Turski L, Schwarz M, Turski W A, Ikonomidou C, Sontag K H
Eur J Pharmacol. 1984 Aug 3;103(1-2):99-105. doi: 10.1016/0014-2999(84)90194-8.
The effect of aminophylline on the muscle relaxant action of both diazepam and phenobarbitone was studied in genetically spastic rats of the Han-Wistar strain which exhibit spontaneous tonic activity in the electromyogram of the gastrocnemius-soleus muscle. Both diazepam (0.8 and 4.0 mg/kg i.p.) and phenobarbitone (20 and 30 mg/kg i.p.) reduced the spontaneous activity measured in the electromyogram in a dose-related manner. Aminophylline (50 mg/kg i.p.), a methylxanthine with potent antagonistic activity of adenosine-mediated inhibition, partially reversed the muscle relaxant action of diazepam (4 mg/kg) but not that produced by phenobarbitone. The muscle relaxant effect of phenobarbitone (30 mg/kg) was antagonised by beta-carboline-3-carboxylic acid methylester (beta-CCM), 2 mg/kg i.p. The reversal of the muscle relaxant effect of phenobarbitone produced by beta-CCM was abolished by CGS 8216 (2-phenylpyrazolo-(4,3c)quinolin-3(5H)-one), 5 mg/kg i.p. Aminophylline altered neither the muscle relaxant effect of a low dose of diazepam (0.8 mg/kg) nor the reversal of the muscle relaxant effect of phenobarbitone produced by beta-CCM. These findings indicate that the interaction between diazepam and aminophylline does not involve competition for the benzodiazepine receptor and add further support to the suggestion that purinergic mechanisms may be engaged in the muscle relaxant action of diazepam.
在汉 - 威斯塔大鼠品系的遗传性痉挛大鼠中，研究了氨茶碱对安定和苯巴比妥肌肉松弛作用的影响。该品系大鼠在腓肠肌 - 比目鱼肌肌电图中表现出自发性强直活动。安定（腹腔注射0.8和4.0毫克/千克）和苯巴比妥（腹腔注射20和30毫克/千克）均以剂量相关的方式降低了肌电图中测得的自发活动。氨茶碱（腹腔注射50毫克/千克）是一种具有腺苷介导抑制作用的强效拮抗活性的甲基黄嘌呤，它部分逆转了安定（4毫克/千克）的肌肉松弛作用，但对苯巴比妥产生的肌肉松弛作用没有逆转。苯巴比妥（30毫克/千克）的肌肉松弛作用被β - 咔啉 - 3 - 羧酸甲酯（β - CCM，腹腔注射2毫克/千克）拮抗。CGS 8216（2 - 苯基吡唑并 - (4,3 - c)喹啉 - 3(5H) - 酮，腹腔注射5毫克/千克）消除了β - CCM对苯巴比妥肌肉松弛作用的逆转。氨茶碱既不改变低剂量安定（0.8毫克/千克）的肌肉松弛作用，也不改变β - CCM对苯巴比妥肌肉松弛作用的逆转。这些发现表明，安定与氨茶碱之间的相互作用不涉及对苯二氮䓬受体的竞争，并进一步支持了嘌呤能机制可能参与安定肌肉松弛作用的观点。
