绑定的特征[3 h] cgs 19755:小说n -甲基- d拮抗剂与摩尔老鼠大脑的亲和力。

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墨菲DE,和记AJ伤害SD,威廉姆斯M,马基石

绑定的特征[3 h] cgs 19755:小说n -甲基- d拮抗剂与摩尔老鼠大脑的亲和力。

Br J杂志。1988年11月,95 (3):932 - 8。

PubMed ID

2850065 (在PubMed

]

文摘

1。CGS 19755 (cis-4-phosphonomethyl-2-piperidine羧酸)刚性模拟2-amino-5-phosphonopentanoic酸(AP5),是一种最有效的竞争n -甲基- d (NMDA)拮抗剂。使用Triton-treated原油从老鼠大脑突触膜,绑定的研究表明[3 h] cgs 19755绑定与高亲和力和选择性NMDA-type兴奋性氨基酸受体。2。[3 h] cgs 19755绑定是饱和的,可逆的,heat-labile, pH-dependent与蛋白质浓度和线性。特定的绑定代表总数的80 - 85%。3所示。使用离心试验,饱和实验显示两个不同的绑定组件与Kd值9和200海里,和相应的Bmax值0.55和1.00 pmol mg-1蛋白质。相比之下,一个绑定组件的Kd值24海里,一个明显Bmax价值0.74 pmol mg-1过滤试验观察蛋白质。4所示。 Competition experiments in which both assay techniques were used, showed that [3H]-CGS 19755 selectively labels the NMDA receptor. The most active inhibitors of [3H]-CGS 19755 binding were L-glutamate and CGS 19755 (IC50 values = 100 nM). 5. In the centrifugation assay, a number of excitatory amino acids were found to generate shallow inhibition curves, and computer analysis indicated the presence of two binding components. The quisqualate receptor ligand AMPA (D,L-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate), kainic acid and the non-competitive NMDA antagonists, such as phencyclidine, tiletamine and MK-801, were without activity. 6. The high affinity binding obtained with [3H]-CGS 19755 by use of filtration techniques thus permits the more rapid evaluation of compounds as potential NMDA antagonists and agonists. Therefore, this rigid analogue of AP5 is a more suitable radioligand for NMDA receptors than [3H]-CPP (34-+/-)2-carboxypiperazin-4-yl)propyl-1-phosphonic acid), the corresponding analogue of 2-amino-7-phosphonoheptanoic acid (AP7).

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药物靶点

药物	目标	类	生物	药理作用	行动
谷氨酸	谷氨酸受体ionotropic kainate 5	蛋白质	人类	未知的	不可用	细节