Nicholson G M, Spence I, Johnston G A
Neuropharmacology. 1985 Jun;24(6):461-4. doi: 10.1016/0028-3908(85)90049-8.
The effect of depressant/convulsant pair of glutarimides on the isolated spinal cord of the immature rat was examined using extracellular recording. At concentrations of 300 microM the depressant beta-butyl-beta-methyl glutarimide enhanced the response of motoneurones and dorsal root fibres to gamma-aminobutyric acid (GABA) while the convulsant bemegride (beta-ethyl-beta-methyl glutarimide) decreased both responses to GABA. At this concentration both the convulsant and depressant reduced mono- and polysynaptic reflex activity. Neither the convulsant or depressant had prominent direct actions, with only a small hyperpolarization being produced by both glutarimides on dorsal root fibres. The overall depressant or convulsant properties of these glutarimides may be due in part therefore to a differential effect on the postsynaptic action of the inhibitory transmitter GABA. Furthermore, the depressant glutarimide reduced the excitatory effects of L-glutamate and the convulsant reduced the inhibitory effects of glycine on spinal neurones; thus, actions on these transmitters may also contribute to the overall effects of these glutarimides.
使用细胞外记录法研究了戊二酰亚胺类抑制/惊厥剂对未成熟大鼠离体脊髓的作用。在300微摩尔浓度下，抑制性的β-丁基-β-甲基戊二酰亚胺增强了运动神经元和背根纤维对γ-氨基丁酸（GABA）的反应，而惊厥剂贝美格（β-乙基-β-甲基戊二酰亚胺）则降低了对GABA的两种反应。在此浓度下，惊厥剂和抑制剂均降低了单突触和多突触反射活动。惊厥剂和抑制剂均无明显的直接作用，两种戊二酰亚胺仅对背根纤维产生微小的超极化作用。因此，这些戊二酰亚胺的总体抑制或惊厥特性可能部分归因于对抑制性递质GABA突触后作用的不同影响。此外，抑制性戊二酰亚胺降低了L-谷氨酸的兴奋作用，惊厥剂降低了甘氨酸对脊髓神经元的抑制作用；因此，对这些递质的作用也可能有助于这些戊二酰亚胺的总体作用。
