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MDL 72222

3-Tropanyl-3,5-dichlorobenzoate, Bemesetron, MDL 72699

An Antagonist of 5-HT3 Receptors

Cat #: M-155
Alternative Name 3-Tropanyl-3,5-dichlorobenzoate, Bemesetron, MDL 72699
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 314.2
    Purity: >95%
    Effective concentration 1 nM - 1µM.
    Structure
    Chemical name (8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 3,5-dichlorobenzoate.
    Molecular formula C15H17Cl2NO2.
    CAS No.: 40796-97-2
    PubChem CID 1683
    Activity MDL 72222 is an antagonist of 5-HT3 receptors1.
    References-Activity
    1. Fozard, J.R. (1984) Naunyn Schmiedebergs Arch. Pharmacol. 326, 36.
    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 25 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 MDL 72222 blocks 5-HT3A receptors expressed in HEK 293T cells.
      Alomone Labs MDL 72222 blocks 5-HT3A receptors expressed in HEK 293T cells.
      5-HT3A receptor currents elicited with 10 µM 5-HT, delivered every 3 minutes. MDL 72222 (#M-155) was applied 30 seconds before stimulation at 1 µM as indicated and completely inhibited the 5-HT induced current in a dose dependent and reversible manner.
    References - Scientific background
    1. Hannon, J. et al. (2008) Behav. Brain Res. 195, 198.
    2. Fozard, J.R. (1984) Naunyn Schmiedebergs Arch. Pharmacol. 326, 36.
    3. Nawrot-Porabka, K. et al. (2013) Pharmacol. Rep. 65, 494.
    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.

    MDL 72222 (Bemesetron) is a synthetic, potent and selective antagonist of the 5-HT3 receptor. MDL 72222 has an effective concentration of 1 nM - 1μM and an ED50 of 9.27 nM. MDL 72222 produces blockade of the Bezold-Jarisch effect of 5-HT in anaesthetized rats. Inhibition of the 5-HT receptor by MDL 72222 is selective since high doses of MDL 72222 fail to alter response to electrical stimulation of efferent vagus nerves. In contrast, MDL 72222 proves only a weak and essentially non-selective antagonist of responses mediated by the 5-HT M-receptor present on the cholinergic nerves of guinea-pig ileum. MDL 72222 does not block smooth muscle contractile responses elicited by oxytocin or mediated through 5-HT D-receptors2. In addition, MDL 72222 also significantly reduces pancreatic enzyme secretion induced by luminal administration of L-trp or melatonin and reverses the effects of 5-HT on amylase secretion3.

    Target 5-HT3 receptor
    Last update: 06/11/2022

    MDL 72222 (#M-155) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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