D-ARG[HYP3-THI5-D-TIC7-TIC8]-BRADYKININ, A POTENT ANTAGONIST OF SMOOTH-MUSCLE BK2 RECEPTORS AND BK3 RECEPTORS

被引：40

作者：

FARMER, SG ^{[1
]}

BURCH, RM ^{[1
]}

KYLE, DJ ^{[1
]}

MARTIN, JA ^{[1
]}

MEEKER, SN ^{[1
]}

TOGO, J ^{[1
]}

机构：

[1] NOVO PHARMACEUT CORP,BALTIMORE,MD 21224

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 1991年 / 102卷 / 04期

关键词：

BRADYKININ; BK2; RECEPTOR; BK3; ANTAGONIST; TRACHEA; ILEUM; SMOOTH MUSCLE; CA-45(2+) EFFLUX; CONTRACTION; BRADYKININ BINDING;

D O I：

10.1111/j.1476-5381.1991.tb12251.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

D-Arg[Hyp3-Thi5-D-Tic7-Tic8]-bradykinin (NPC 16731) inhibited bradykinin (BK) binding and BK-induced contraction in guinea-pig ileum, being markedly more potent than D-Phe7-BK analogues as a BK2 receptor antagonist. In isolated trachea NPC 16731, unlike other BK2 antagonists, inhibited BK binding and BK-induced contraction, and 45-Ca2+ efflux in tracheal smooth muscle cells. That NPC 16731 potently inhibits BK effects in trachea provides further evidence for the existence of the airway BK3 receptor.

引用

页码：785 / 787

页数：3

共 9 条

[1] BRADYKININ RECEPTOR ANTAGONISTS [J].