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Vol. 281, Issue 2, 845-854, 1997
Molecular Pharmacology Unit, Alcon Laboratories, Inc., Fort Worth,
Texas
A detailed pharmacological characterization of the prostaglandin (PG)
receptor coupled to phosphoinositide (PI) turnover and intracellular
calcium mobilization in Swiss 3T3 mouse fibroblast cells was
undertaken. The pharmacological profile of this functional receptor was
compared with the pharmacological profile of specific [3H]PGF2
binding to bovine
corpus luteum membranes, which are known to contain a bona
fide FP receptor. PGs that were potent stimulators and full
agonists in the PI turnover assay in the 3T3 cells were the following
(for all, n = 3-45):
16-phenoxy-PGF2 (EC50 = 0.61 ± 0.1 nM), cloprostenol (EC50 = 0.73 ± 0.04 nM), 17-phenyl-PGF2 (EC50 = 2.71 ± 0.35 nM), fluprostenol (EC50 = 3.67 ± 0.61 nM), PhXA85 (EC50 = 27.3 ± 5.63 nM) and
PGF2 (EC50 = 28.5 ± 5.26 nM). However, PGD2 (EC50 = 155 ± 29.9 nM; Emax = 49% of cloprostenol),
PGE2 (EC50 = 2570 ± 566 nM;
Emax = 59%) and U46619 (EC50 = 1060 ± 310 nM; Emax = 63%) were less potent and were partial agonists, and iloprost and BW245C were inactive. Although the PGs tested exhibited lower affinities in the
[3H]PGF2 binding assay than
their functional potencies in the PI turnover assay, the rank orders of
potencies and affinities were well correlated (r = 0.94; n = 15 compounds). However, the PI turnover
assay was more sensitive than the calcium mobilization assay for rank
ordering PG agonists. In conclusion, the Swiss 3T3 cells express an FP
receptor coupled to PI turnover and intracellular Ca++
mobilization signal transduction pathways. The pharmacological profile
of this receptor was similar to that of the FP receptor found in the
bovine corpus luteum, a tissue previously used to clone the first
pharmacologically defined FP receptor.
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