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左旋多巴对麻醉猫外周肌肉的影响。

Peripheral muscle effects of levodopa in the anesthetized cat.

作者信息

Bowman W C, Nott M W

出版信息

Clin Exp Pharmacol Physiol. 1978 Jul-Aug;5(4):305-12. doi: 10.1111/j.1440-1681.1978.tb00679.x.

Abstract
  1. Levodopa, dopamine, noraderanaline and adrenaline (in increasing order of potency) depressed the tension and degree of fusion of incomplete tetanic contractions of the slow-contracting soleus muscle in chloralose-anaesthetized cats. 2. The effects of all compounds were antagonized by propranolol (50-20 microgram/kg), but not practolol (1.0-5.0 mg/kg). This indicates that effects are mediated by beta2-adrenoceptor stimulation. 3. The effect of levodopa, but not of the catecholamines, was antagonized by prior administration of the dopa decarboxylase inhibitior benserazide. This indicates that levodopa itself is inactive, whereas its decarbodylated metabolites are active. 4. The depressant action of beta-adrenoceptor agonists on incomplete tetanic contractions of the cat soleus muscle, which are exerted directly on the muscle fibres, is a model for effects exerted on slow-contracting units of human muscles; the latter effects probably underlie the tremor observed after beta-adrenoceptor agonist administration. 5. These results therefore suggest that levodopa, via its decarboxylated metabolites, dopamine, noradrenaline and adrenaline, may produce or exacerabate tremor in man. Thus in Parkinsonian patients any centrally induced relief of tremor that levodopa may produce may be masked by tremorogenic effects of such metabolites exerted in the periphery.
摘要
  1. 左旋多巴、多巴胺、去甲肾上腺素和肾上腺素(作用强度依次增加)可降低水合氯醛麻醉猫的慢收缩比目鱼肌不完全强直收缩的张力和融合程度。2. 所有化合物的作用均被普萘洛尔(50 - 20微克/千克)拮抗,但不被醋丁洛尔(1.0 - 5.0毫克/千克)拮抗。这表明其作用是由β2 - 肾上腺素能受体刺激介导的。3. 预先给予多巴脱羧酶抑制剂苄丝肼可拮抗左旋多巴的作用,但不能拮抗儿茶酚胺的作用。这表明左旋多巴本身无活性,而其脱羧代谢产物有活性。4. β - 肾上腺素能受体激动剂对猫比目鱼肌不完全强直收缩的抑制作用直接作用于肌纤维,是对人类肌肉慢收缩单位作用的一个模型;后者的作用可能是β - 肾上腺素能受体激动剂给药后观察到的震颤的基础。5. 因此,这些结果表明左旋多巴可能通过其脱羧代谢产物多巴胺、去甲肾上腺素和肾上腺素在人体产生或加重震颤。因此,在帕金森病患者中,左旋多巴可能产生的任何中枢性震颤缓解可能会被这些代谢产物在外周产生的致震颤作用所掩盖。

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