Lactams as Prostanoid Receptor Ligands. Part 4. 2-Piperidones as Selective EP4 Receptor Agonists.

ChemInform ◽  
2005 ◽  
Vol 36 (38) ◽  
Author(s):  
Todd R. Elworthy ◽  
Emma R. Brill ◽  
Christopher C. Caires ◽  
Woongki Kim ◽  
Leang K. Lach ◽  
...  
Keyword(s):  
Receptor Ligands ◽  
Prostanoid Receptor ◽  
Receptor Agonists ◽  
Ep4 Receptor

Lactams as prostanoid receptor ligands. Part 4: 2-Piperidones as selective EP4 receptor agonists

2005 ◽  
Vol 15 (10) ◽  
pp. 2523-2526 ◽  
Author(s):  
Todd R. Elworthy ◽  
Emma R. Brill ◽  
Christopher C. Caires ◽  
Woongki Kim ◽  
Leang K. Lach ◽  
...  
Keyword(s):  
Receptor Ligands ◽  
Prostanoid Receptor ◽  
Receptor Agonists ◽  
Ep4 Receptor

scholarly journals N-Phenethyl Substitution in 14-Methoxy-N-methylmorphinan-6-ones Turns Selective µ Opioid Receptor Ligands into Dual µ/δ Opioid Receptor Agonists

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Maria Dumitrascuta ◽  
Marcel Bermudez ◽  
Tanila Ben Haddou ◽  
Elena Guerrieri ◽  
Lea Schläfer ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Ligands ◽  
Receptor Agonists ◽  
Opioid Receptor Ligands ◽  
Δ Opioid Receptor ◽  
Opioid Receptor Agonists

Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats

2006 ◽  
Vol 16 (7) ◽  
pp. 1799-1802 ◽  
Author(s):  
Kimberly O. Cameron ◽  
Bruce A. Lefker ◽  
Margaret Y. Chu-Moyer ◽  
David T. Crawford ◽  
Paul DaSilva Jardine ◽  
...  
Keyword(s):  
Bone Formation ◽  
Bone Mass ◽  
Ovariectomized Rats ◽  
New Bone Formation ◽  
Receptor Agonists ◽  
Ep4 Receptor

A novel series of potent and selective EP4 receptor ligands: Facile modulation of agonism and antagonism

2011 ◽  
Vol 21 (1) ◽  
pp. 484-487 ◽  
Author(s):  
Michael J. Boyd ◽  
Carl Berthelette ◽  
Jean-François Chiasson ◽  
Patsy Clark ◽  
John Colucci ◽  
...  
Keyword(s):  
Receptor Ligands ◽  
Ep4 Receptor

scholarly journals Selective E‐prostanoid receptor agonists mediate phosphorylation of aquaporin‐2 in vitro and ex vivo

2011 ◽  
Vol 25 (S1) ◽  
Author(s):  
Emma Tina Bisgaard Olesen ◽  
Michael R. Rützler ◽  
Robert A. Fenton
Keyword(s):  
Ex Vivo ◽  
Prostanoid Receptor ◽  
Receptor Agonists ◽  
Aquaporin 2

Prostaglandin E2 Receptors as Potential Bone Anabolic Targets – Selective EP4 Receptor Agonists

2012 ◽  
Vol 5 (2) ◽  
pp. 174-181 ◽  
Author(s):  
Joseph Pagkalos ◽  
Andreas Leonidou ◽  
Mohammed As-Sultany ◽  
Manolis Heliotis ◽  
Athanasios Mantalaris ◽  
...  
Keyword(s):  
Prostaglandin E2 ◽  
Receptor Agonists ◽  
Ep4 Receptor

Desensitization of adenylate cyclase responses following exposure to IP prostanoid receptor agonists

1994 ◽  
Vol 47 (6) ◽  
pp. 953-959 ◽  
Author(s):  
Anke Krane ◽  
John MacDermot ◽  
Mary Keen
Keyword(s):  
Adenylate Cyclase ◽  
Prostanoid Receptor ◽  
Receptor Agonists

scholarly journals Regulation of Expression of Renal Organic Anion Transporters OAT1 and OAT3 in a Model of Ischemia/Reperfusion Injury

2015 ◽  
Vol 37 (1) ◽  
pp. 1-13 ◽  
Author(s):  
Christina Preising ◽  
Reinhard Schneider ◽  
Michael Bucher ◽  
Michael Gekle ◽  
Christoph Sauvant
Keyword(s):  
Transcriptional Activity ◽  
Ischemia Reperfusion ◽  
Organic Anion ◽  
Anion Transport ◽  
Receptor Type ◽  
Ischemia And Reperfusion ◽  
Organic Anion Transport ◽  
Prostanoid Receptor ◽  
Promoter Sequences ◽  
Ep4 Receptor

Background: Recently, we gained evidence that impairment of rOat1 and rOat3 expression induced by ischemic acute kidney injury (AKI) is mediated by COX metabolites and this suppression might be critically involved in renal damage. Methods: (i) Basolateral organic anion uptake into proximal tubular cells after model ischemia and reperfusion (I/R) was investigated by fluorescein uptake. The putative promoter sequences from hOAT1 (SLC22A6) and hOAT3 (SCL22A8) were cloned into a reporter plasmid, transfected into HEK cells and (ii) transcriptional activity was determined after model ischemia and reperfusion as a SEAP reporter gen assay. Inhibitors or antagonists were applied with the beginning of reperfusion. Results: By using inhibitors of PKA (H89) and PLC (U73122), antagonists of E prostanoid receptor type 2 (AH6809) and type 4 (L161,982), we gained evidence that I/R induced down regulation of organic anion transport is mediated by COX1 metabolites via E prostanoid receptor type 4. The latter signaling was confirmed by application of butaprost (EP2 agonist) or TCS2510 (EP4 agonist) to control cells. In brief, the latter signaling was verified for the transcriptional activity in the reporter gen assay established. Therein, selective inhibitors for COX1 (SC58125) and COX2 (SC560) were also applied. Conclusion: Our data show (a) that COX1 metabolites are involved in the regulation of renal organic anion transport(ers) after I/R via the EP4 receptor and (b) that this is due to transcriptional regulation of the respective transporters. As the promoter sequences cloned were of human origin and expressed in a human renal epithelial cell line we (c) hypothesize that the regulatory mechanisms described after I/R is meaningful for humans as well.

Vascular Activities of Prostaglandins and Selective Prostanoid Receptor Agonists in Human Retinal Microvessels

2002 ◽  
Vol 75 (2) ◽  
pp. 155-163 ◽  
Author(s):  
Clayton S. Spada ◽  
Amelia L. Nieves ◽  
David F. Woodward
Keyword(s):  
Prostanoid Receptor ◽  
Receptor Agonists
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