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Granisetron hydrochloride

A Potent and Selective Antagonist of 5-Hydroxytryptamine Receptor 3A
Cat #: G-105
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 348.87
    Purity: >98%
    Effective concentration 0.1-10 nM.
    Chemical name 1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)indazole-3-carboxamide;hydrochloride.
    Molecular formula C18H25ClN4O.
    CAS No.: 107007-99-8.
    Activity Granisetron hydrochloride is a potent and selective 5-HT3A channel blocker with Ki~2 nM1.
    1. Sanger, G.J. and Nelson, D.R. (1989) Eur.J.Pharmacol. 159, 113.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 50 mg/ml in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Granisetron Hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells.
      Alomone Labs Granisetron Hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells.
      Currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Antagonist Granisetron hydrochloride (#G-105) was applied 30 seconds before stimulation at 1 and 10 nM, as indicated and inhibited the 5-HT induced current in a dose-dependent and reversible manner.
    References - Scientific background
    1. Hannon, J. and Hoyer, D. (2008) Behav. Brain Res. 195, 198.
    2. Aapro, M. (2004) Oncologist 9, 673.
    3. Verheij, M.H. et al. (2012) J. Med. Chem. 55, 8603.
    4. Brygger, L and Herrstedt, J. (2014) Expert Opin. Drug. Saf. 13, 1407.
    Scientific background

    Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid Tryptophan by the enzyme Tryptophan-decarboxylase. The 5-HT3 channel is a ligand gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel1.

    Granisetron Hydrochloride is a synthetic, potent and selective antagonist of 5-HT3A channel. Unlike other 5-HT antagonists Granisetron has little affinity for other receptors while having a pKi of 8.42 for 5-HT3A receptor2. Granisetron binds to an extracellular domain of the receptor. Currently, Granisetron is widely used in clinical practices to prevent vomiting and diarrhea post chemotherapy, radiotherapy and surgery. It was also found to alleviate the effects of irritable bowel syndrome3. Granisetron and other antiemetics induce cardiovascular side effects including orthostatic hypotension and the prolongation of the QT interval that might cause Torsades de Pointes (TdP) ventricular tachycardia4.

    Target 5-Hydroxytryptamine Receptor 3A
    Last update: 22/09/2020

    Granisetron hydrochloride (#G-105) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background


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