Odagaki Y, Nishi N, Koyama T
Department of Psychiatry, Hokkaido University School of Medicine, Sapporo, Japan.
Eur J Pharmacol. 1996 Apr 4;300(1-2):151-4. doi: 10.1016/0014-2999(96)00033-7.
Functional activation of GTP-binding (G) proteins coupled with metabotropic glutamate receptors was evaluated in rat brain membranes. L-Glutamate stimulated the high-affinity GTPase activity in cerebral cortical, hippocampal, and striatal membranes with a mean concentration eliciting a half-maximal response (EC50) of 4.8, 1.6, and 4.9 microM, respectively. The enzyme activity in cerebral cortical membranes was also stimulated by (2S, 1'S,2'S)-2-(carboxycyclopropyl)glycine (L-CCG-I) with a mean EC50 of 0.90 microM, but not by L-2-amino-4-phosphonobutyrate (L-AP4) up to 10 microM. This method opens up a strategy for investigation of functional coupling between Group II metabotropic glutamate receptors and G proteins in native brain membranes.
在大鼠脑膜中评估了与促代谢型谷氨酸受体偶联的GTP结合（G）蛋白的功能激活情况。L-谷氨酸刺激大脑皮质、海马和纹状体膜中的高亲和力GTP酶活性，引起半数最大反应（EC50）的平均浓度分别为4.8、1.6和4.9微摩尔。大脑皮质膜中的酶活性也受到（2S，1'S，2'S）-2-（羧基环丙基）甘氨酸（L-CCG-I）的刺激，平均EC50为0.90微摩尔，但高达10微摩尔的L-2-氨基-4-膦酰丁酸（L-AP4）对其没有刺激作用。该方法为研究天然脑膜中II型促代谢型谷氨酸受体与G蛋白之间的功能偶联开辟了一种策略。
