K Takeyama, J Tamaoki, A Chiyotani, N Sakai, T Kanemura, K Konno
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引用次数: 0
摘要
为了确定非典型β -肾上腺素受体(β - 3-肾上腺素受体)激动剂BRL 37344是否刺激气道纤毛运动,如果是,其作用机制是什么,我们在体外研究了兔气管上皮。将培养7 d的上皮细胞置于玫瑰室中,采用光电法测定睫状体搏动频率(CBF)。BRL 37344的加入使CBF从15.5 +/- 0.6 Hz迅速增加到20.3 +/- 1.4 Hz(平均+/- SE, p < 0.01),并持续升高至少20分钟。该效应具有浓度依赖性,较基线值和EC50的最大增幅分别为27.2 +/- 0.4%(平均+/- SE, p < 0.01)和1.75 × 10(-7) M。其他β -肾上腺素能受体激动剂同样增加CBF,效价排序为沙丁胺醇(1)> BRL 37344(0.57) >去甲肾上腺素(1.3 x 10(-3))。心得安预孵育细胞抑制沙丁胺醇产生的CBF增加,BRL 37344显著提高细胞内环AMP含量。这些结果表明,β 3-肾上腺素能受体可能存在于兔气管上皮中,并且这种受体的刺激通过循环amp依赖机制增加纤毛的运动性,这种作用可能对增强气道粘膜纤毛运输功能有价值。
[Stimulation of ciliary motility by beta 3-adrenoceptor agonist rabbit tracheal epithelium].
To determine whether atypical beta-adrenoceptor (beta 3-adrenoceptor) agonist, BRL 37344, stimulates airway ciliary motility and, if so, what its mechanism of action is, we studied rabbit tracheal epithelium in vitro. Epithelial cells cultured for 7 days were mounted in the Rose chamber and ciliary beat frequency (CBF) was measured by a photoelectric method. Addition of BRL 37344 rapidly increased CBF from 15.5 +/- 0.6 to 20.3 +/- 1.4 Hz (mean +/- SE, p < 0.01), which remained elevated for at least 20 min. This effect was concentration-dependent, the maximal increase from the baseline value and the EC50 being 27.2 +/- 0.4% (mean +/- SE, p < 0.01) and 1.75 x 10(-7) M, respectively. Other beta-adrenoceptor agonists likewise increased CBF, where the rank order of potency was salbutamol (1) > BRL 37344 (0.57) >> norepinephrine (1.3 x 10(-3)). Preincubation of cells with propranolol inhibited the increase in CBF produced by salbutamol, and BRL 37344 significantly raised intracellular cyclic AMP contents. These results suggest that beta 3-adrenoceptor probably exists in rabbit tracheal epithelium and that stimulation of this type of receptor increases ciliary motility through a cyclic AMP-dependent mechanism, an effect that might be of value in enhancing mucociliary transport function in the airway.