BK1 and BK2 bradykinin receptors in the rat duodenum smooth muscle

BK1 and BK2 bradykinin receptors in the rat duodenum smooth muscle
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大鼠十二指肠平滑肌中的 BK1 和 BK2 缓激肽受体

DOI:
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发表时间:
1992
影响因子:
7.3
通讯作者:
T. B. Paiva
T. B. Paiva
中科院分区:
医学2区
文献类型:
--
作者:
T. Feres;A. Paiva;T. B. Paiva

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通过研究缓激素对培养十二指肠平滑肌细胞中腺苷3′:5′-环磷酸腺苷(环AMP)水平的影响,以及apamin对分离肌肉对BK1和BK2受体激动剂和拮抗剂反应的影响,探讨了缓激素(舒张和收缩)对大鼠十二指肠的双重作用。2与缓激肽孵育至100 nm时,培养细胞的环AMP含量未见变化。3 . Apamin (100-500 nm)抑制了缓激肽和BK2特异性类似物[thi5,8,d - Phe7] -缓激肽反应的松弛成分,增强了收缩成分。4 . Apamin (100-500 nm)不影响拉伸十二指肠制剂对BK1特异性激动剂des - Arg9 - bradykinin的收缩反应。BK2拮抗剂[d‐arg0hyp3thi5,8,d‐Phe7]‐bradykinin的浓度可以完全抑制对bradykinin和[thi5,8,d‐Phe7]‐bradykinin的松弛反应,也可以在apamin存在时阻止对任何一种激动剂的收缩反应。我们的研究结果表明,大鼠十二指肠中存在两种缓激肽受体:BK2亚型负责非拉伸十二指肠的双相反应,BK1亚型负责拉伸组织的收缩作用。
1 The dual action of bradykinin (relaxation and contraction) on the rat duodenum was investigated by studying its effect on adenosine 3′:5′‐cyclic monophosphate (cyclic AMP) levels in cultured duodenal smooth muscle cells, and the effects of apamin on the isolated muscle responses to agonists and antagonists of BK1 and BK2 receptors. 2 No change was observed in the cyclic AMP content of cultured cells incubated with up to 100 nm bradykinin. 3 Apamin (100–500 nm) inhibited the relaxant component and enhanced the contractile component of the responses to bradykinin and to the BK2‐specific analogue [Thi5,8,d‐Phe7]‐bradykinin. 4 Apamin (100–500 nm) did not affect the contractile response of stretched duodenum preparations to the BK1‐specific agonist des‐Arg9‐bradykinin. 5 The BK2 antagonist, [d‐Arg0Hyp3Thi5,8,d‐Phe7]‐bradykinin, at a concentration which completely inhibited the relaxant response to bradykinin and to [Thi5,8,d‐Phe7]‐bradykinin, also prevented the contraction in response to either agonist in the presence of apamin. 6 Our results demonstrate two populations of bradykinin receptors in rat duodenum: a BK2 subtype responsible for the biphasic response of the non‐stretched duodenum, and a BK1 subtype responsible for the contractile effect on the stretched tissue.
经典激肽系统的缓激肽竞争性拮抗剂。
DOI: 10.1007/978-1-4684-5143-6_71
发表时间: 1986
影响因子: --
作者:
Stewart,JM;Vavrek,RJ
通讯作者: Vavrek,RJ