Pharmacologic characterization of S-1255, a highly potent and orally active endothelin a receptor antagonist

Journal of Cardiovascular Pharmacology

Volumn 37, Issue 4, 2001, Pages 471-482

  Iwasaki, T ^a   Mihara, S I ^a   Shimamura, T ^a   Kawakami, M ^a   Masui, M ^a   Hayasaki Kajiwara, Y ^a   Naya, N ^a   Ninomiya, M ^a   Fujimoto, M ^a   Nakajima, M ^a  

^a SHIONOGI AND CO LTD   (Japan)

Author keywords

Antagonist; Contraction; Endothelin; Hypotensive effect; Rat; Relaxation

Indexed keywords

2 (1,3 BENZODIOXOL 5 YL) 6 ISOPROPYL 4 (4 METHOXYPHENYL) 2H CHROMENE 3 CARBOXYLIC ACID; 2 (BENZO 1,3 DIOXOL 5 YL) 6 ISOPROPYL 4 (4 METHOXYPHENYL) 2H CHROMENE 3 CARBOXYLIC ACID; 3 (2 CARBOXYMETHOXY 4 METHOXYPHENYL) 1 (3,4 METHYLENEDIOXYPHENYL) 5 PROPOXY 2 INDANCARBOXYLIC ACID; BOSENTAN; CYCLO(DEXTRO TRYPTOPHYL DEXTRO ASPARTYLPROLYL DEXTRO VALYLLEUCYL); DEOXYCORTICOSTERONE ACETATE; ENDOTHELIN 1; ENDOTHELIN A RECEPTOR; ENDOTHELIN A RECEPTOR ANTAGONIST; ENDOTHELIN B RECEPTOR ANTAGONIST; L 749329; N (2,6 DIMETHYLPIPERIDINOCARBONYL) 4 METHYLLEUCYL DEXTRO (1 METHOXYCARBONYLTRYPTOPHANYL) DEXTRO NORLEUCINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANTIHYPERTENSIVE ACTIVITY; ARTICLE; BINDING AFFINITY; DOSE RESPONSE; DRUG INHIBITION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; MALE; NONHUMAN; PRESSOR RESPONSE; PRIORITY JOURNAL; RABBIT; RAT; SMOOTH MUSCLE CONTRACTION; SWINE;

ANIMALS; AORTA; BENZOPYRANS; BLOOD PRESSURE; CHO CELLS; CRICETINAE; ENDOTHELINS; ENDOTHELIUM, VASCULAR; HUMANS; HYPERTENSION; MALE; MOLECULAR STRUCTURE; MUSCLE, SMOOTH, VASCULAR; RABBITS; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; RECEPTOR, ENDOTHELIN A; RECEPTORS, ENDOTHELIN; SWINE; VASOCONSTRICTOR AGENTS; VIPER VENOMS;

EID: 0035081207     PISSN: 01602446     EISSN: None     Source Type: Journal    
DOI: 10.1097/00005344-200104000-00014     Document Type: Article

References (38)

1. A novel potent vasoconstrictor peptide produced by vascular endothelial cells
2. The human endothelin family: Three structurally and pharmacologically distinct isopeptides predicted by three separate genes
3. Cloning and expression of a cDNA encoding an endothelin receptor
4. Cloning of a cDNA encoding a non-isopeptide-selective subtypes of the endothelin receptor
5. B receptors mediating venous smooth muscle contraction
6. B receptors cause vasoconstriction of human resistance and capacitance vessels in vivo
7. Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor
8. B receptor in rabbit mesenteric arteries
9. Evidence for endothelin-1-mediated vasoconstriction in severe chronic heart failure
10. Increased plasma endothelin-1 in pulmonary hypertension: Marker or mediator of disease?
11. The effect of an endothelin-receptor antagonist, bosentan, on blood pressure in patients with essential hypertension
12. Role of endothelin in the increased vascular tone of patients with essential hypertension
13. Acute endothelin A receptor blockade causes selective pulmonary vasodilation in patients with chronic heart failure
14. Hemodynamic effects of bosentan, an endothelin receptor antagonist, in patients with pulmonary hypertension
15. A receptor subtype
16. Molecular cloning and characterization of the major endothelin receptor subtype in porcine cerebellum
17. A receptor in the maintenance of deoxycorticosterone acetate-salt-induced hypertension
18. Pharmacological characterization of PABSA, an orally active and highly potent endothelin-receptor antagonist
19. Quantitative analysis of drug receptor interactions. I. Determination of kinetic and equilibrium properties
20. The attractions of proteins for small molecules and ions
21. 50) of an enzyme reaction
22. The estimation of the ED50 for a logistic response curve
23. Some quantitative uses of drug antagonists
24. Endothelin-3-induced relaxation of rat thoracic aorta: A role for nitric oxide formation
25. A receptor antagonist
26. Nonpeptide endothelin receptor antagonists. II. Pharmacological characterization of SB 209670
27. Pharmacology of L-754,142, a highly potent, orally active, nonpeptidyl endothelin antagonist
28. Pharmacological profile of T-0201, a highly potent and orally active endothelin receptor antagonist
29. A receptor
30. Use of the endothelin antagonists BQ-123 and PD 142893 to reveal three endothelin receptors mediating smooth muscle contraction and the release of EDRF
31. Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist
32. Dup753 is a specific antagonist for the angiotensin receptor
33. Molecular cloning of the canine angiotensin II receptor
34. Agonist-antagonist interactions at angiotensin receptors: Application of a two-state receptor model
35. Tissue specificity of endothelin binding sites
36. Contribution of endogenous endothelin-1 to the progression of cardiopulmonary alterations in rats with monocrotaline-induced pulmonary hypertension
37. Inhibition of myocardial endothelin pathway improves long-term survival in heart failure
38. Acute hemodynamic and neurohumoral effects of selective ETA receptor blockade in patients with congestive heart failure