Collins R C
Neurology. 1980 Jun;30(6):575-81. doi: 10.1212/wnl.30.6.575.
Muscimol is a potent agonist at GABA-inhibitory synapses in mammalian brain. Given systemically at 7 mumol per kilogram, it blocks topical penicillin seizures and delays the onset of generalized metrazol convulsions in rats. It has no effect against generalized seizures caused by picrotoxin or strychnine. Higher doses of muscimol cause bradykinesia, ataxia, catatonic posturing, and slowing of the electroencephalogram. When applied topically to cortex, muscimol blocks focal penicillin, bicuculline, and picrotoxin discharges in a dose-response relationship. It has no effect against topical strychnine. Muscimol offers a potential new approach to the treatment of epilepsy.
蝇蕈醇是哺乳动物大脑中γ-氨基丁酸(GABA)抑制性突触的强效激动剂。以每千克7微摩尔的剂量全身给药时,它能阻断局部应用青霉素引起的癫痫发作,并延迟大鼠全身性戊四氮惊厥的发作。它对印防己毒素或士的宁引起的全身性惊厥无效。更高剂量的蝇蕈醇会导致运动迟缓、共济失调、紧张性姿势和脑电图减慢。当局部应用于皮层时,蝇蕈醇以剂量反应关系阻断局部青霉素、荷包牡丹碱和印防己毒素的放电。它对局部应用士的宁无效。蝇蕈醇为癫痫治疗提供了一种潜在的新方法。