Henricks P A, Van Esch B, Van Oosterhout A J, Nijkamp F P
Department of Veterinary Pharmacology, State University of Utrecht, The Netherlands.
Eur J Pharmacol. 1988 Aug 2;152(3):321-30. doi: 10.1016/0014-2999(88)90727-3.
The existence of beta-adrenoceptors on guinea pig alveolar macrophage membranes was determined by means of radioligand binding studies. Saturable binding with [125I]cyanopindolol demonstrated 38 +/- 6 fmol binding sites per 10(6) alveolar macrophages with a Kd of 0.85 +/- 0.15 nM. With timolol, atenolol and ICI 118.551 for competition of [125I]cyanopindolol binding it became clear that guinea pig alveolar macrophages possessed adrenergic binding sites of the beta 2-subtype. The cyclic AMP levels of alveolar macrophages could be increased by selective beta 2-adrenoceptor agonists but not by selective beta 1-adrenoceptor agonists. The influence of non-selective beta- and selective beta 1- and beta 2-adrenoceptor agonists on the phagocytic and metabolic responsiveness of alveolar macrophages was also studied. Addition of beta-adrenoceptor agonists had no effect on the uptake of bacteria by alveolar macrophages. Incubation of alveolar macrophages with increasing amounts of non-selective and selective beta 1-agonists resulted in a dose-dependent decrease in the detection of hydrogen peroxide released by alveolar macrophages. This effect was due to the scavenging properties of these drugs. The selective beta 2-receptor agonists, salbutamol and terbutaline, had no effect on the oxidative metabolism of alveolar macrophages. We conclude that guinea pig alveolar macrophages possess beta 2-adrenoceptors on their cell surface and that these receptors are not involved in the phagocytic activity of alveolar macrophages.
通过放射性配体结合研究确定了豚鼠肺泡巨噬细胞膜上β-肾上腺素能受体的存在。用[125I]氰吲哚洛尔进行的饱和结合显示，每10(6)个肺泡巨噬细胞有38±6 fmol的结合位点，解离常数（Kd）为0.85±0.15 nM。用噻吗洛尔、阿替洛尔和ICI 118.551竞争[125I]氰吲哚洛尔的结合，结果表明豚鼠肺泡巨噬细胞具有β2-亚型的肾上腺素能结合位点。选择性β2-肾上腺素能受体激动剂可增加肺泡巨噬细胞的环磷酸腺苷水平，而选择性β1-肾上腺素能受体激动剂则无此作用。还研究了非选择性β-、选择性β1-和β2-肾上腺素能受体激动剂对肺泡巨噬细胞吞噬和代谢反应性的影响。添加β-肾上腺素能受体激动剂对肺泡巨噬细胞摄取细菌没有影响。用越来越多的非选择性和选择性β1-激动剂孵育肺泡巨噬细胞，导致肺泡巨噬细胞释放的过氧化氢检测量呈剂量依赖性下降。这种作用是由于这些药物的清除特性。选择性β2-受体激动剂沙丁胺醇和特布他林对肺泡巨噬细胞的氧化代谢没有影响。我们得出结论，豚鼠肺泡巨噬细胞在其细胞表面具有β2-肾上腺素能受体，并且这些受体不参与肺泡巨噬细胞的吞噬活性。
