New, long‐acting, potent bradykinin antagonists
New, long‐acting, potent bradykinin antagonists
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新型、长效、强效缓激肽拮抗剂
DOI：
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发表时间：
1991
影响因子：
7.3
通讯作者：
J. Knolle
中科院分区：
文献类型：
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作者：
F. Lembeck;T. Griesbacher;M. Eckhardt;S. Henke;G. Breipohl;J. Knolle
1 Three new bradykinin (BK) antagonists, d‐Arg0‐Hyp3‐Thi5‐d‐Tic7‐Oic8‐BK (compound I), d‐Arg0‐Hyp3‐d‐Tic7‐Oic8‐BK (compound II), and Arg(Tos)1‐Hyp3‐Thi5‐d‐Tic7‐Oic8‐BK (compound III), were tested against the effects of BK in 9 bioassay preparations including visceral smooth muscles, vasoconstriction, plasma protein extravasation, release of prostaglandin E2, bronchoconstriction, and stimulation of afferent C‐fibre nociceptors. In some of these tests the effects of the new compounds were compared with those of the antagonist d‐Arg0‐Hyp2‐Thi5,8‐d‐Phe7‐BK (compound IV), described by Stewart & Vavrek (1987). 2 For all bioassays the general rank order of potency of the compounds was found to be I > II > III ≫ IV. The new antagonists were long‐acting; in some bioassays their effects outlasted the duration of the experiment. 3 The inhibitory effects of the new BK antagonists were specific for BK; actions of noradrenaline, angiotensin II, acetylcholine or histamine were unaffected by the antagonists. They did not stimulate the release of histamine or prostaglandins. An agonistic effect was observed only with very high concentrations of compounds I and II in the plasma protein extravasation test. 4 The long duration of action of the new BK antagonists is probably due to a high and long‐lasting affinity to the BK receptors. A high resistance of the antagonists to enzymatic destruction may be another reason. 5 The new BK antagonists will be valuable tools for the investigation of the pathophysiological role of BK. In addition they may offer a potential for therapeutic applications.
缓激肽作为疼痛介质：受体定位于感觉神经元，拮抗剂具有镇痛作用。
DOI：
10.1073/pnas.85.9.3245
发表时间：
1988
影响因子：
11.1
作者：
Steranka,LR;Manning,DC;DeHaas,CJ;Ferkany,JW;Borosky,SA;Connor,JR;Vavrek,RJ;Stewart,JM;Snyder,SH
通讯作者：
Snyder,SH
缓激肽类似物拮抗感觉神经元细胞系中缓激肽诱导的第二信使产生。
影响因子：
3.6
作者：
Francel,PC;Keefer,JF;Dawson,G
通讯作者：
Dawson,G
DOI：
10.1515/bc.2001.006
发表时间：
2001
期刊：
Biological chemistry.
影响因子：
--
作者：
Stewart,JM;Gera,L;York,EJ;Chan,DC;Whalley,EJ;BunnJr,PA;Vavrek,RJ
通讯作者：
Vavrek,RJ