Prostaglandin DP receptors positively coupled to adenylyl cyclase in embryonic bovine tracheal (EBTr) cells: pharmacological characterization using agonists and antagonists

Various prostaglandin agonists representing various classes of receptor subtypes were evaluated for their ability to stimulate adenylyl cyclase via the endogenous DP receptor in embryonic bovine tracheal (EBTr) cells. Two antagonists were used to block the agonist‐induced cyclic AMP production. ZK11...

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Veröffentlicht in:	British journal of pharmacology 1999-05, Vol.127 (1), p.204-210
Hauptverfasser:	Crider, J Y, Griffin, B W, Sharif, N A
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Monophosphate - biosynthesis adenylyl cyclase Adenylyl Cyclase Inhibitors Adenylyl Cyclases - metabolism AH6809 Animals Biological and medical sciences BW245C BWA868C Cattle Cell receptors Cell structures and functions Cells, Cultured cyclic AMP Cyclic AMP - metabolism DP receptor EBTr cells Embryo, Mammalian Enzyme Inhibitors - pharmacology Fundamental and applied biological sciences. Psychology Hormone receptors. Growth factor receptors. Cytokine receptors. Prostaglandin receptors Hydantoins - pharmacology Molecular and cellular biology Prostaglandin Prostaglandin Antagonists - pharmacology Prostaglandin D2 - metabolism Receptors, Immunologic Receptors, Prostaglandin - agonists Receptors, Prostaglandin - antagonists & inhibitors Receptors, Prostaglandin - metabolism RS93520 Stimulation, Chemical Trachea - cytology Trachea - drug effects Trachea - enzymology Trachea - metabolism Xanthenes - pharmacology Xanthones ZK118182
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Zusammenfassung:	Various prostaglandin agonists representing various classes of receptor subtypes were evaluated for their ability to stimulate adenylyl cyclase via the endogenous DP receptor in embryonic bovine tracheal (EBTr) cells. Two antagonists were used to block the agonist‐induced cyclic AMP production. ZK118182 (EC50=16±4 nM), RS‐93520 (EC50=23±4 nM), SQ27986 (EC50=33±9 nM), ZK110841 (EC50=33±5 nM), BW245C (EC50=59±19 nM) and PGD2 (EC50=101±10 nM) (n=4–70) were the most potent agonists. Whilst most compounds were full agonists (Emax=100% relative to PGD2), BW245C was significantly more efficacious than PGD2 (Emax=121±3%; P
ISSN:	0007-1188 1476-5381
DOI:	10.1038/sj.bjp.0702490