Kawajiri S, Kojima H, Akashi A
Nihon Yakurigaku Zasshi. 1984 Mar;83(3):263-8.
Muscle relaxant effects of baclofen were compared with those of dantrolene, diazepam, chlordiazepoxide and tolperisone. When administered intraduodenally (i.d.), baclofen and dantrolene but not diazepam suppressed the sustained rigidity of forelimbs in anemically decerebrated rats, and ED50 values of the former two drugs were 2.9 and 22 mg/kg, respectively. Baclofen, dantrolene and diazepam reduced the phasic rigidity of the decerebrated animals induced by mechanical stimulation of hindlimbs, with their respective ED50 values of 6.2, 140 and 1.4 mg/kg, i.d. Both the rigidities were almost insensitive to chlordiazepoxide and tolperisone. With the exception of tolperisone, these drugs also produced a muscle relaxation in intact animals as measured by traction (rats), rotarod (mice), and grip-strength (mice) tests. ED50 or eD25 values were calculated to be in the following ranges: 5.6 approximately 12 mg/kg, p.o. for baclofen, 15 approximately 35 mg/kg, p.o. for dantrolene, 2.1 approximately 6.5 mg/kg, p.o. for diazepam and 33 approximately 64 mg/kg, p.o. for chlordiazepoxide. These results suggest that baclofen, unlike other drugs, may be effective in reducing both tonic and phasic rigidities at lower doses than those causing muscle relaxation in intact animals.
将巴氯芬的肌肉松弛作用与丹曲林、地西泮、氯氮卓和托哌酮的作用进行了比较。十二指肠内给药时,巴氯芬和丹曲林可抑制贫血去大脑大鼠前肢的持续性强直,但地西泮无此作用,前两种药物的半数有效量(ED50)分别为2.9和22mg/kg。巴氯芬、丹曲林和地西泮可降低后肢机械刺激诱导的去大脑动物的相位性强直,十二指肠内给药时它们各自的ED50值分别为6.2、140和1.4mg/kg。两种强直对氯氮卓和托哌酮几乎均不敏感。除托哌酮外,通过牵引(大鼠)、转棒(小鼠)和握力(小鼠)试验测定,这些药物在完整动物中也产生肌肉松弛作用。计算得出的ED50或ED25值在以下范围内:巴氯芬口服为5.6至12mg/kg,丹曲林口服为15至35mg/kg,地西泮口服为2.1至6.5mg/kg,氯氮卓口服为33至64mg/kg。这些结果表明,与其他药物不同,巴氯芬可能在低于导致完整动物肌肉松弛的剂量时,对降低强直性和相位性强直均有效。