普萘洛尔对大鼠眼外肌的箭毒样作用。
Curare-like effect of propranolol on rat extraocular muscles.
作者信息
Chiarandini D J
出版信息
Br J Pharmacol. 1980 May;69(1):13-9. doi: 10.1111/j.1476-5381.1980.tb10877.x.
Abstract
1 The effects were studied of the beta-adrenoceptor blocking drug, (+/-)-propranolol and its (+)- and (-)-isomers on contractility of rat isolated diaphragm and inferior rectus muscles. 2 Propranolol (10(-5) M) did not modify the resting tension nor the electrically-induced twitch contraction in diaphragm and extraocular muscles, nor the tonic tension evoked in the latter by high K concentrations. 3 In inferior rectus preparations (+/-)-propranolol (5 x 10(-6) M) reduced significantly tensions evoked by succinylcholine (SCh). Cumulative dose-response curves to SCh were shifted to the right in a nearly parallel manner by (+)- and (-)-propranolol which were about equiactive. 4 It is concluded that the depressant action of propranolol is independent of its adrenoceptor blocking potency and it is not due to an alteration of the contraction mechanism. Propranolol appears to depress SCh-evoked tensions through a curare-like effect on cholinoceptors.
摘要
- 研究了β-肾上腺素能受体阻断药（±）-普萘洛尔及其（+）-和（-）-异构体对大鼠离体膈肌和下直肌收缩性的影响。2. 普萘洛尔（10⁻⁵ M）不改变膈肌和眼外肌的静息张力以及电诱发的抽搐收缩，也不改变高钾浓度在后者诱发的强直张力。3. 在下直肌标本中，（±）-普萘洛尔（5×10⁻⁶ M）显著降低了琥珀酰胆碱（SCh）诱发的张力。（+）-和（-）-普萘洛尔对SCh的累积剂量-反应曲线以几乎平行的方式右移，二者活性相当。4. 得出结论，普萘洛尔的抑制作用与其肾上腺素能受体阻断效力无关，也不是由于收缩机制的改变。普萘洛尔似乎通过对胆碱能受体的箭毒样作用来降低SCh诱发的张力。
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