COMPARATIVE ACTION OF NEW HIGHLY POTENT BRADYKININ RECEPTOR ANTAGONISTS IN THE GUINEA-PIG TRACHEA

被引：22

作者：

TRIFILIEFF, A ^{[1
]}

AMRANI, Y ^{[1
]}

LANDRY, Y ^{[1
]}

GIES, JP ^{[1
]}

机构：

[1] UNIV STRASBOURG I,INSERM,CJF 9105,NEUROIMMUNOPHARMACOL LAB,F-67401 ILLKIRCH GRAFFENS,FRANCE

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1993年 / 239卷 / 1-3期

关键词：

BRADYKININ; BRADYKININ RECEPTOR ANTAGONISTS; TRACHEA; BRADYKININ BINDING; (GUINEA-PIG);

D O I：

10.1016/0014-2999(93)91000-D

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

We investigated the effect of two new bradykinin receptor antagonists, D-Arg0[Hyp3,D-HypE(trans-propyl)7,OiC8]bradykinin (NPC 17731) and D-Argo[Hyp3,D-HypE(trans-thiophenyl)7,Oic8]bradykinin (NPC 17761) on [H-3]bradykinin binding and on bradykinin-induced contraction of the guinea-pig trachea. Both of these compounds inhibited [H-3]bradykinin binding with an affinity similar to that of unlabelled bradykinin. NPC 17731 inhibited bradykinin-induced contraction in a non-competitve manner, whereas NPC 17761 showed competitive antagonism. Therefore, NPC 17761 could contribute to the investigation of the bradykinin receptors in guinea-pig airways.

引用

页码：227 / 229

页数：3

共 11 条

[1]

BARNES PJ, 1988, PHARMACOL REV, V40, P49

[2]

FARMER SG, 1989, MOL PHARMACOL, V36, P1

[3]

HOCK FJ, 1991, BRIT J PHARMACOL, V102, P769, DOI 10.1111/j.1476-5381.1991.tb12248.x

[4] PROBING THE BRADYKININ RECEPTOR - MAPPING THE GEOMETRIC TOPOGRAPHY USING ETHERS OF HYDROXYPROLINE IN NOVEL PEPTIDES [J].

KYLE, DJ ;

MARTIN, JA ;

BURCH, RM ;

CARTER, JP ;

LU, SF ;

MEEKER, S ;

PROSSER, JC ;

SULLIVAN, JP ;

TOGO, J ;

NORONHABLOB, L ;

SINSKO, JA ;

WALTERS, RF ;

WHALEY, LW ;

HINER, RN .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (08) :2649-2653

[5] CONVERSION OF KININS AND THEIR ANTAGONISTS INTO-B-1 RECEPTOR ACTIVATORS AND BLOCKERS IN ISOLATED VESSELS [J].

REGOLI, D ;

DRAPEAU, G ;

ROVERO, P ;

DION, S ;

RHALEB, NE ;

BARABE, J ;

DORLEANSJUSTE, P ;

WARD, P .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1986, 127 (03) :219-224

[6]

REGOLI D, 1980, PHARMACOL REV, V32, P1

[7] NEW SELECTIVE BRADYKININ RECEPTOR ANTAGONISTS AND BRADYKININ-B2 RECEPTOR CHARACTERIZATION [J].

REGOLI, D ;

RHALEB, NE ;

DION, S ;

DRAPEAU, G .

TRENDS IN PHARMACOLOGICAL SCIENCES, 1990, 11 (04) :156-161

[8] PHARMACOLOGICAL CHARACTERIZATION OF A NEW HIGHLY POTENT B2-RECEPTOR ANTAGONIST (HOE 140-D-ARG-[HYP3,THI5,D-TIC7,OIC8]BRADYKININ) [J].

RHALEB, NE ;

ROUISSI, N ;

JUKIC, D ;

REGOLI, D ;

HENKE, S ;

BREIPOHL, G ;

KNOLLE, J .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 210 (02) :115-120

[9]

TRIFILIEFF A, 1992, J PHARMACOL EXP THER, V263, P1377

[10] COMPETITIVE ANTAGONISTS OF BRADYKININ [J].

VAVREK, RJ ;

STEWART, JM .

PEPTIDES, 1985, 6 (02) :161-164

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