Goldie R G, Paterson J W, Spina D, Wale J L
Br J Pharmacol. 1984 Apr;81(4):611-5. doi: 10.1111/j.1476-5381.1984.tb16125.x.
(+/-)-Isoprenaline (Iso), (-)-adrenaline (Ad), (-)-noradrenaline (NA), (+/-)-phenylephrine (Phe) and the beta 2-selective adrenoceptor agonist (+/-)-fenoterol (Fen) caused a concentration-dependent relaxation of human isolated bronchial preparations. Iso, Ad and NA caused complete relaxation of both spontaneous and carbachol-induced bronchial tone. Fen, which was only tested in preparations where tone was induced with carbachol, also caused complete relaxation. However, Phe was a partial agonist in all preparations tested. When relaxation responses to these amines were calculated as a % of their maximal effects, comparison of EC50 values showed that the order of potency was Iso greater than Ad = Fen greater than NA greater than Phe (92:27:25:1:0.2) in preparations with carbachol-induced tone and Iso greater than Ad greater than NA greater than Phe (112:38:1:0.3) in preparations with spontaneous tone. pA2 values determined for the beta-adrenoceptor antagonists propranolol (non-selective), atenolol (beta-selective) and ICI-118, 551 (beta 2-selective), using Iso as an agonist were, 9.3, 5.3 and 9.1 respectively. These results indicate that beta 2-adrenoceptors mediate relaxation of human isolated bronchus to sympathomimetic amines in preparations obtained 4-14 h post-mortem from non-diseased lung. alpha-Adrenoceptors were apparently sparse or absent in this tissue.
（±）-异丙肾上腺素（Iso）、（-）-肾上腺素（Ad）、（-）-去甲肾上腺素（NA）、（±）-去氧肾上腺素（Phe）以及β2选择性肾上腺素能受体激动剂（±）-非诺特罗（Fen）可引起人离体支气管标本浓度依赖性舒张。Iso、Ad和NA可使自发性和卡巴胆碱诱导的支气管张力完全舒张。仅在卡巴胆碱诱导张力的标本中测试的Fen也可引起完全舒张。然而，Phe在所有测试标本中均为部分激动剂。当将这些胺类的舒张反应计算为其最大效应的百分比时，比较半数有效浓度（EC50）值显示，在卡巴胆碱诱导张力的标本中，效价顺序为Iso＞Ad = Fen＞NA＞Phe（92:27:25:1:0.2），在自发性张力的标本中为Iso＞Ad＞NA＞Phe（112:38:1:0.3）。以Iso为激动剂测定的β肾上腺素能受体拮抗剂普萘洛尔（非选择性）、阿替洛尔（β选择性）和ICI-118,551（β2选择性）的pA2值分别为9.3、5.3和9.1。这些结果表明，β2肾上腺素能受体介导人离体支气管对拟交感胺类的舒张作用，该标本取自非病变肺脏，死后4 - 14小时获得。α肾上腺素能受体在该组织中明显稀少或不存在。
