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Angiotensin II receptors and functional correlates.
The angiotensin receptor and its functional correlates have been redefined by the cloning of angiotENSin receptors and the discovery and widespread study of specific nonpeptide ANG II-receptor antagonists losartan (AT1 selective) and PD123177 (AT2 selective). Expand
Angiotensin II receptor subtypes.
The AT1 and AT2 receptor subtypes/binding sites identified so far appears widespread and the presence and proportion of these receptors vary significantly among different tissues/organs of the same species and within the same tissue/organ of different species. Expand
Nonpeptide angiotensin II receptor antagonists. XI. Pharmacology of EXP3174: an active metabolite of DuP 753, an orally active antihypertensive agent.
The results demonstrate that EXP3174 is a selective and noncompetitive AII receptor antagonist and lacks agonistic effect and may be responsible for part of the antihypertensive effect of DuP 753 in rats. Expand
Functional studies of nonpeptide angiotensin II receptor subtype-specific ligands: DuP 753 (AII-1) and PD123177 (AII-2).
A function of the PD123177-sensitive AII binding site (AII-2) has not yet been identified, however, the DuP 753-sensitive site appears to mediate the AII-induced responses such as adrenal aldosterone and catecholamine secretion, release from sympathetic ganglia, drinking and vasoconstriction. Expand
Proposed update of angiotensin receptor nomenclature.
Angiotensin II exerts a wide range of actions on the heart, blood vessels, adrenals, kidneys, and nervous system and plays a major role in blood pressure maintenance and volume homeostasis. ItsExpand
Hypotensive action of DuP 753, an angiotensin II antagonist, in spontaneously hypertensive rats. Nonpeptide angiotensin II receptor antagonists: X.
The results suggest that the renin-angiotensin system plays a significant role in the control of blood pressure in spontaneously hypertensive rats, and indicates that captopril would need to be supplemented by a diuretic to reduce blood pressure to a similar extent as that of DuP 753. Expand
Nonpeptide angiotensin II receptor antagonists.
P Pieter Timmermans and colleagues review the pharmacology and the course of events that led to the identification of the lead compound and clinical candidate DuP753, and provides evidence for the existence of different binding sites/receptors for angiotensin II. Expand
Angiotensin II-1 receptors mediate both vasoconstrictor and hypertrophic responses in rat aortic smooth muscle cells.
Data indicate that the AII receptors on aortic smooth muscle cells of the rat are of the A II-1 receptor subtype, which is responsible for both the vasoconstrictor and hypertrophic responses of AII. Expand
Angiotensin II receptor subtypes: selective antagonists and functional correlates.
Both ACE (Ang II synthesis) inhibitors and Ang II receptor antagonists produce beneficial effects in experimental models of heart failure, suggesting Ang II is an important mediator ofheart failure. Expand