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m-Chlorophenylbiguanide hydrochloride


A Potent and Selective Agonist of 5-HT3 Receptors

Cat #: M-160
Alternative Name mCPG
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 248.11
    Purity: >99%
    Effective concentration 0.1-20 µM.
    Chemical name 2-(3-chlorophenyl)-1-(diaminomethylidene)guanidine;hydrochloride.
    Molecular formula C8H11Cl2N5.
    CAS No.: 05/05/2113
    Activity m-Chlorophenylbiguanide is an activator/agonist of 5-HT3 channels1.
    1. Kilpatrick, G.J. et al. (1990) Eur. J. Pharmacol. 182, 193.
    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 100 mM 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 m-Chlorophenylbiguanide hydrochloride activates  5-HT3A receptors expressed in HEK 293T cells.
      Alomone Labs m-Chlorophenylbiguanide hydrochloride activates  5-HT3A receptors expressed in HEK 293T cells.
      Currents were elicited by 1 or 10 µM m-Chlorophenylbiguanide hydrochloride (#M-160), as indicated. Currents elicited by m-Chlorophenylbiguanide hydrochloride were comparable in amplitude to the cells response to 10 µM 5-HT (not shown).
    References - Scientific background
    1. Hannon, J. and Hoyer, D. (2008) Behav. Brain Res. 195, 198.
    2. Sepulveda, M.I. et al. (1991) Br. J. Pharmacol. 104, 536.
    3. Schlicker, E. et al. (1994) Naunyn Schmiedebergs Arch. Pharmacol. 349, 20.
    4. Rothlin, C.V. et al. (2003) Mol. Pharmacol. 63, 1067.
    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.

    m-Chlorophenylbiguanide hydrochloride (mCPG) is a prototypical, potent and selective 5-HT3 receptor agonist. In a study conducted in N1E-115 neuroblastoma cells mCPG exhibited inward rectification and reversed currents similar to those induced by 5-HT binding to the 5-HT3 receptor. The rate of receptor desensitization is similar to that of 5-HT binding but the peak current amplitude provoked by the agonist was found to be only 20% at saturating concentration2. Interestingly, mCPG seems to facilitate noradrenaline release in mouse brain cortex cell. When mouse brain slices were incubated with H-noradrenaline, electrical field stimulation was facilitated by mCPG and this effect was blocked by the α2 adrenergic receptor antagonist, Rauwolscine3. mCPG binds and activates recombinant α9/α10 acetylcholine receptors in Xenopus oocytes (although 5-HT does not) thus producing inwards currents that are 3.1±0.7% of the maximum effect obtained by ACh binding4.

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

    m-Chlorophenylbiguanide hydrochloride (#M-160) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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