Candesartan (CAS 139481-59-7) is an angiotensin II receptor I (AT1) antagonist, IC50s=1.12 and 2.86 nM for bovine adrenal cortex and rabbit aorta respectively.1 Selectively inhibits angiotensin II-induced contraction of rabbit aortic strips with no effect on contraction induced by other agents such as norepinephrine, KCl, serotonin, PGF2αor endothelin. Prevents astrocyte and microglial activation and neuroinflammation and improves hippocampal neurogenesis.2 Attenuates angiogenesis in hepatocellular carcinoma.3 Clinically useful antihypertensive agent. Ameliorates brain inflammation associated with Alzheimer’s disease.4 Active in vivo and orally active.
1) Shibouta et al. (1993), Pharmacological profile of a highly potent and long-acting angiotension II receptor antagonist, 2-ethoxy-1-[[2’-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazol-7-carboxylic acid (CV-11974), and its prodrug, (+/-)-1-(cyclohexyloxycarbonyloxy)-ethyl 2-ethoxy-1-[[2’-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate (TCV-116); J. Pharmacol. Exp. Therap., 266 114
2) Bhat et al. (2017), Angiotensin receptor Blockade by Inhibiting Glial Activation Promates Hippocampal Neurogenesis Via Activation of Wnt/B-Catenin signaling in hypertension; Mol. Neurobiol., Epub ahead of print
3) Fan et al. (2016), Candesartan attenuates angiogenesis in hepatocellular carcinoma via downregulating AT1R/VEGF pathway; Biomed. Pharmacother., 83 704
4) Torika et al. (2018), Candesartan ameliorates brain inflammation associated with Alzheimer’s disease; CNS Neurosci. Ther. 24 231