The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs

Stable cell lines that individually express the eight known human prostanoi d receptors (EP1, EP2, EP3, EP4, DP, FP, IP and TP) have been established u sing human embryonic kidney (HEK) 293(EBNA) cells. These recombinant cell l ines have been employed in radioligand binding assays to determine the equi librium inhibitor constants of known prostanoid receptor ligands at these e ight 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 understan ding of prostanoid receptor biology. (C) 2000 Elsevier Science B.V. All rig hts reserved.