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特布他林对豚鼠比目鱼肌β-肾上腺素能受体的脱敏作用:与功能变化相关的生化改变

Desensitization by terbutaline of beta-adrenoceptors in the guinea-pig soleus muscle: biochemical alterations associated with functional changes.

作者信息

Buur T, Clausen T, Holmberg E, Johansson U, Waldeck B

出版信息

Br J Pharmacol. 1982 Jun;76(2):313-7. doi: 10.1111/j.1476-5381.1982.tb09222.x.

Abstract

1 The effects of adrenaline and terbutaline on cyclic adenosine 3',5'-monophosphate (cyclic AMP) content, 22Na-efflux, 42K-influx and subtetanic contractions have been assessed in soleus muscles isolated from guniea-pigs which had been maintained on food with or without terbutaline for 5 days. 2 Terbutaline and adrenaline increased cyclic AMP content and suppressed subtetanic contractions, and regression analysis indicates a statistically significant correlation between these two effects (P less than 0.01). 3 In muscles obtained from terbutaline-treated animals, the effects of terbutaline and adrenaline on cyclic AMP content, active Na-K-transport and subtetanic contractions were all considerably suppressed, but insulin stimulated 22Na-efflux and affected subtetanic contractions to the same extent as in the muscles obtained from the control group. 4 The results suggest that terbutaline treatment leads to a reduction in the number of beta 2-adrenoceptors in skeletal muscle or an impairment of their function. 5 The results provide further support for the idea that the effect of adrenaline or insulin on skeletal muscle contractions is the outcome of stimulation of active Na-K-transport.

摘要
  1. 已经在从豚鼠分离出的比目鱼肌中评估了肾上腺素和特布他林对环磷酸腺苷(cAMP)含量、22Na外流、42K内流和不完全强直收缩的影响。这些豚鼠分别以含或不含特布他林的食物喂养5天。

  2. 特布他林和肾上腺素增加了cAMP含量并抑制了不完全强直收缩,回归分析表明这两种效应之间存在统计学上的显著相关性(P<0.01)。

  3. 在从接受特布他林治疗的动物获得的肌肉中,特布他林和肾上腺素对cAMP含量、活性钠钾转运和不完全强直收缩的作用均受到显著抑制,但胰岛素刺激22Na外流并对不完全强直收缩产生的影响与从对照组获得的肌肉相同。

  4. 结果表明,特布他林治疗导致骨骼肌中β2肾上腺素能受体数量减少或其功能受损。

  5. 这些结果进一步支持了以下观点,即肾上腺素或胰岛素对骨骼肌收缩的作用是刺激活性钠钾转运的结果。

相似文献

7
An in vitro method for the study of beta-receptor mediated effects on slow contracting skeletal muscle.
J Pharm Pharmacol. 1976 May;28(5):434-6. doi: 10.1111/j.2042-7158.1976.tb04649.x.
8
Steric aspects of agonism and antagonism at beta-adrenoceptors: experiments with the enantiomers of terbutaline and pindolol.
Acta Pharmacol Toxicol (Copenh). 1984 Apr;54(4):285-91. doi: 10.1111/j.1600-0773.1984.tb01932.x.

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