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1-Phenylbiguanide hydrochloride

PBG

A Potent and Selective Agonist of 5-HT3 Receptors

Cat #: P-190
Alternative Name PBG
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 213.67
    Purity: >99%
    Effective concentration 0.1-100 µM.
    Structure
    Chemical name 1-(diaminomethylidene)-2-phenylguanidine;hydrochloride.
    Molecular formula C8H12ClN5.
    CAS No.: 55-57-2
    Activity 1-Phenylbiguanide hydrochloride is an activator of 5-HT3 channels1.
    References-Activity
    1. Ireland, S.J. and Tyers, M.B. (1987) Br. J. Pharmacol. 90, 229.
    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 1-Phenylbiguanide hydrochloride activates 5-HT3A receptors expressed in HEK 293T cells.
      Alomone Labs 1-Phenylbiguanide hydrochloride activates 5-HT3A receptors expressed in HEK 293T cells.
      Currents were elicited by 10 or 100 µM 1-Phenylbiguanide hydrochloride (#P-190), as indicated. The currents that were elicited by this agonist were comparable in amplitude to the cells response to 10 µM 5-HT (not shown here).
    References - Scientific background
    1. Ireland, S.J. and Tyers, M.B. (1987) Br. J. Pharmacol. 90, 229.
    2. Zhang, Z. et al. (2013) Neurosci. Lett. 552, 10.
    3. Fu, L.W. and Longhurst, J.C. (1998) Am. J. Physiol. 275, 6.
    Scientific background

    Phenylbiguanide (PBG) acts as an agonist of 5-HT3 receptors, with an EC50 value two fold greater than that of 5-HT and was found to imitate the effects of 5-HT on mammalian peripheral neurons. PBG causes dopamine release and has been used in many studies as a selective agonist to arouse reflex bradycardia and hypotension through activation of cardiac and pulmonary vagal afferents1,3.

    For over 40 years, PBG has been used as a selective agonist to identify cardiac and pulmonary vagal C fibers and the associated reflex bradycardia and depressor responses. It is capable to stimulate cardiac chemosensitive receptors with vagal afferent pathways and the sensory nerves in different regions of the body3.

    In one study conducted in rats, it was found that phenylbiguanide depolarizes the rat vagus nerve and mimics the effects of 5-HT on the vagus nerve. In addition, it was shown that phenylbiguanide causes reflex falls in heart rate and blood pressure in the cat and induces pain following application to the bases of blisters in human subjects1.

    It has been documented that right atrial bolus injection of phenylbiguanide can stimulate bronchopulmonary C-fibers that play an important role in modulating the respiratory rhythm to produce apnea2.

    Target Serotonin-gated channels
    Lyophilized Powder
    Last update: 02/01/2022

    1-Phenylbiguanide hydrochloride (#P-190) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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