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Clinical and Experimental Hypertension Volume 18, 1996 - Issue 2
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Original Article

Nonpeptide Angiotensin II Receptor Antagonists: In Vivo Inhibition of [125I-SAR1, ILE8]Angiotensin II Binding by Losartan, EXP597 and L-159,282 in Rats

Pancras C. Wong Preclinical Pharmacology Group The DuPont Merck Pharmaceutical Company, Wilmington, Delaware, 19880-0400
,
William F. Herblin Preclinical Pharmacology Group The DuPont Merck Pharmaceutical Company, Wilmington, Delaware, 19880-0400
,
Frank A. Barbera Preclinical Pharmacology Group The DuPont Merck Pharmaceutical Company, Wilmington, Delaware, 19880-0400
,
Roberta Bernard Preclinical Pharmacology Group The DuPont Merck Pharmaceutical Company, Wilmington, Delaware, 19880-0400
,
Tracy A. Bozarth Preclinical Pharmacology Group The DuPont Merck Pharmaceutical Company, Wilmington, Delaware, 19880-0400
,
Carol A. Watson Preclinical Pharmacology Group The DuPont Merck Pharmaceutical Company, Wilmington, Delaware, 19880-0400
&
Raymond E. Gibson Merck Research Laboratories West Point, Pennsylvania, 19486
 show all
Pages 189-200 | Received 19 Jun 1995, Accepted 16 Aug 1995, Published online: 03 Jul 2009

References

  • Wong P C, Chiu A T, Duncia J V, Herblin W F, Smith R D, Timmermans P BMWM. Angiotensin II receptor antagonists and receptor subtypes. Trends Endocrinol Metab 1992; 3: 211–217
  • Chang R SL, Lotti V J. Two distinct angiotensin II receptor binding sites in rat adrenal revealed by new selective nonpeptide ligands. Mol Pharmacol 1990; 29: 347–351
  • Chiu A T, Herblin W F, Ardecky R J, McCall D E, Carini D J, Duncia J V, Pease L J, Wexler R R, Wong P C, Johnson A L, Timmermans P BMWM. Identification of angiotensin II receptor subtypes. Biochem Biophys Res Commun 1989; 165: 196–203
  • Whitebread S, Mele M, Kamber B, de Gasparo M. Preliminary biochemical characterization of two angiotensin II receptor subtypes. Biochem Biophys Res Commun 1989; 163: 284–291
  • Wong P C, Hajj-Ali A F. Functional correlates of angiotensin receptor stimulation. Medicinal Chemistry of the Renin-Angiotensin System, P BMW Timmerman, R R Wexler. Elsevier Science, Amsterdam 1994; 313–346
  • Wong P C, Duncia J V, Santella J B, III, Smith R D, Wexler R R, Timmermans P BMWM, Chiu A T. EXP597, a nonpeptide angiotensin II receptor antagonist with high affinities for the AT1 and AT2 receptor subtypes. Eur J Pharmacol 1994; 260: 261–264
  • Gibson R E, Beauchamp H T, Fioravanti C, Brenner N, Burns H D. Receptor binding radiotracers for the angiotensin II receptor: radioiodinated [Sar1,Ile8]angiotensin II. Nucl Med Biol 1994; 21: 593–600
  • Chakravarty P K, Naylor E M, Chen A, Chang R SL, Chen T B, Faust K A, Lotti V J, Kivlighn S D, Gable R A, Zingaro G J, Schorn T W, Schaffer L W, Broten T P, Siegl P KS, Patchett A A, Greenlee W J. A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1 selective angiotensin II receptor antagonist. J Med Chem 1994; 37: 4068–4070
  • Beauchamp H T, Chang R SL, Siegl P KS, Gibson R E. In vivo receptor occupancy of the angiotensin II receptor by nonpeptide antagonists: relationship to in vitro affinities and in vivo pharmacologic potency. J Pharmacol Exp Ther 1995; 272: 612–618
  • Wong PC, Price W A, Chiu A T, Duncia J V, Carini D J, Wexler R R, Johnson A L, Timmermans P BMWM. Nonpeptide angiotensin II receptor antagonists XI. Pharmacology of EXP3174, an active metabolite of DuP 753 — an orally active antihypertensive agent. J Pharmacol Exp Ther 1990; 255: 211–217

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