BETA-ADRENOCEPTOR HETEROGENEITY IN GUINEA-PIG AIRWAYS - COMPARISON OF FUNCTIONAL AND RECEPTOR LABELING STUDIES
BETA-ADRENOCEPTOR HETEROGENEITY IN GUINEA-PIG AIRWAYS - COMPARISON OF FUNCTIONAL AND RECEPTOR LABELING STUDIES
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DOI：
10.1111/j.1476-5381.1983.tb10542.x
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发表时间：
1983-01-01
影响因子：
7.3
通讯作者：
NAHORSKI, SR
中科院分区：
文献类型：
--
作者：
CARSWELL, H;NAHORSKI, SR
的分布。通过放射配体结合试验和机械反应分析研究了豚鼠气道中的-肾上腺素能受体亚型。与配体[3H]-二氢阿普萘洛尔和[125I]-cyanopindolol的结合研究表明。肾上腺素受体在气道内分布不均匀，其密度以实质最高，气管密度最低。.beta.1的相对比例：.beta。通过计算机辅助分析选择性药物产生的抑制曲线来评估2-肾上腺素能受体结合位点。这两个区域几乎是相同的，另一个区域是15:85%。肾上腺素能受体激动剂引起气管螺旋和肺实质条的浓度依赖性松弛。这种反应似乎是由。1和。2-肾上腺素受体在气管螺旋中的pA2[竞争性拮抗活性]值。1选择性拮抗剂，阿替洛尔，根据使用的激动剂而变化，并且，在。β。2-肾上腺素受体拮抗剂ICI 118551[红- dl -1-（7-甲基林丹-4-氧基）-3-异丙基氨基丁醇]、去甲肾上腺素和异丙肾上腺素产生双相浓度-效应曲线。在肺实质条中，只有1亚型作为拮抗剂，pA2值不依赖于所使用的激动剂，其性质与预期的β - 2肾上腺素受体一致。
The distribution of .beta.-adrenoceptor subtypes in guinea-pig airways was studied by radioligand binding assays and analysis of mechanical responses. Binding studies with the ligands [3H]-dihydroalprenolol and [125I]-cyanopindolol, revealed that .beta.-adrenoceptors were unevenly distributed throughout the airways with the highest density located in the parenchyma and the lowest density in the trachea. The relative proportion of .beta.1:.beta.2-adrenoceptor binding sites was assessed by computer-assisted analysis of the inhibition curves generated by selective agents. It was virtually identical in each region and in the other of 15:85%. .beta.-Adrenoceptor agonists caused concentration-dependent relaxations of both tracheal spirals and parenchymal lung strips. This response appeared to be mediated by both .beta.1- and .beta.2-adrenoceptors in tracheal spirals as the pA2 [competitive antagonistic acitivty] value for the .beta.1-selective antagonist, atenolol, varied depending upon which agonist was used, and, in the presence of the .beta.2-adrenoceptor antagonist ICI 118,551 [erythro-DL-1-(7-methylindan-4-yloxy)-3-isopropylamino-butan-2-ol], noradrenaline [norepinephrine] and isoprenaline produced biphasic concentration-effect curves. In parenchymal lung strips only the 1 subtype was involved as antagonist pA2 values were not dependent on the agonist used and the properties were consistent with those expected for a .beta.2-adrenoceptor.