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Vol. 286, Issue 1, 411-418, July 1998
Molecular Pharmacology Unit (B.W.G. and N.A.S.) and
Glaucoma
Therapeutic Target Research (P.E.M. and I.-H.P.), Alcon Laboratories,
Inc., Fort Worth, Texas
An FP prostaglandin (PG) receptor on the A7r5 rat aorta smooth muscle
cell line has been characterized by assays of phosphoinositide (PI)
turnover and intracellular calcium mobilization stimulated by
structurally diverse PGs. In the PI turnover assay, cloprostenol was
the most potent PG tested, with a potency (EC50) of
0.84 ± 0.06 nM (mean ± S.E.M., n = 34), and
was a full agonist. Other known FP receptor agonists tested in this
assay had efficacies 
85% of the cloprostenol value and high
potencies: 16-phenoxy PGF2
(2.05 ± 0.19 nM),
17-phenyl PGF2 (2.80 ± 0.59 nM), fluprostenol
(4.45 ± 0.19 nM), PGF2 (30.9 ± 2.82 nM) and PhXA85 (43.5 ± 11.4 nM). Other classes of PGs evaluated
(PGD2, enprostil, 17-phenyl PGE2,
PGE2, sulprostone and U-46619) were less potent and less
efficacious than the FP receptor agonists, or were inactive. For a
large group of standard PGs evaluated in the PI turnover assay, both
potencies and efficacies correlated well with those reported for the FP
receptor of Swiss mouse 3T3 fibroblasts. The potencies of fluprostenol
and PGF2 as stimuli of intracellular calcium
mobilization matched well their potencies in the PI turnover assay, but
fluprostenol had twice the efficacy of PGF2. Both
signaling responses stimulated by fluprostenol were significantly
inhibited by U73122, a selective inhibitor of phosphoinositide turnover
(IC50 = 1.25 ± 0.16 µM for PI turnover), and by
chelation of calcium in the medium. Together with the PI turnover data,
these studies of intracellular calcium mobilization linked to
activation of the FP receptor, provide additional characterization of
the pharmacological properties of this receptor.
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