EXP597, A NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONIST WITH HIGH AFFINITIES FOR THE ANGIOTENSIN AT(1) AND AT(2) RECEPTOR SUBTYPES

AT(1) and AT(2) are the two major receptor subtypes for angiotensin II that have been pharmacologically defined by using the selective ligan ds losartan and PD123177, respectively. EXP597 '-isoamyloxycarbonylami nosulfonyl-[1,1']-biphenyl, potassium salt) is a nonpeptide angiotensi n II receptor ligand which in the rat adrenal exhibits binding affinit ies (IC50) of 0.5 and 0.7 nM for angiotensin AT(1) and AT(2) receptor subtypes, respectively. Further, EXP597 is an insurmountable angiotens in II receptor antagonist in the isolated rabbit aorta and lowers bloo d pressure in renal hypertensive rats with i.v. and p.o. ED(30) values of 0.05 and 0.9 mg/kg, respectively.