetron Hydrochloride; Granisetron HCl; GRAN; US trade name: Kytril.


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    In Vitro

    In vitro activity: 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.


    Cell Assay: In rat forestomach GR reduced 5-HT-evoked contractions at IC50 17 /- 6 uM. In isolated rabbit heart, GR 0.003-0.03 nM dose-dependently reduced s-HT tachycardia; at high levels GR reduced submaximal and maximal responses to 5-HT.

    In VivoGranisetron 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. 
    Animal modelPiglet
    Formulation & Dosage1 mg/kg, i.m.
    ReferencesBr J Pharmacol. 1994 Oct;113(2):527-35; J Pharmacol Exp Ther. 1996 Oct;279(1):255-61. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     
    Granisetron HCl
    Br J Pharmacol. 1994 Oct; 113(2): 527–535.
     
    Granisetron HCl
    Br J Pharmacol. 1994 Oct; 113(2): 527–535.
     
    Granisetron HCl
    Br J Pharmacol. 1994 Oct; 113(2): 527–535.


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