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Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Molecular Cloning and Characterization of the Human Prostanoid DP Receptor (*)
- Y. Boie, N. Sawyer, D. Slipetz, K. Metters, M. Abramovitz
- BiologyThe Journal of Biological Chemistry
- 11 August 1995
The cloned and expressed a functional cDNA for the hDP receptor showed the highest degree of identity with the hIP and hEP2 receptors, followed by the hEP4 receptor and the rank order of affinities for prostaglandins and prostaglandsin analogs was as predicted for the DP receptor.
Prostaglandin receptor EP(4) mediates the bone anabolic effects of PGE(2).
The pharmacological evidence presented here provides strong support for the hypothesis that the bone anabolic effect of PGE(2) in rats is mediated by the EP(4) receptor.
Cloning and expression of a cDNA for the human prostanoid FP receptor.
NEW CLASS OF POTENT LIGANDS FOR THE HUMAN PERIPHERAL CANNABINOID RECEPTOR
Cloning and expression of a cDNA for the human prostanoid IP receptor.
A cDNA clone coding for a functional human prostanoid IP receptor that is functionally coupled to a signaling pathway involving stimulation of intracellular cAMP production is cloned and expressed.
Prostaglandin Receptor EP4 Mediates the Bone Anabolic Effects of PGE2
The pharmacological evidence presented here provides strong support for the hypothesis that the bone anabolic effect of PGE2 in rats is mediated by the EP4 receptor, and the ability of EP4A, an EP4-selective ligand, to act as an antagonist.
Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).
Rat bile duct cannulation studies revealed that high concentrations of parent drug were present in the biliary fluid, which was circumvented by replacing the 7-methylsulfone substituent present in 6 and 7 with a fluorine atom resulting in antagonists with diminished propensity for biliary excretion and with superior pharmacokinetic profiles.
Structure activity relationships of tetrahydrocannabinol analogues on human cannabinoid receptors