Fimasartan (BR-A-657) is an orally active, highly potent angiotensin II receptor AT1 (AGTR1) antagonist (blocker) that selectively blocks AngII-, but not KCl- or noradrenaline-, induced contraction of rabbit thoracic aortic rings (IC50 = 0.42 nM) with 615-fold higher AT1 affinity than losartan (IC50 = 0.13 nM vs. 80 nM against 0.05 nM AngII for binding rat adrenal cortex). Fimasartan significantly decreases mean arterial blood pressure with rapid onset (in 0.5 h) in spontaneously hypertensive rats (Emax of 75% reduction, 5-24 hr post 10 mg/kg p.o.) and is ~19-fold more effective than losartan against AngII (100 ng/kg i.v.)-induced pressor response in rats in vivo (ED50 = 18 ng/kg vs. 336 ng/kg i.v.).
Orally active, highly potent angiotensin II receptor AT1 (AGTR1) antagonist with superior in vivo antihypertensive efficacy than Losartan.
The pharmacological profile of BR-A-657, 2-n-butyl-5-dimethylamino-thiocarbonyl-methyl-6-methyl-3-{[2-(1H-tetrazole-5-yl)biphenyl-4-yl]methyl}-pyrimidin-4(3H)-one, a new nonpeptide AT1-selective angiotensin receptor antagonist, has been investigated in a variety of in vitro and in vivo experimental models. In the present study, BR-A-657 displaced [(125)I][Sar(1)-Ile(8)]angiotensin II (Ang II) from its specific
Expert opinion on drug metabolism & toxicology, 14(5), 533-541 (2018-04-21)
Fimasartan is the ninth and latest Angiotensin Receptor Blockers for the treatment of hypertension. Fimasartan is a derivative of losartan in which the imidazole ring has been replaced. It provides a selective type 1 angiotensin II receptor antagonist effect with
Journal of cardiovascular pharmacology, 62(2), 229-236 (2013-04-26)
To evaluate the effect of the novel angiotensin receptor blocker Fimasartan on the development of atherosclerosis and plaque stabilization in an animal model. Twenty-four rabbits received an aortic balloon injury from 30 cm to a level just above the aortic
