Hydrochlorothiazide-13C6 is the 13C labeled drochlorothiazide[1]. drochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. drochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. drochlorothiazide improves cardiac function, reduces fibrosis and has antipertensive effect[2][3][4].
Stable heavy isotopes of drogen, 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[1].
References:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
[2]. Duarte, J.D. and R.M. Cooper-DeHoff, Mechanisms for blood pressure lowering and metabolic effects of thiazide and thiazide-like diuretics. Expert Rev Cardiovasc Ther, 2010. 8(6): p. 793-802.
[3]. Magdy M Abdelquader, et al. Inhibition of Co-Crystallization of Olmesartan Medoxomil and drochlorothiazide for Enhanced Dissolution Rate in Their Fixed Dose Combination. AAPS PharmSciTech. 2018 Dec 1720(1):3.
[4]. Jinghong Luo, et al. drochlorothiazide modulates ischemic heart failure-induced cardiac remodeling via inhibiting angiotensin II type 1 receptor pathway in rats. Cardiovasc Ther. 2017 Apr35(2).