Carbocisteine- 13 C 3 -1 (Carbocysteine- 13 C 3 -1) is 13 C labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research [1] [2] [3] [4] [5] [6] [7] [8] [9] [10] [11] [12] [13].
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Yageta Y, et al. Carbocisteine reduces virus-induced pulmonary inflammation in mice exposed to cigarette smoke. Am J Respir Cell Mol Biol. 2014 May;50(5):963-73.
[3]. Inoue M, et al. Carbocisteine promotes phagocytosis of apoptotic cells by alveolar macrophages. Eur J Pharmacol. 2012 Feb 29;677(1-3):173-9.
[4]. Wang W, et al. Carbocisteine attenuates hydrogen peroxide-induced inflammatory injury in A549 cells via NF-κB and ERK1/2 MAPK pathways. Int Immunopharmacol. 2015 Feb;24(2):306-313.
[5]. Yamaya M, et al. Inhibitory effects of carbocisteine on type A seasonal influenza virus infection in human airway epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2010 Aug;299(2):L160-8.
[6]. Hanaoka M, et al. Carbocisteine protects against emphysema induced by cigarette smoke extract in rats. Chest. 2011 May;139(5):1101-1108.
[7]. Abdelhamid AM, et al. Carbocisteine as a Modulator of Nrf2/HO-1 and NFκB Interplay in Rats: New Inspiration for the Revival of an Old Drug for Treating Ulcerative Colitis. Front Pharmacol. 2022 Jun 8;13:887233.
[8]. Song Y, et al. Carbocisteine inhibits the expression of Muc5b in COPD mouse model. Drug Des Devel Ther. 2019 Sep 16;13:3259-3268.
[9]. Song Y, et al. A mucoactive drug carbocisteine ameliorates steroid resistance in rat COPD model. Pulm Pharmacol Ther. 2016 Aug;39:38-47.
[10]. Ishibashi Y, et al. Effects of carbocisteine on altered activities of glycosidase and glycosyltransferase and expression of Muc5ac in SO2-exposed rats. Eur J Pharmacol. 2004 Mar 8;487(1-3):7-15.
[11]. Song Y, et al. Carbocysteine restores steroid sensitivity by targeting histone deacetylase 2 in a thiol/GSH-dependent manner. Pharmacol Res. 2015 Jan;91:88-98.
[12]. Yoshida M, et al. Carbocisteine inhibits oxidant-induced apoptosis in cultured human airway epithelial cells. Respirology. 2009 Sep;14(7):1027-34.
[13]. Wang W, et al. Carbocisteine attenuates TNF-α-induced inflammation in human alveolar epithelial cells in vitro through suppressing NF-κB and ERK1/2 MAPK signaling pathways. Acta Pharmacol Sin. 2016 May;37(5):629-36.
[14]. Paola Rogliani, et al. Efficacy and safety profile of mucolytic/antioxidant agents in chronic obstructive pulmonary disease: a comparative analysis across erdosteine, carbocysteine, and N-acetylcysteine. Respir Res. 2019 May 27;20(1):104.
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Yageta Y, et al. Carbocisteine reduces virus-induced pulmonary inflammation in mice exposed to cigarette smoke. Am J Respir Cell Mol Biol. 2014 May;50(5):963-73.
[3]. Inoue M, et al. Carbocisteine promotes phagocytosis of apoptotic cells by alveolar macrophages. Eur J Pharmacol. 2012 Feb 29;677(1-3):173-9.
[4]. Wang W, et al. Carbocisteine attenuates hydrogen peroxide-induced inflammatory injury in A549 cells via NF-κB and ERK1/2 MAPK pathways. Int Immunopharmacol. 2015 Feb;24(2):306-313.
[5]. Yamaya M, et al. Inhibitory effects of carbocisteine on type A seasonal influenza virus infection in human airway epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2010 Aug;299(2):L160-8.
[6]. Hanaoka M, et al. Carbocisteine protects against emphysema induced by cigarette smoke extract in rats. Chest. 2011 May;139(5):1101-1108.
[7]. Abdelhamid AM, et al. Carbocisteine as a Modulator of Nrf2/HO-1 and NFκB Interplay in Rats: New Inspiration for the Revival of an Old Drug for Treating Ulcerative Colitis. Front Pharmacol. 2022 Jun 8;13:887233.
[8]. Song Y, et al. Carbocisteine inhibits the expression of Muc5b in COPD mouse model. Drug Des Devel Ther. 2019 Sep 16;13:3259-3268.
[9]. Song Y, et al. A mucoactive drug carbocisteine ameliorates steroid resistance in rat COPD model. Pulm Pharmacol Ther. 2016 Aug;39:38-47.
[10]. Ishibashi Y, et al. Effects of carbocisteine on altered activities of glycosidase and glycosyltransferase and expression of Muc5ac in SO2-exposed rats. Eur J Pharmacol. 2004 Mar 8;487(1-3):7-15.
[11]. Song Y, et al. Carbocysteine restores steroid sensitivity by targeting histone deacetylase 2 in a thiol/GSH-dependent manner. Pharmacol Res. 2015 Jan;91:88-98.
[12]. Yoshida M, et al. Carbocisteine inhibits oxidant-induced apoptosis in cultured human airway epithelial cells. Respirology. 2009 Sep;14(7):1027-34.
[13]. Wang W, et al. Carbocisteine attenuates TNF-α-induced inflammation in human alveolar epithelial cells in vitro through suppressing NF-κB and ERK1/2 MAPK signaling pathways. Acta Pharmacol Sin. 2016 May;37(5):629-36.
[14]. Paola Rogliani, et al. Efficacy and safety profile of mucolytic/antioxidant agents in chronic obstructive pulmonary disease: a comparative analysis across erdosteine, carbocysteine, and N-acetylcysteine. Respir Res. 2019 May 27;20(1):104.