The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs
The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs
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DOI：
10.1016/s1388-1981(99)00164-x
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发表时间：
2000-01-17
影响因子：
4.8
通讯作者：
Metters, KM
中科院分区：
文献类型：
--
作者：
Abramovitz, M;Adam, M;Metters, KM
已经使用人胚肾（HEK）293（EBNA）细胞建立了单独表达八种已知的人前列腺素类受体（EP 1、EP 2、EP 3、EP 4、DP、FP、IP和TP）的稳定细胞系。这些重组细胞系已被用于放射性配体结合试验，以确定已知的前列腺素受体配体在这八个受体的平衡抑制剂常数。这使得，第一次，在个人的人前列腺素受体的亲和力和选择性的几种新的化合物的评估。这些信息应有助于解释药理学研究，采用这些配体作为工具来研究人体组织和细胞系，因此，应导致前列腺素受体生物学的更好的理解。(C)2000 Elsevier Science B.V.保留所有权利。
Stable cell lines that individually express the eight known human prostanoid receptors (EP1, EP2, EP3, EP4, DP, FP, IP and TP) have been established using human embryonic kidney (HEK) 293(EBNA) cells. These recombinant cell lines have been employed in radioligand binding assays to determine the equilibrium inhibitor constants of known prostanoid receptor ligands at these eight receptors. This has allowed, for the first time, an assessment of the affinity and selectivity of several novel compounds at the individual human prostanoid receptors. This information should facilitate interpretation of pharmacological studies that employ these ligands as tools to study human tissues and cell lines and should, therefore, result in a greater understanding of prostanoid receptor biology. (C) 2000 Elsevier Science B.V. All rights reserved.