pyridin-3-yl)methyl)(l,l'-biphenyl)-2-yl)sulfonyIbenzamide) interacted in a competitive manner with rabbit aortic angiotensin II (All) receptors as determined by Scatchard analysis of specific binding of ['251]-Sar'lle8-All. MK-936 also exhibited high affinity at All receptors in several tissues from different animal species (K, = 0.1-0.4 nM). In vitro functional assays utilizing All-induced aldosterone release in rat adrenal cortical cells demonstrated further that MK-996 acts as a competitive, high affinity antagonist of All (PA, = 10.3) and lacks agonist activity. MK-996 also potently inhibited All-induced contractile response in isolated rabbit aorta and pulmonary artery with a reduction in maximal response. The specificity of for All receptors was demonstrated by its lack of activity (

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and selective ligand for the AT1 receptor, was prepared by N-benzoylation of L-159,221 with [a-llClbenzoyl chloride in tetrahydrofuran using lithium bis(trimethylsily1)amide as a base. The radiotracer was purified by semi-preparative reverse-phase HPLC. The average specific activity was 1162 mCi/pmol calculated at end-ofsynthesis (EOS). The average time of synthesis including formulation was 38 minutes.

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