Ambroxol hydrochloride

Mucosolvan®, Mucobrox®, Lasolvan®, Mucoangin®, Surbronc®, Lysopain®
A Local Anesthetic, NaV Channel Blocker
Cat #: A-145
Alternative Name Mucosolvan®, Mucobrox®, Lasolvan®, Mucoangin®, Surbronc®, Lysopain®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 414.6
    Purity: >99%
    Effective concentration 10-200 μM.
    Chemical name trans-4-[[(2-Amino-3,5-dibromophenyl)methyl]amino]cyclohexanol hydrochloride.
    Molecular formula C13H18Br2N2O•HCl.
    CAS No.: 23828-92-4.
    Activity Ambroxol hydrochloride is a Na+ channel blocker1 and secretolytic compound for the treatment of respiratory diseases2. Ambroxol inhibits tetrodotoxin (TTX)-resistant channels more potently than TTX-sensitive subtypes (IC50 values for tonic block are 35 and 100 μM, respectively)1.
      • Weiser, T. et al. (2002) Mol. Pharmacol. 62, 433.

      • Malerba, M. et al. (2008) Expert. Opin. Drug Metab. Toxicol. 4, 1119.

    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 Water. 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.
      • Alomone Labs Ambroxol hydrochloride inhibits NaV1.7 channels expressed in HEK293 cells.
        A: Time course of current reversible inhibition by 100 μM Ambroxol hydrochloride (#A-145). Currents were elicited by a voltage ramp from a holding potential of -100 mV to 60 mV (30 ms) delivered every 10 seconds. B: Example traces of current response to voltage ramp stimulation before and during 100 μM Ambroxol hydrochloride application.
      • Amir, E. et al. (2006) J. Pain 7, S1.

      • Malerba, M. et al. (2008) Expert. Opin. Drug Metab. Toxicol. 4, 1119.

      • Laoag-Fernandez, J. B. et al. (2000) J. Obstet. Gynaecol. Res. 26, 307.

      • Matthys, H. et al. (2000) Arzneimittelforschung 50, 700.

      • Weiser, T. et al. (2002) Mol. Pharmacol. 62, 433.

      • De Mey, C. et al. (2008) Arzneimittelforschung 58, 557.

      • Fischer, J. et al. (2002) Arzneimittelforschung 52, 256.

      • Gaida, W. et al. (2005) Neuropharmacology. 49, 1220.

      • Gibbs, F. et al. (1999) Inflamm. Res. 48, 86.

      • Felix, K. et al. (1996) Life. Sci. 59, 1141.

      • Nowak, D. et al. (1994) Free Radic Biol. Med. 16, 517.

      • Malerba, M. et al. (2008) Expert. Opin. Drug Metab. Toxicol. 4, 1119.

      • Voltage-gated Na+ channels (VGSC, Nav) are critically important for electrogenesis and nerve impulse conduction. Certain Na+ channel isoforms are predominantly expressed in peripheral sensory neurons associated with pain sensation, and the expression and functional properties of NaV in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation1.

        Ambroxol is a secretolytic compound for the treatment of respiratory diseases2. It is an effective expectorant, has been shown to normalize the structure of surfactant, to prevent the infant respiratory distress syndrome, and to be effective for the treatment of bronchitis3-4.

        In addition to its effects on the respiratory system, Ambroxol is an effective blocker of neuronal Na+ channels5. In rat dorsal root ganglia, TTX-resistant Na+ currents were suppressed in a concentration-dependent manner with IC50 values of 35.2 and 22.5 μM for tonic and phasic block, respectively. TTX-sensitive currents were inhibited with lower potency; approximately 50% inhibition with 100 μM5.

        Ambroxol has local anesthetic properties, which make it an efficacious treatment for sore throat6 and to reduce symptoms of chronic, neuropathic, and inflammatory pain in vivo7,8.
        Ambroxol inhibits the release of histamine, leukotrienes and cytokines from human leukocytes and mast cells9. It has also well documented antioxidant properties10,11.

    Target NaV Na+ channels
    Last update: 11/03/2019

    Ambroxol hydrochloride (#A-145) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use