Hicks T P, Jang E K
Neurosci Lett. 1985 Jun 24;57(3):295-9. doi: 10.1016/0304-3940(85)90508-7.
The 8-carbon chain analogue of gamma-aminobutyric acid (GABA), omega-aminocaprylic acid (omega-AC), was administered to single cortical neurones of rat by microiontophoresis and its effect on cell firing compared to the effect elicited by GABA. The spontaneous and glutamate-elicited firing rates of all cells examined were decreased by omega-AC, the molecule having an apparent potency approximately one-fifth that of GABA. Inhibitions induced by omega-AC were antagonized by bicuculline and enhanced by flurazepam. These data favour the view that extending chain length per se of the GABA molecule decreases the inhibitory potency of postsynaptic GABA receptor agonists. The results do not support the view that such structural changes alter the mode of action of GABA analogues, from inhibition to excitation, as has been suggested previously.
将γ-氨基丁酸（GABA）的8碳链类似物ω-氨基辛酸（ω-AC）通过微量离子电泳法施用于大鼠的单个皮层神经元，并将其对细胞放电的影响与GABA引起的影响进行比较。所检测的所有细胞的自发放电率和谷氨酸诱发的放电率均因ω-AC而降低，该分子的表观效力约为GABA的五分之一。ω-AC诱导的抑制作用被荷包牡丹碱拮抗，被氟西泮增强。这些数据支持这样一种观点，即GABA分子本身链长的延长会降低突触后GABA受体激动剂的抑制效力。结果不支持先前有人提出的这种结构变化会改变GABA类似物的作用方式，从抑制变为兴奋的观点。
