Tropisetron hydrochloride

A Potent and Selective Antagonist of 5-Hydroxytryptamine Receptor 3A

Cat #: T-125
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 320.76
    Purity: >98%
    Effective concentration 0.1-10 nM.
    Structure
    Chemical name [(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 1H-indole-3-carboxylate;hydrochloride.
    Molecular formula C17H21ClN2O2.
    CAS No.: 105826-92-4
    Activity Tropisetron hydrochloride is a potent and selective 5-HT3A channel blocker with Ki ~ 2 nM1.
    References-Activity
    1. Seynaeve, C. et al. (1991) Anticancer Drugs 2, 343.
    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 Tropisetron Hydrochloride blocks 5HT3A receptors expressed in HEK 293T cells.
      Alomone Labs Tropisetron Hydrochloride blocks 5HT3A receptors expressed in HEK 293T cells.
      Currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Tropisetron hydrochloride (#T-125) was applied 30 seconds before stimulation at 1, 10 and 100 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. Jack, T. et al. (2014) Neuropharmacology 90, 63.
    3. Stratz, C. et al. (2012) Int. Immunopharmacol. 13, 398.
    4. Bandschapp, O. et al. (2011) Pain 152, 1304.
    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.

    Tropisetron hydrochloride is a synthetic, potent and selective antagonist of 5-HT3A channel. In fluorescence polarization it was found to have an affinity 8.31 pKi (M) for 5-HT3A receptor2. Tropisetron binds to an extracellular domain of the receptor. Tropisetron was found to have an analgesic and anti-inflammatory activity via inhibition of lipopolysaccharide (LPS) stimulated tumor necrosis factor (TNF) and interleukin-1-β release from human monocytes. This inhibition is conducted by preventing the phosphorylation of the p38 mitogen activated kinase (MAPK)3. Interestingly, when combined with acetaminophen in an experimental pain inducing assay, Tropisetron blocked the analgesic effect of acetaminophen thus indicating that perhaps the analgesic action of acetaminophen is also mediated through 5-HT receptors4.

    Target 5-Hydroxytryptamine Receptor 3A
    Last update: 11/04/2021

    Tropisetron hydrochloride (#T-125) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

    Citations

    Citations
    Shipping and Ordering information