SIGNAL TRANSDUCTION AND PHARMACOLOGICAL CHARACTERISTICS OF A METABOTROPIC GLUTAMATE RECEPTOR, MGLUR1, IN TRANSFECTED CHO CELLS
SIGNAL TRANSDUCTION AND PHARMACOLOGICAL CHARACTERISTICS OF A METABOTROPIC GLUTAMATE RECEPTOR, MGLUR1, IN TRANSFECTED CHO CELLS
复制标题
DOI：
10.1016/0896-6273(92)90096-v
复制
发表时间：
1992-04-01
期刊：
影响因子：
16.2
通讯作者：
NAKANISHI, S
中科院分区：
文献类型：
--
作者：
ARAMORI, I;NAKANISHI, S
代谢型谷氨酸受体mGluR 1的信号转导和药理学特性进行了研究，在CHO细胞永久表达克隆受体。mGluR 1刺激磷脂酰肌醇（PI）水解的效力等级顺序为使君子酸> L-谷氨酸大于或等于鹅膏蕈氨酸> L-同型半胱氨酸亚磺酸大于或等于反式-ACPD。该受体还引起cAMP形成和花生四烯酸释放的刺激，具有可比的激动剂效力。DL-AP 3和L-AP 4是脑切片中谷氨酸刺激PI水解的有效拮抗剂，对mGluR 1没有明显影响，表明存在该受体家族的其他亚型。百日咳毒素和佛波酯对3个转导级联产生不同的影响，这意味着mGluR 1可能通过不同的G蛋白独立地连接到多个转导通路。
The signal transduction and pharmacological properties of a metabotropic glutamate receptor, mGluR1, were studied in CHO cells permanently expressing the cloned receptor. mGluR1 stimulated phosphatidylinositol (PI) hydrolysis in the potency rank order of quisqualate > L-glutamate greater-than-or-equal-to ibotenate > L-homocysteine sulfinate greater-than-or-equal-to trans-ACPD. This receptor also evoked the stimulation of cAMP formation and arachidonic acid release with comparable agonist potencies. DL-AP3 and L-AP4, the effective antagonists reported for glutamate-stimulated PI hydrolysis in brain slices, showed no appreciable effects on mGluR1, suggesting the existence of an additional subtype of this receptor family. Pertussis toxin and phorbol ester produced distinct effects on the three transduction cascades, implying that mGluR1 independently links to the multiple transduction pathways probably through different G proteins.