Pharmacology of SC‐52458, an Orally Active, Nonpeptide Angiotensin AT1 Receptor Antagonist

@article{Olins1993PharmacologyOS,
  title={Pharmacology of SC‐52458, an Orally Active, Nonpeptide Angiotensin AT1 Receptor Antagonist},
  author={Gillian M. Olins and Valerie M. Corpus and Susan T. Chen and Ellen G. Mcmahon and Maria A. Palomo and D. E. Mcgraw and Glenn J. Smits and Christopher L Null and Melanie A. Brown and S E Bittner and John P. Koepke and Delores J. Blehm and Joseph R. Schuh and Chris J. Baierl and Robert E. Schmidt and Chyung S. Cook and David B. Reitz and Mark Andrew Penick and Robert E. Manning and Edward H. Blaine},
  journal={Journal of Cardiovascular Pharmacology},
  year={1993},
  volume={22},
  pages={677}
}
Summary We describe the pharmacologic properties of SC-52458, 5-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl]-2-[2-(1H-tetrazol-5-ylphenyl)]pyridine, a novel nonpeptide angiotensin II (AH) receptor antagonist. SC-52458 was a potent inhibitor of [125I]AII binding to AT, receptors in rat adrenal cortex and uterine smooth muscle membranes (IC50 values of 2.8 and 6.9 nM, respectively). Contraction of rabbit aortic rings by AII was antagonized by SC-52458 in a competitive and reversible manner (pA2 of… 
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Effects of SC-52458, an angiotensin AT1 receptor antagonist, in the dog.

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Results suggest that KT3-671 is a potentially useful antihypertensive drug and reduced the severity of the pathological changes in the kidney.

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The angiotensin II type 1 receptor antagonists. A new class of antihypertensive drugs.

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The expression of skeletal alpha-actin and ANP was selectively enhanced in the heart of vehicle-treated SHR compared with Wistar-Kyoto rats (WKY), thereby suggesting that the phenotypic modulation of myocytes occurred at the early stage of hypertension.