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负责缓激肽在大鼠十二指肠中双相效应的受体的特性研究。

Characterization of the receptors responsible for the diphasic effect of bradykinin in rat duodenum.

作者信息

Pereira C C, Paiva T B

机构信息

Departamento de Biofísica, Escola Paulista de Medicina, São Paulo, Brasil.

出版信息

Braz J Med Biol Res. 1989;22(9):1137-40.

PMID:2561460
Abstract

The response of the rat duodenum to bradykinin (BK) consists of relaxant and contractile components, which have been attributed to different receptor types. To characterize the receptors responsible for this diphasic response we studied the effects of BK analogues known to act on B1 or B2 receptors in other systems. DesArg9-Leu8-BK and Thi5,8DPhe7-BK presented only relaxant and only contractile effects, respectively, whereas DArg0Hyp3Thi5,8DPhe7-BK was a potent antagonist of the relaxation (but not of the contraction) induced by BK. Our results show that the relaxant and contractile components of the rat duodenum's response to BK are due to B2 and B1 receptor subtypes, respectively.

摘要

大鼠十二指肠对缓激肽(BK)的反应包括舒张和收缩成分,这两种成分被认为分别归因于不同的受体类型。为了表征介导这种双相反应的受体,我们研究了已知在其他系统中作用于B1或B2受体的BK类似物的效应。去精氨酸9-亮氨酸8-缓激肽(DesArg9-Leu8-BK)和噻吩5,8-二苯丙氨酸7-缓激肽(Thi5,8DPhe7-BK)分别仅呈现舒张和收缩效应,而D-精氨酸0-羟脯氨酸3-噻吩5,8-二苯丙氨酸7-缓激肽(DArg0Hyp3Thi5,8DPhe7-BK)是BK诱导的舒张(而非收缩)的强效拮抗剂。我们的结果表明,大鼠十二指肠对BK反应的舒张和收缩成分分别归因于B2和B1受体亚型。

相似文献

1
Characterization of the receptors responsible for the diphasic effect of bradykinin in rat duodenum.负责缓激肽在大鼠十二指肠中双相效应的受体的特性研究。
Braz J Med Biol Res. 1989;22(9):1137-40.
2
Role of B1 and B2 receptors and of nitric oxide in bradykinin-induced relaxation and contraction of isolated rat duodenum.B1和B2受体以及一氧化氮在缓激肽诱导的离体大鼠十二指肠舒张和收缩中的作用。
Life Sci. 1994;55(17):1351-63. doi: 10.1016/0024-3205(94)00768-3.
3
Selectivity of bradykinin analogues for receptors mediating contraction and relaxation of the rat duodenum.缓激肽类似物对介导大鼠十二指肠收缩和舒张的受体的选择性。
Br J Pharmacol. 1989 Sep;98(1):206-10. doi: 10.1111/j.1476-5381.1989.tb16883.x.
4
Further evidence for the existence of two receptor sites for bradykinin responsible for the diphasic effect in the rat isolated duodenum.缓激肽存在两个受体位点,这两个位点对大鼠离体十二指肠的双相效应负责,进一步的证据。
Br J Pharmacol. 1984 Oct;83(2):591-600. doi: 10.1111/j.1476-5381.1984.tb16523.x.
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Bradykinin B2 receptor evoked K+ permeability increase mediates relaxation in the rat duodenum.缓激肽B2受体诱发的钾离子通透性增加介导大鼠十二指肠舒张。
Eur J Pharmacol. 1991 Feb 7;193(2):231-8. doi: 10.1016/0014-2999(91)90041-n.
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Inflammation modifies the role of cyclooxygenases in the contractile responses of the rat detrusor smooth muscle to kinin agonists.炎症改变了环氧化酶在大鼠逼尿肌平滑肌对激肽激动剂收缩反应中的作用。
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DesArg9-D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin (desArg10-[Hoe140]) is a potent bradykinin B1 receptor antagonist.
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Bradykinin suppresses endothelin-induced contraction of coronary artery through its B2-receptor on the endothelium.
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DesArg10[Hoe 140] is a potent B1 bradykinin antagonist.
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Bradykinin-induced burst of prostaglandin formation in osteoblasts is mediated via B2 bradykinin receptors.缓激肽诱导成骨细胞中前列腺素生成的爆发是通过B2缓激肽受体介导的。
J Bone Miner Res. 1991 Aug;6(8):807-15. doi: 10.1002/jbmr.5650060805.

引用本文的文献

1
New, long-acting, potent bradykinin antagonists.新型长效强效缓激肽拮抗剂。
Br J Pharmacol. 1991 Feb;102(2):297-304. doi: 10.1111/j.1476-5381.1991.tb12169.x.
2
BK1 and BK2 bradykinin receptors in the rat duodenum smooth muscle.大鼠十二指肠平滑肌中的BK1和BK2缓激肽受体。
Br J Pharmacol. 1992 Dec;107(4):991-5. doi: 10.1111/j.1476-5381.1992.tb13396.x.
3
Kinin-induced relaxations of the rat duodenum.激肽诱导的大鼠十二指肠舒张
Naunyn Schmiedebergs Arch Pharmacol. 1992 Jul;346(1):102-7. doi: 10.1007/BF00167578.