IRL 2500: A potent ET(B) selective endothelin antagonist

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 19, 1996, Pages 2323-2328

  Fruh Th ^a   Saika, H ^a   Svensson, L ^a   Pitterna, Th ^a   Sakaki, J ^a   Okada, T ^a   Urade, Y ^a   Oda, K ^a   Fujitani, Y ^a   Takimoto, M ^a   Yamamura, T ^a   Inui, T ^a   Makatani, M ^a   Takai, M ^a   Umemura, I ^a   Teno, N ^a   Toh, H ^b   Hayakawa, K ^a   Murata, T ^a  

^a CIBA GEIGY LTD   (Switzerland)

^b BIOMOL ENG RESEARCH INSTITUTE   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLO(DEXTRO TRYPTOPHYL DEXTRO ASPARTYLPROLYL DEXTRO VALYLLEUCYL); ENDOTHELIN B RECEPTOR; ENDOTHELIN RECEPTOR ANTAGONIST;

ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; GUINEA PIG; NONHUMAN; RAT; SMOOTH MUSCLE CONTRACTION; STRUCTURE ACTIVITY RELATION; THORACIC AORTA; TRACHEA;

EID: 0030575624     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00421-0     Document Type: Article

References (26)

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18. 3, 400 MHz) δ [ppm] 8.29 (s), 8.11 (s), 7.59 (d, J = 7.5 Hz), 7.33-6.90 (m), 6.81 (br), 6.69 (br), 6.52 (s), 5.95 (br), 5.86 (s), 5.35 (dxd, J = 7, 9.5 Hz), 4.2 (br), 3.76 (m), 3.62 (dxd, J = 7, 13 Hz), 3.52 (m), 3.35 (dxd, J = 7, 15 Hz), 3.15 (dxd, J = 10, 15 Hz), 3.05-2.8 (m), 2.72 (s), 2.22 (s), 1.97 (s).
19. 3, 400 MHz) δ [ppm] 8.29 (s), 8.15 (s), 7.56 (d, J = 7.8 Hz), 7.47 (d, J = 7.8 Hz), 7.3-6.7 (m), 6.48 (s), 5.92 (s), 5.41 (dxd, J = 6.8, 9.7 Hz), 4.84 (dxd, J = 5.8, 13.2 Hz), 4.33 (dxd, J = 2, 7.2 Hz), 3.4-2.75 (m), 2.70 (s), 2.18 (s), 1.91 (s).
20. 3, 400 MHz) δ [ppm] 8.32 (s), 8.22 (s), 7.6-6.8 (m), 6.93 (s), 6.8 (m), 6.51 (s), 5.97 (s), 5.46 (t, J = 8 Hz), 4.85 (q, J = 6 Hz), 4.36 (m), 3.4-2.8 (m), 2.73 (s), 2.15 (s), 1.85 (s).
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23. 3, 5.5 glucose and 0.01 EDTA; pH 7.4; 37°C) for isometric tension measurement at a resting tension of 1 g. Each preparation was first stimulated with 10 μM carbachol for the trachea or with 100 nM norepinephrine for the aorta to use as a reference standard for the responses to ET-3 for the trachea or ET-1 for the aorta. IRL 2500 was dissolved in dimethyl sulfoxide, the solution was diluted to 1/1000 with the Krebs-Henseleit solution, and then the whole volume of the Krebs-Henseleit solution in the organ bath was replaced with the solution containing IRL 2500.
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