Abstract:
:Abbott-81282 (A-81282) has been identified among a series of related compounds as being a highly potent and selective antagonist of angiotensin receptors. At AT1 receptors of the rabbit aorta, A-81282 exhibited a pA2 of 9.64 (+/- 0.33) vs. angiotensin-II, and demonstrated characteristics consistent with competitive antagonism of this receptor. These results were supported in radioligand binding assays in which A-81282 inhibited the binding of [125I]-Sar-Il8-Angiotensin-II to rat liver membranes with a pKI of 8.505 (+/- 0.102). Selectivity of this agent for AT1 receptors was validated by its lack of activity at other receptor sites, such as alpha 1 receptors of isolated rabbit aorta. Moreover, A-81282 lacked affinity for AT2 receptors of bovine cerebellar membranes or for alpha or beta adrenergic receptor sites in radioligand binding assays. A-81282 lowered blood pressure significantly in vivo in renal artery-ligated rats at doses of 1 mg/kg i.v. or 5 mg/kg p.o. The compound was slowly and moderately absorbed from the duodenum of anesthetized rats and demonstrated low first-pass metabolism in the rat liver. Because of its selectivity and potency for antagonizing AT1 receptors, and its activity in lowering blood pressure in experimental animals, A-81282 has the potential to be a useful antihypertensive agent in man.
journal_name
Life Scijournal_title
Life sciencesauthors
Hancock AA,Buckner SA,Lee JY,Brune M,Morse PA,Oheim K,Warner RB,Winn M,Zydowsky TM,De Bdoi
10.1016/0024-3205(93)90445-9subject
Has Abstract,Author List Incompletepub_date
1993-01-01 00:00:00pages
929-37issue
11eissn
0024-3205issn
1879-0631pii
0024-3205(93)90445-9journal_volume
53pub_type
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