Telmisartan-13C,d3

Names

[ Name ]:
Telmisartan-13C,d3

[Synonym ]:
[1,1'-Biphenyl]-2-carboxylic acid, 4'-[[4'-methyl-1-(methyl-13C-d3)-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl]methyl]-
4'-{[7'-Methyl-1-(13C,2H3)methyl-2'-propyl-1H,3'H-2,5'-bibenzimidazol-3'-yl]methyl}-2-biphenylcarboxylic acid

Biological Activity

[Description]:

Telmisartan-13C,d3 is the 13C- and deuterium labeled. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Research Areas >> Endocrinology

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

[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[55].

[References]

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.

[2]. Maillard MP, et al. In vitro and in vivo characterization of the activity of telmisartan: an insurmountable angiotensin II receptor antagonist. J Pharmacol Exp Ther. 2002 Sep;302(3):1089-95.

[3]. Xuan H, et al. Inhibition or deletion of angiotensin II type 1 receptor suppresses elastase-induced experimental abdominal aortic aneurysms. J Vasc Surg. 2017 Apr 20. pii: S0741-5214(17)30100-3.

[4]. Torika N, et al. Intranasal telmisartan ameliorates brain pathology in five familial Alzheimer's disease mice. Brain Behav Immun. 2017 Apr 3.

[5]. Aswar U, et al. Telmisartan attenuates diabetes induced depression in rats. Pharmacol Rep. 2017 Apr;69(2):358-364.

[6]. Fujihara S, et al. The angiotensin II type 1 receptor antagonist telmisartan inhibits cell proliferation and tumor growth of esophageal adenocarcinoma via the AMPKα/mTOR pathway in vitro and in vivo. Oncotarget. 2017 Jan 31;8(5):8536-8549.