Table 8.

Binding affinity (K_i) and signaling efficiency (EC₅₀) of prostanoids and agonists on the recombinant FP receptors expressed in cell cultures and in various tissues

	Ki (nM)
Receptor	PGE2	PGF2a	PGD2	fluprostenol	Iloprost	U46619	bimatoprost	Reference
hFP/HEK293a	119 ± 12	3.2 ± 0.3	6.7 ± 0.5	-	11 ± 1	241 ± 8	-	Abramovitz et al. 2000
mFP/CHOa	100	3	47	-	-	1000	-	Narumiya et al. 1999, Wheeldon and Vardey 1993
hFP/COS-M6b	85	2.8	7.0	3.5	1200	146	-	Abramovitz et al. 1994
bFP/corpus leuteumc	110	10	17	-	-	-	-	Anderson et al. 1999
hFP-altFP4 dimer	-	100	-	-	-	-	-	Liang et al. 2008a
bFP/corpus leuteuma	3400 ± 710	130 ± 6	2500 ± 760	98 ± 9	-	-	6310 ± 1650	Sharif et al. 2003
	EC50 (nM)
Receptor	PGE2	PGF2a	PGD2	fluprostenol	Iloprost	U46619	bimatoprost	Reference
hFP/HEK293a	-	10 ± 1.7	-	-	-	-	-	Kunapuli et al. 1997
rFP/rat myocytesa	-	50 ± 12	-	-	-	-	-	Kunapuli et al. 1998
hFP/COS7b	-	60.0	-	-	-	-	-	Neuschäfer-Rube et al. 2003
hFP/HEK293c	-	11.2	-	-	-	-	-	Woodward et al. 2000
rFP/A7r5a	2607 ± 270	30.90 ± 2.82	222.0 ± 71.4	4.45 ± 0.19	NA	5900 ± 1230	-	Griffin et al. 1998
hFP/HEK293c	-	-	-	-	-	-	4762	Woodward et al. 2003
mFP/Swiss 3T3a	-	-	-	4	-	-	-	Sharif et al. 2000b
rFP/hepatocytes	-	1000	-	50	-	-	-	Meisdalen et al. 2007
hFP/HEK293	-	29 ± 2	-	4.6 ± 0.4	-	-	168 ± 165	Sharif et al. 2003

Abbreviations: h, human; HEK293, human embryonic kidney cells; COS7, monkey fibroblast-like cells; CHO. Chinese hamster ovary cells; A7r5, rat aorta cells; Swiss 3T3, Swiss albino mouse embryo tissue cells. The K_i values were determined from [³H]PGF_2α displacement assays. The EC₅₀ determined from intracellular changes in [IP₃] or [Ca²⁺]. a) IC₅₀ estimated from a graph of agonist vs. [³H]PGF_2α and the K_i value calculated using Cheng-Prusoff equation (Suganami et al. 2016); b) K_i value calculated from reported IC₅₀ for displacement of using Cheng-Prusoff equation; c) EC₅₀ determined from change in [IP₃].