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A Potent Antagonist of 5-HT3 Receptors

Cat #: L-180
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 298.38
    Purity: >97%
    Effective concentration 1 nM - 1 µM.
    Chemical name 1-methyl-N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]indazole-3-carboxamide.
    Molecular formula C17H22N4O.
    PubChem CID 5311254
    Activity LY278584 is a specifiic 5-HT3 antagonist. 0.1 μM completely blocks 1 μM 5HT evoked current in Xenopus oocytes1.
    1. Abi-Dargham, A. et al. (1993) J. Neurochem. 60, 730.
    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 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 LY278584 blocks 5-HT3A receptors expressed in  HEK 293T cells. 
      Alomone Labs LY278584 blocks 5-HT3A receptors expressed in  HEK 293T cells. 
      5-HT3A receptor currents were elicited by 10 µM 5-HT, delivered every 3 minutes. LY278584 (#L-180) applied 30 seconds before stimulation at 100 nM, inhibited the 5-HT induced current in a dose dependent and reversible manner.
    References - Scientific background
    1. Miller, K. et al. (1992) Synapse 11, 58.
    2. Abi-Dargham, A. et al. (1993) J. Neurochem. 60, 730.
    3. Kuo, C.C. et al. (2013) Evid. Based Complement. Alternat. Med. 2013, 291972.
    4. Kato, S. (2013Biol. Pharm. Bull. 36, 1406.
    Scientific background

    LY278584 is a potent and selective antagonist of 5-HT3 receptors. Its structure is very similar to granisetron, also a 5-HT3 receptor antagonist. LY278584 is a useful ligand for studying the localization of 5-HT3 receptors in rat brain1,2.

    Numerous studies have shown that 5-HT3 antagonism is able to modulate mesolimbic dopaminergic activity in rodents. There is evidence that blockade of 5-HT3 receptors may be involved in nociception. Another study conducted on 5-HT3 antagonism showed that LY278584 significantly inhibits high frequency electroacupuncture antinociception in early stages3.

    The 5-HT3 receptors mediate the action of serotonin in the body. These receptors are members of the Cys-loop ligand-gated cation channels, which are expressed throughout the central and peripheral nervous systems and mediate a variety of physiological functions such as emotion, cognition, memory, pain perception, and gastrointestinal functions including secretion and motility4.

    Target 5-HT3 receptors
    Last update: 12/08/2021

    LY278584 (#L-180) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information