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体外β受体介导对快速收缩骨骼肌作用的分析。

Analysis of the beta-receptor mediated effect on fast-contracting skeletal muscle in vitro.

作者信息

Holmberg E, Waldeck B

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1977 Dec;301(2):109-13. doi: 10.1007/BF00501424.

Abstract

Subtetanic contractions of the isolated extensor digitorum longus (EDL) of the guinea-pig, a fast-contracting muscle, were evoked by transmural field stimulation. Isoprenaline, adrenaline, terbutaline, and noradrenaline each caused a dose-dependent increase in the force of contraction, their potencies decreasing in that order. Tyramine was without effect in this respect. Curare depressed the contractions of EDL by about 20% but did not appreciably change the response to the beta-adrenoceptor agonists. The effects of isoprenaline and noradrenaline were blocked by propranolol (unselective) and H 35/25 (1-(p-tolyl)-2-isopropylamino-1-propanol, beta2-selective) but not by practolol (beta1-selective). Moreover, the increase in the force of subtetanic contractions of EDL produced by noradrenaline was unaffected by phentolamine. It is concluded that the adrenoceptor mediating the increase in the force of contraction of the isolated EDL is of the beta2-type and that the site of action is direct on the muscle. Its similarity to the receptor mediating the inverse effect on the slow-contracting soleus-muscle is pointed out.

摘要

通过跨壁场刺激诱发豚鼠离体趾长伸肌(EDL,一种快速收缩肌肉)的不完全强直收缩。异丙肾上腺素、肾上腺素、特布他林和去甲肾上腺素均引起收缩力呈剂量依赖性增加,其效力按此顺序降低。酪胺在这方面没有作用。筒箭毒碱使EDL的收缩降低约20%,但并未明显改变对β-肾上腺素能受体激动剂的反应。异丙肾上腺素和去甲肾上腺素的作用被普萘洛尔(非选择性)和H 35/25(1-(对甲苯基)-2-异丙氨基-1-丙醇,β2选择性)阻断,但未被普拉洛尔(β1选择性)阻断。此外,去甲肾上腺素引起的EDL不完全强直收缩力增加不受酚妥拉明影响。结论是,介导离体EDL收缩力增加的肾上腺素能受体为β2型,作用部位直接在肌肉上。文中指出了它与介导对慢收缩比目鱼肌产生相反作用的受体的相似性。

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