生物活性

• 靶点	Sodium Channel (neuronal) IC50:22.5μM~35.2μM

• 描述Ambroxol hydrochloride, an active metabolite of the prodrug Bromhexine, has potent expectorant effects^[3]. Ambroxol hydrochloride is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol hydrochloride induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research. Ambroxol hydrochloride (1, 3, 4, 5 mM for 12 consecutive days in drinking water) results in increased brain glucocerebrosidase activity in wild-type mice, transgenic mice expressing the heterozygous L444P mutation in the murine glucocerebrosidase 1 gene, and transgenic mice overexpressing human α-synuclein^[4]. In addition, ambroxol hydrochloride improved motor recovery and muscle re-innervation after transient sciatic nerve injury in non-transgenic mice and promoted axonal elongation in an in vitro model of motor unit^[5]. Ambroxol hydrochloride administered intravenously more than 48 hours prior to chemotherapy optimally increased the concentrations of paclitaxel and carboplatin in lung tissue without significantly increasing hematologic toxicity^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00144274	Pharyngitis	Phase 3	Completed	-	South Africa ... more >> Boehringer Ingelheim Investigational Site Boksburg, South Africa, 1461 Boehringer Ingelheim Investigational Site Cape Town, South Africa, 7646 Boehringer Ingelheim Investigational Site Cape Town, South Africa, 7700 Boehringer Ingelheim Investigational Site Cape Town, South Africa, 7945 Boehringer Ingelheim Investigational Site Durban, South Africa, 4091 Boehringer Ingelheim Investigational Site Johannesburg, South Africa, 2033 Boehringer Ingelheim Investigational Site Johannesburg, South Africa, 2192 Boehringer Ingelheim Investigational Site Krugersdorp, South Africa, 1739 Boehringer Ingelheim Investigational Site Midrand, South Africa, 1685 Boehringer Ingelheim Investigational Site Pretoria, South Africa, 0038 Boehringer Ingelheim Investigational Site Pretoria, South Africa, 0157 Boehringer Ingelheim Investigational Site Sandton, South Africa, 2021 Collapse <<
  NCT00148499	Pharyngitis	Phase 3	Completed	-	Romania ... more >> Medicover Bucharest, Romania, 010224 Medicover Bucharest, Romania, 010626 Medicover Bucharest, Romania, 021106 Victor Babes Clincial Hospital Bucharest, Romania, 030303 Ukraine Regional Student Hospital Kharkov, Ukraine, 61002 Regional Clinical Hospital Kharkov, Ukraine, 61022 City Clinical Otolaryngological Hospital Kharkov, Ukraine, 61024 City Clinical Hospital No. 17 Kharkov, Ukraine, 61037 City Clinical Hospital No. 11 Kharkov, Ukraine, 61050 City Clinical Hospital No. 26 Kharkov, Ukraine, 61072 Academy of Medical Science named after O.S. Kolomyichenko Kiev, Ukraine, 03057 City Clinical Hospital No. 9 Kiev, Ukraine, 04112 City Clinical Hospital No. 11 Odessa, Ukraine, 65006 Regional Clinical Hospital Zaporozhye, Ukraine, 69600 Collapse <<
  NCT03583658	Pharyngitis	Phase 3	Completed	-	South Africa ... more >> Investigational Site Number 7100005 Johannesburg, South Africa Collapse <<

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• 参考文献

• [1] Weiser T, Wilson N. Inhibition of tetrodotoxin (TTX)-resistant and TTX-sensitive neuronal Na(+) channels by the secretolytic ambroxol. Mol Pharmacol. 2002 Sep;62(3):433-8.

  [2] Gibbs BF, Schmutzler W, et al. Ambroxol inhibits the release of histamine, leukotrienes and cytokines from human leukocytes and mast cells. Inflamm Res. 1999 Feb;48(2):86-93.

  [3] Deretic V, Timmins GS. Enhancement of lung levels of antibiotics by ambroxol and bromhexine. Expert Opin Drug Metab Toxicol. 2019 Mar;15(3):213-218

  [4] Migdalska-Richards A, Daly L, Bezard E, Schapira AH. Ambroxol effects in glucocerebrosidase and α-synuclein transgenic mice. Ann Neurol. 2016 Nov;80(5):766-775

  [5] Bouscary A, Quessada C, Mosbach A, Callizot N, Spedding M, Loeffler JP, Henriques A. Ambroxol Hydrochloride Improves Motor Functions and Extends Survival in a Mouse Model of Familial Amyotrophic Lateral Sclerosis. Front Pharmacol. 2019 Aug 7;10:883

  [6] Li J, Yi W, Jiang P, Sun R, Li T. Effects of ambroxol hydrochloride on concentrations of paclitaxel and carboplatin in lung cancer patients at different administration times. Cell Mol Biol (Noisy-le-grand). 2016 Nov 30;62(13):85-89

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