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Ricasetron

BRL 46470A

A Potent Antagonist of 5-HT3 Receptors

Cat #: R-150
Alternative Name BRL 46470A
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 313.22
    Purity: >99%
    Effective concentration 0.1 nM - 1 µM.
    Structure
    Chemical name 3,3-dimethyl-N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2H-indole-1-carboxamide.
    Molecular formula C19H27N3O.
    CAS No.: 117086-68-7
    PubChem CID 71785
    Activity Ricasetron is a 5-HT3 antagonist with Ki 0.32 nM1.
    References-Activity
    1. Blackburn, T.P. et al. (1993) Psychopharmacology (Berl). 110, 257.
    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 150 mM in DMSO. 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 Ricasetron blocks 5-HT3A channels expressed in  HEK 293T cells. 
      Alomone Labs Ricasetron blocks 5-HT3A channels expressed in  HEK 293T cells. 
      5-HT3A channel currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Ricasetron (#R-150) 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. Link, C.G. et al. (1993) Br. J. Clin. Pharmacol. 35, 395.
    2. Blackburn, T.P. et al. (1993) Psychopharmacology (Berl). 110, 257.
    3. Kato, S. (2013Biol. Pharm. Bull. 36, 1406.
    Scientific background

    Ricasetron, also named BRL 46470A, is a highly potent and selective blocker of 5-HT3 channels. The compound shows no obvious affinity for other 5-HT receptor subtypes.

    In human, ricasetron demonstrates good absorption and tolerance with wide therapeutic range1.

    in vivo studies of several animal models of anxiety, Ricasetron showed a significant reduction in passive and provoked interaction responses following acute and chronic administration. These findings suggest that Ricasetron may have potent psychopharmacological properties that can contribute to treating anxiety1,2.

    Studies show that Ricasetron is 100 times more potent than ondansetron, and 1000 times more potent than the standard anxiolytic diazepam in rat models. In these experiments the compound showed long duration of action1,2.

    The 5-HT3 receptor mediates the action of serotonin in the body. This receptor is a member of the Cys-loop ligand-gated cation channels, which are expressed throughout the central and peripheral nervous systems and mediates a variety of physiological functions such as emotion, cognition, memory, pain perception, and gastrointestinal functions including secretion and motility3.

    Target 5-HT3 receptors
    Last update: 11/04/2021

    Ricasetron (#R-150) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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