scholarly journals LY3127760, a Selective Prostaglandin E4 (EP4) Receptor Antagonist, and Celecoxib: A Comparison of Pharmacological Profiles

2017 ◽  
Vol 11 (1) ◽  
pp. 46-53 ◽  
Author(s):  
Yan Jin ◽  
Claire Smith ◽  
Leijun Hu ◽  
David E. Coutant ◽  
Kelly Whitehurst ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Ep4 Receptor ◽  
Ep4 Receptor Antagonist ◽  
Pharmacological Profiles

Discovery of AAT-008, a novel, potent, and selective prostaglandin EP4 receptor antagonist

2017 ◽  
Vol 27 (5) ◽  
pp. 1186-1192 ◽  
Author(s):  
Yoshiyuki Okumura ◽  
Tatsuya Yamagishi ◽  
Seiji Nukui ◽  
Kazunari Nakao
Keyword(s):  
Receptor Antagonist ◽  
Ep4 Receptor ◽  
Ep4 Receptor Antagonist

Effects of selective prostaglandin EP4 receptor antagonist on osteoclast formation and bone resorption in vitro

Bone ◽  
2002 ◽  
Vol 30 (1) ◽  
pp. 159-163 ◽  
Author(s):  
M Tomita ◽  
X Li ◽  
Y Okada ◽  
F.N Woodiel ◽  
R.N Young ◽  
...  
Keyword(s):  
Bone Resorption ◽  
Receptor Antagonist ◽  
Osteoclast Formation ◽  
Ep4 Receptor ◽  
Ep4 Receptor Antagonist

Synthesis of a Prostaglandin EP4 Receptor Antagonist

Synfacts ◽  
2010 ◽  
Vol 2010 (09) ◽  
pp. 0981-0981
Author(s):  
D. Gauvreau ◽  
S. Dolman ◽  
G. Hughes ◽  
P. O’Shea ◽  
I. Davies
Keyword(s):  
Receptor Antagonist ◽  
Ep4 Receptor ◽  
Ep4 Receptor Antagonist

Effect of prostanoid EP4 receptor antagonist, CJ-042,794, in rat models of pain and inflammation

2008 ◽  
Vol 580 (1-2) ◽  
pp. 116-121 ◽  
Author(s):  
Akio Murase ◽  
Takako Okumura ◽  
Ayano Sakakibara ◽  
Hiroko Tonai-Kachi ◽  
Kazunari Nakao ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Rat Models ◽  
Ep4 Receptor ◽  
Ep4 Receptor Antagonist

In vitro pharmacological characterization of CJ-042794, a novel, potent, and selective prostaglandin EP4 receptor antagonist

Life Sciences ◽  
2008 ◽  
Vol 82 (3-4) ◽  
pp. 226-232 ◽  
Author(s):  
Akio Murase ◽  
Yasuhito Taniguchi ◽  
Hiroko Tonai-Kachi ◽  
Kazunari Nakao ◽  
Junji Takada
Keyword(s):  
Receptor Antagonist ◽  
Pharmacological Characterization ◽  
Ep4 Receptor ◽  
Ep4 Receptor Antagonist

Activation of EP4 receptors contributes to prostaglandin E2-mediated stimulation of renal sensory nerves

2004 ◽  
Vol 287 (6) ◽  
pp. F1269-F1282 ◽  
Author(s):  
Ulla C. Kopp ◽  
Michael Z. Cicha ◽  
Kazuhiro Nakamura ◽  
Rolf M. Nüsing ◽  
Lori A. Smith ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Sensory Nerve ◽  
Nerve Fibers ◽  
Prostaglandin E ◽  
Ep4 Receptor ◽  
Pelvic Wall ◽  
Ep4 Receptor Antagonist ◽  
Cox 2 ◽  
Ep3 Receptor ◽  
Stimulation Of

Induction of cyclooxygenase-2 (COX-2) in the renal pelvic wall increases prostaglandin E2 (PGE2) leading to stimulation of cAMP production, which results in substance P (SP) release and activation of renal mechanosensory nerves. The subtype of PGE receptors involved, EP2 and/or EP4, was studied by immunohistochemistry and renal pelvic administration of agonists and antagonists of EP2 and EP4 receptors. EP4 receptor-like immunoreactivity (LI) was colocalized with calcitonin gene-related peptide (CGRP)-LI in dorsal root ganglia (DRGs) at Th9-L1 and in nerve terminals in the renal pelvic wall. Th9-L1 DRG neurons also contained EP3 receptor-LI and COX-2-LI, each of which was colocalized with CGRP-LI in some neurons. No renal pelvic nerves contained EP3 receptor-LI and only very few nerves COX-2-LI. The EP1/EP2 receptor antagonist AH-6809 (20 μM) had no effect on SP release produced by PGE2 (0.14 μM) from an isolated rat renal pelvic wall preparation. However, the EP4 receptor antagonist L-161,982 (10 μM) blocked the SP release produced by the EP2/EP4 receptor agonist butaprost (10 μM) 12 ± 2 vs. 2 ± 1 and PGE2, 9 ± 1 vs. 1 ± 0 pg/min. The SP release by butaprost and PGE2 was similarly blocked by the EP4 receptor antagonist AH-23848 (30 μM). In anesthetized rats, the afferent renal nerve activity (ARNA) responses to butaprost 700 ± 100 and PGE2·780 ± 100%·s (area under the curve of ARNA vs. time) were unaffected by renal pelvic perfusion with AH-6809. However, 1 μM L-161,982 and 10 μM AH-23848 blocked the ARNA responses to butaprost by 94 ± 5 and 78 ± 10%, respectively, and to PGE2 by 74 ± 16 and 74 ± 11%, respectively. L-161,982 also blocked the ARNA response to increasing renal pelvic pressure 10 mmHg, 85 ± 5%. In conclusion, PGE2 increases renal pelvic release of SP and ARNA by activating EP4 receptors on renal sensory nerve fibers.

scholarly journals The pharmacological effect of BGC20-1531, a novel prostanoid EP4 receptor antagonist, in the Prostaglandin E2 human model of headache

2011 ◽  
Vol 12 (5) ◽  
pp. 551-559 ◽  
Author(s):  
Maria Antonova ◽  
Troels Wienecke ◽  
Karen Maubach ◽  
Emma Thomas ◽  
Jes Olesen ◽  
...  
Keyword(s):  
Prostaglandin E2 ◽  
Receptor Antagonist ◽  
Pharmacological Effect ◽  
Human Model ◽  
Ep4 Receptor ◽  
Ep4 Receptor Antagonist
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