Stone W E, Javid M J
Arch Int Pharmacodyn Ther. 1981 Oct;253(2):294-300.
Muscimol (MU) was tested on mice for anticonvulsive action against chemical convulsants. 3-Mercaptopropionic acid (3-MP) was more sensitive to inhibition by MU (1.5 mg/kg) than was either pentylenetretrazol (PTZ) or bicuculline (BIC); picrotoxin (PIC) and kainic acid were not measurably antagonized; aminophylline was potentiated. The profile of action of MU closely resembles that of aminooxyacetic acid (AOAA), except that the latter strongly antagonizes kainic acid. MU distinguished more clearly than did AOAA between the action of 3-MP and that of either PTZ or BIC, inasmuch as the differences between the respective potency ratios were larger with MU than with AOAA. The results are consistent with the view that MU acts as a GABA agonist, that GABA antagonism is not a sufficient basis on which to explain the convulsive action of BIC or PIC, and that the antagonism of AOAA toward seizures induced by kainic acid may not be due to an action on the GABA system.
对小鼠进行了蝇蕈醇(MU)针对化学惊厥剂的抗惊厥作用测试。与戊四氮(PTZ)或荷包牡丹碱(BIC)相比,3-巯基丙酸(3-MP)对MU(1.5毫克/千克)的抑制作用更敏感;苦味毒(PIC)和 kainic 酸未表现出可测量的拮抗作用;氨茶碱的作用得到增强。MU的作用模式与氨氧基乙酸(AOAA)非常相似,只是后者强烈拮抗 kainic 酸。MU比AOAA更能清楚地区分3-MP与PTZ或BIC的作用,因为MU的各自效价比之间的差异比AOAA更大。结果与以下观点一致:MU作为一种γ-氨基丁酸(GABA)激动剂起作用,GABA拮抗作用不是解释BIC或PIC惊厥作用的充分依据,并且AOAA对 kainic 酸诱导的癫痫发作的拮抗作用可能不是由于对GABA系统的作用。