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β-肾上腺素能受体激动剂对豚鼠输尿管氯化钾诱导的节律性收缩的影响。

The effects of beta-adrenoceptor agonists on KCl-induced rhythmic contraction in the ureter of guinea pig.

作者信息

Yamamoto Y, Koike K

机构信息

Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Funabashi, Chiba, Japan.

出版信息

J Smooth Muscle Res. 2000 Feb;36(1):13-9. doi: 10.1540/jsmr.36.13.

Abstract

In the present study, we tried to determine what effects were induced by beta-adrenoceptor agonists on 40 mM KCl-induced rhythmic contraction and to clarify which beta-adrenoceptor subtypes are involved in the regulation of ureter motility in the guinea pig by using in vitro functional analysis. 40 mM KCl-induced rhythmic contraction was abolished by papaverine (10(-6) M), nicardipine (10(-5) M) and cromakalim (10(-5) M), but was not influenced by atropine (10(-6) M). Isoprenaline decreased the amplitude, and changed the pattern of 40 mM KCl-induced rhythmic contraction in concentration-dependent manner. These results suggest the possibility that the stimulation of beta-adrenoceptors may regulate the ureteral peristalsis. Salbutamol (selective beta2-AR agonist) and CGP12177 (beta(1,2)-AR antagonist and beta3-AR partial agonist) were also effective in decreasing the amplitude and changing the pattern of the rhythmic contraction. The pD2 values of agonists were 7.57 (isoprenaline), 5.80 (CGP12177) and 7.63 (salbutamol), respectively. The concentration-response curves of isoprenaline and salbutamol were rightward shifted by the presence of propranolol, and the apparent pA2 values for propranolol against isoprenaline and salbutamol were 7.12 and 6.29, respectively. These results suggest that inhibition for 40 mM KCl-induced rhythmic contraction of the ureter by isoprenaline and salbutamol mediated mainly via atypical beta-adrenoceptor subtype.

摘要

在本研究中,我们试图确定β-肾上腺素能受体激动剂对40 mM氯化钾诱导的节律性收缩有何影响,并通过体外功能分析阐明豚鼠输尿管运动调节中涉及哪些β-肾上腺素能受体亚型。罂粟碱(10^(-6) M)、尼卡地平(10^(-5) M)和克罗卡林(10^(-5) M)可消除40 mM氯化钾诱导的节律性收缩,但不受阿托品(10^(-6) M)影响。异丙肾上腺素以浓度依赖的方式降低了振幅,并改变了40 mM氯化钾诱导的节律性收缩模式。这些结果提示,刺激β-肾上腺素能受体可能调节输尿管蠕动。沙丁胺醇(选择性β2-AR激动剂)和CGP12177(β(1,2)-AR拮抗剂和β3-AR部分激动剂)在降低振幅和改变节律性收缩模式方面也有效。激动剂的pD2值分别为7.57(异丙肾上腺素)、5.80(CGP12177)和7.63(沙丁胺醇)。普萘洛尔的存在使异丙肾上腺素和沙丁胺醇的浓度-反应曲线右移,普萘洛尔对异丙肾上腺素和沙丁胺醇的表观pA2值分别为7.12和6.29。这些结果表明,异丙肾上腺素和沙丁胺醇对40 mM氯化钾诱导的输尿管节律性收缩的抑制作用主要通过非典型β-肾上腺素能受体亚型介导。

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