Bradykinin receptor antagonists containing N-substituted amino acids: in vitro and in vivo B2 and B1 receptor antagonist activity

…, KG Kuhlman, TD Fitzpatrick, D Cuadrado…

文献索引：Goodfellow, Val S.; Marathe, Manoj V.; Kuhlman, Karen G.; Fitzpatrick, Timothy D.; Cuadrado, David; Hanson, Wendy; Zuzack, John S.; Ross, Sherman E.; Wieczorek, Maciej; Burkard, Michael; Whalley, Eric T. Journal of Medicinal Chemistry, 1996 , vol. 39, # 7 p. 1472 - 1484

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被引用次数: 31

摘要

We report a systematic probing of the structural requirements of the bradykinin (BK) type 2 (B2) receptor for antagonist activity by incorporating N-alkyl-amino acid residues at positions 7 and 8 of a potent antagonist sequence. Compound 1 (d-Arg0-Arg 1-Pro 2-Hyp 3-Gly 4-Thi 5-Ser 6-d-Tic 7-N-Chg 8-Arg 9, CP-0597) 1, 2 is a potent (p A 2= 9.3, rat uterus; p K i= 9.62, binding, human receptor clone) B2 receptor antagonist devoid of in vitro B1 antagonist ...