大鼠十二指肠平滑肌中的BK1和BK2缓激肽受体。

BK1 and BK2 bradykinin receptors in the rat duodenum smooth muscle.

Feres T, Paiva A C, Paiva T B

Department of Biophysics, Escola Paulista de Medicina, São Paulo, Brazil.

Br J Pharmacol. 1992 Dec;107(4):991-5. doi: 10.1111/j.1476-5381.1992.tb13396.x.

Abstract

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 preparation 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.

摘要

通过研究缓激肽对培养的十二指肠平滑肌细胞中3':5'-环磷酸腺苷（环磷酸腺苷）水平的影响以及蜂毒明肽对分离的肌肉对BK1和BK2受体激动剂和拮抗剂反应的影响，研究了缓激肽对大鼠十二指肠的双重作用（舒张和收缩）。2. 用高达100 nM缓激肽孵育的培养细胞中环磷酸腺苷含量未观察到变化。3. 蜂毒明肽（100 - 500 nM）抑制了对缓激肽和BK2特异性类似物[Thi5,8,D-Phe7]-缓激肽反应的舒张成分，并增强了收缩成分。4. 蜂毒明肽（100 - 500 nM）不影响拉伸十二指肠制剂对BK1特异性激动剂去-Arg9-缓激肽的收缩反应。5. BK2拮抗剂[D-Arg0Hyp3Thi5,8,D-Phe7]-缓激肽在完全抑制对缓激肽和[Thi5,8,D-Phe7]-缓激肽的舒张反应的浓度下，也能在蜂毒明肽存在时阻止对任何一种激动剂的收缩反应。6. 我们的结果表明大鼠十二指肠中存在两种缓激肽受体群体：一种BK2亚型负责未拉伸十二指肠的双相反应，一种BK1亚型负责对拉伸组织的收缩作用。