Molecular Weight(MW): 414.56
AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.
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|Description||AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.|
Ambroxol inhibits Na+ channels in sensory neurons. The potency for tonic block of TTX-r channels is relatively high. Ambroxol affects the Na+ current kinetics of TTX-r and TTX-s channels differently. In CNaIIA cells, the compound behaves like a charged local anesthetic: the block is dependent on stimulus number and increases with higher frequencies in a train of depolarizing stimuli. In CNaIIA cells, ambroxol inhibits inactivated channels 5.5-fold more potently than resting channels. The corresponding factor for TTX-r channels is only 3.3. Ambroxol inhibits the release of histamine, leukotrienes and cytokines from human leukocytes and mast cells. 
|In vivo||Ambroxol inhibited histamine release by more than 50% from human adenoidal mast cells (1000 microM ambroxol) and skin mast cells (100 microM ambroxol) stimulated by Con A and compound 48/80, respectively. Ambroxol (100 microM) strikingly inhibited anti-IgE induced release of both histamine, LTC4, IL-4 and IL-13 from basophils and reduced both histamine and LTB4 release induced by C5a or Zymosan in monocytes. The drug also reduced LTB4 and superoxide anion production in granulocytes stimulated by zymosan or fMLP.|
|In vitro||DMSO||4 mg/mL warmed (9.64 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02941822||Not yet recruiting||Parkinson Disease||University College, London|Cure Parkinsons Trust|PRO.MED.CS Praha a.s - Czech Republic||December 2016||Phase 2|
|NCT02914366||Recruiting||Parkinsons Disease Dementia||Lawson Health Research Institute|Weston Foundation|University of Western Ontario, Canada|London Health Sciences Centre||November 2015||Phase 2|
|NCT01463215||Suspended||Type I Gaucher Disease||Exsar Corporation||December 2012||Phase 1|Phase 2|
|NCT01573663||Completed||Healthy||Hanmi Pharmaceutical Company Limited||February 2012||Phase 1|
|NCT02572609||Completed||Healthy||Boehringer Ingelheim||November 2011||Phase 1|
|NCT01713179||Completed||In the Present Study, we Investigated the Effects of Oral Ambroxol on Tear Film and Ocular Surface.||Hallym University Kangnam Sacred Heart Hospital||August 2011||Phase 1|Phase 2|
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