合成的谷氨酸结构类似物- β -羟基-l-谷氨酸的生物作用。

K Watanabe, M Onozuka, M Niwa, A Pongchaidecha
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引用次数: 0

摘要

1. 采用电压钳法、电生理法和结合法研究了l -谷氨酸(Glu)的合成类似物- β -羟基- l -谷氨酸(BHGA)的生物活性。2. 将BHGA作用于电压箝制的蜗牛神经元,可引起向内电流,该电流可被无Na(+)生理盐水阻断,而不被Co(2+)取代的无Ca(2+)生理盐水阻断。3.这种反应表现出比谷氨酸强10倍的效力,并且不被dl -2-氨基-5-磷酸戊酸或犬尿酸完全阻断。4. 脑室内注射BHGA引起大鼠脑皮质电图(ECoG)爆发放电,其模式与谷氨酸引起的放电相似,但与NMDA、准质酸或kainic酸引起的ECoG电荷有很大不同。5. 使用特异性放射性配体的受体结合试验表明,BHGA与Glu受体的结合亲和力与其他激动剂不同。
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Biological actions of beta-hydroxy-l-glutamic acid, a synthesized structural analogue of glutamic acid.

1. Biological actions of beta-hydroxy-L-glutamic acid (BHGA), a synthesized analog of L-glutamic acid (Glu), were examined using voltage-clamp, electrophysiological and binding assay techniques. 2. Application of BHGA to the voltage-clamped snail neurons elicited an inward current which was blocked by Na(+)-free saline but not by Co(2+)-substituted Ca(2+)-free saline in the voltage-clamped snail neurons. 3. This response exhibited a potency about 10 times stronger than Glu, and was not completely blocked by DL-2-amino-5-phosphonovaleric acid or kynurenic acid. 4. Intraventricular injection of BHGA caused burst discharges in the electrocorticograph (ECoG) of rats whose pattern was similar to that elicited by Glu, but quite different from the ECoG charges induced by NMDA, quisqualic acid, or kainic acid. 5. Receptor binding assays using specific radioactive ligands showed that the binding affinity of BHGA to the Glu receptor was different from that of other agonists tested.

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