Johansson L H, Persson H, Rosengren E
Acta Pharmacol Toxicol (Copenh). 1984 May;54(5):346-51. doi: 10.1111/j.1600-0773.1984.tb01941.x.
We tried to find functional evidence for the existence of beta 1- and beta 2-adrenoceptors in the isolated guinea-pig lung parenchymal strip preparation, using potent and selective beta 1- and beta 2-adrenoceptor stimulation. To obtain potent beta 1-adrenoceptor stimulation the nonselective beta-adrenoceptor agonist isoprenaline was combined with a highly selective beta 2-adrenoceptor antagonist--ICI 118,551. Potent beta 2-adrenoceptor stimulation was obtained by procaterol. Practolol (beta 1-adrenoceptor antagonist) and ICI 118,551 were used as antagonists. ICI 118,551, 10(-7) mol/l, shifted the concentration response (C/R) curve of isoprenaline to a higher concentration range. The C/R curve of procaterol was shifted in the same way and to the same degree by this concentration of ICI 118,551. The C/R curve of isoprenaline was not further shifted after blockade with a combination of ICI 118,551, 10(-7) mol/l, and practolol, 10(-6). However, in the trachea preparation, a tissue containing both beta 1- and beta 2-adrenoceptors, there was a further shift of the C/R curve of isoprenaline to a higher concentration range after blockade with a combination of ICI 118,551 and practolol in the concentrations given above. In this preparation the shift of the C/R curve of procaterol was ten times greater than that of isoprenaline after blockade with ICI 118,551, 10(-7) mol/l. We conclude that it is possible to characterize small fractions of beta 1-adrenoceptors coexisting with beta 2-adrenoceptors with the technique used. Furthermore there is still no functional evidence of the existence of beta 1-adrenoceptors in the lung parenchyma.
我们试图通过强效且选择性的β1和β2肾上腺素能受体刺激,在分离的豚鼠肺实质条制备物中寻找β1和β2肾上腺素能受体存在的功能证据。为了获得强效的β1肾上腺素能受体刺激,将非选择性β肾上腺素能受体激动剂异丙肾上腺素与高选择性β2肾上腺素能受体拮抗剂——ICI 118,551联合使用。通过丙卡特罗获得强效的β2肾上腺素能受体刺激。心得宁(β1肾上腺素能受体拮抗剂)和ICI 118,551用作拮抗剂。10(-7)mol/L的ICI 118,551将异丙肾上腺素的浓度-反应(C/R)曲线移至更高浓度范围。该浓度的ICI 118,551以相同方式且相同程度移动了丙卡特罗的C/R曲线。在用10(-7)mol/L的ICI 118,551和10(-6)的心得宁联合阻断后,异丙肾上腺素的C/R曲线未进一步移动。然而,在气管制备物中,一种同时含有β1和β2肾上腺素能受体的组织,在用上述浓度的ICI 118,551和心得宁联合阻断后,异丙肾上腺素的C/R曲线进一步移至更高浓度范围。在该制备物中,在用10(-7)mol/L的ICI 118,551阻断后,丙卡特罗的C/R曲线的移动比异丙肾上腺素的移动大十倍。我们得出结论,用所使用的技术可以表征与β2肾上腺素能受体共存的一小部分β1肾上腺素能受体。此外,在肺实质中仍然没有β1肾上腺素能受体存在的功能证据。