TH-142177

**TH-142177** is a potent and selective small molecule antagonist of the angiotensin II type 1 (AT1) receptor. In preclinical studies, it exhibited three times greater potency than losartan for inhibiting angiotensin II-induced vasoconstriction and specifically blocked AT1 receptors without affecting AT2 receptors at tested concentrations. TH-142177 produces a dose-dependent, long-lasting reduction in blood pressure when administered orally in hypertensive rats without a significant effect on heart rate. It also selectively and durably occupies angiotensin II receptors in the myocardium and adrenal cortex, with kinetics paralleling its antihypertensive effects. It has been studied primarily for antihypertensive and cardiovascular applications, including effects on vascular smooth muscle proliferation and neointimal formation[1][4][7].

Other names

N-n-butyl-N-[2'-(1-H-tetrazole-5-yl) biphenyl-4-yl]-methyl-(N-carboxymethyl-benzylamino)-acetamide