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猪离体支气管中β-肾上腺素能受体的分类

Classification of beta-adrenoceptors in isolated bronchus of the pig.

作者信息

Goldie R G, Paterson J W, Wale J L

出版信息

Br J Pharmacol. 1983 May;79(1):177-80. doi: 10.1111/j.1476-5381.1983.tb10510.x.

Abstract

1 (+/-)-Isoprenaline (Iso), (-)-adrenaline (Ad), (-)-noradrenaline (NA), the beta 2-selective adrenoceptor agonist (+/-)-fenoterol (Fen) and the beta 1-selective adrenoceptor agonist (+/-)-RO363 caused concentration-dependent relaxation of preparations of pig bronchus pre-contracted with carbachol 40-ng/ml (0.22 microM). Iso, Ad, NA and Fen caused complete relaxation of carbachol-induced tone, but RO363 caused relaxation equivalent to only 59% of the maximal response to Iso. 2 When relaxation responses to these amines were plotted as a % of their maximal effects, comparison of EC50 values showed that the order of potency was RO363 greater than Iso greater than NA greater than Fen greater than Ad (14.4:4.6:1:0.4:0.3). 3 pA2 values determined for the beta-adrenoceptor antagonists propranolol (non-selective) and atenolol (beta 1-selective), or the partial agonist salbutamol (beta 2-selective) using Iso as agonist were 8.3, 7.3 and 4.4 respectively. The pA2 value for atenolol using RO363 as the agonist was 7.6. 4 These results indicate that porcine bronchus contains a homogeneous population of beta 1-adrenoceptors.

摘要
  1. (±)-异丙肾上腺素(Iso)、(-)-肾上腺素(Ad)、(-)-去甲肾上腺素(NA)、β2 选择性肾上腺素能受体激动剂(±)-非诺特罗(Fen)以及β1 选择性肾上腺素能受体激动剂(±)-RO363 可使预先用 40 ng/ml(0.22 μM)卡巴胆碱预收缩的猪支气管制剂产生浓度依赖性舒张。Iso、Ad、NA 和 Fen 可使卡巴胆碱诱导的张力完全舒张,但 RO363 引起的舒张仅相当于对 Iso 最大反应的 59%。2. 当将这些胺类的舒张反应绘制为其最大效应的百分比时,对半数有效浓度(EC50)值的比较表明,效价顺序为 RO363 > Iso > NA > Fen > Ad(14.4:4.6:1:0.4:0.3)。3. 以 Iso 作为激动剂时,测定β肾上腺素能受体拮抗剂普萘洛尔(非选择性)、阿替洛尔(β1 选择性)或部分激动剂沙丁胺醇(β2 选择性)的 pA2 值分别为 8.3、7.3 和 4.4。以 RO363 作为激动剂时,阿替洛尔的 pA2 值为 7.6。4. 这些结果表明猪支气管含有均一的β1 肾上腺素能受体群体。

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1
Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.
2
Catecholamine transport in isolated lung parenchyma of pig.猪离体肺实质中的儿茶酚胺转运
Br J Pharmacol. 1982 Aug;76(4):507-13. doi: 10.1111/j.1476-5381.1982.tb09247.x.

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