Fukuda H
Nihon Yakurigaku Zasshi. 1979 Sep;75(6):535-42.
Effects of diazepam and baclofen on the anemic decerebrate rigidity in rats were studied by using the drugs that modify GABAergic mechanisms of deplete catecholamine. Rigid forelimb tension in anemic decerebrate rats took the form of tonically sustained tension (tonic component), while the phasic tension (phasic component) was induced by mechanical stimulation of hindlimbs. Diazepam exerted a marked dose-dependent inhibition of the phasic component, whereas baclofen produced a similar effect on both tonic and phasic components. In rats pretreated with semicarbazide, the inhibitory effect of diazepam on phasic component was reduced, and the effect of semicarbazide was antagonized by pyridoxine. The effect of diazepam was slightly enhanced by pretreatment with aminooxyacetic acid, and antagonized by picrotoxin. In contrast to diazepam, the depressant actions of baclofen on both components were not affected by semicarbazide, aminooxyacetic acid or picrotoxin. Catecholamine depletion produced by alpha-methyltyrosine or disulfiram significantly reduced the effect of baclofen on the phasic component. It thus appears that GABA is involved in the effect of diazepam on the phasic component, and noradrenaline is involved in the same effect of baclofen in anemic decerebrate rats.
通过使用改变γ-氨基丁酸(GABA)能机制或耗竭儿茶酚胺的药物,研究了地西泮和巴氯芬对大鼠贫血去大脑强直的影响。贫血去大脑大鼠的前肢强直张力表现为持续性张力(强直成分),而后肢的机械刺激可诱发相位性张力(相位成分)。地西泮对相位成分有明显的剂量依赖性抑制作用,而巴氯芬对强直成分和相位成分均有类似作用。在用氨基脲预处理的大鼠中,地西泮对相位成分的抑制作用减弱,且氨基脲的作用可被吡哆醇拮抗。用氨氧基乙酸预处理可使地西泮的作用略有增强,而可被印防己毒素拮抗。与地西泮不同,巴氯芬对两种成分的抑制作用不受氨基脲、氨氧基乙酸或印防己毒素的影响。由α-甲基酪氨酸或双硫仑引起的儿茶酚胺耗竭显著降低了巴氯芬对相位成分的作用。因此,似乎GABA参与了地西泮对相位成分的作用,而去甲肾上腺素参与了巴氯芬在贫血去大脑大鼠中的相同作用。