scholarly journals Pharmacologic Characterization of Omidenepag Isopropyl, a Novel Selective EP2 Receptor Agonist, as an Ocular Hypotensive Agent

2018 ◽  
Vol 59 (1) ◽  
pp. 145 ◽  
Author(s):  
Tomoko Kirihara ◽  
Takazumi Taniguchi ◽  
Kenzo Yamamura ◽  
Ryo Iwamura ◽  
Kenji Yoneda ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Hypotensive Agent ◽  
Ep2 Receptor

Synthesis and pharmacological characterization of a new benzoxazole derivative as a potent 5-HT 3 receptor agonist

2003 ◽  
Vol 11 (13) ◽  
pp. 2709-2714 ◽  
Author(s):  
Pedro Luis López-Tudanca ◽  
Luis Labeaga ◽  
Ana Innerárity ◽  
Luisa Alonso-Cires ◽  
Inés Tapia ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Pharmacological Characterization

Pharmacological Characterization of PD151832, an M1 Muscarinic Receptor Agonist

1997 ◽  
pp. 311-315
Author(s):  
Roy D. Schwarz ◽  
Michael J. Callahan ◽  
Robert E. Davis ◽  
Mark R. Emmerling ◽  
Juan C. Jaen ◽  
...  
Keyword(s):  
Muscarinic Receptor ◽  
Receptor Agonist ◽  
Pharmacological Characterization ◽  
M1 Muscarinic

scholarly journals Effects of selective EP2 receptor agonist, omidenepag, on trabecular meshwork cells, Schlemm’s canal endothelial cells and ciliary muscle contraction

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Natsuko Nakamura ◽  
Megumi Honjo ◽  
Reiko Yamagishi ◽  
Nozomi Igarashi ◽  
Rei Sakata ◽  
...  
Keyword(s):  
Trabecular Meshwork ◽  
Receptor Agonist ◽  
Ciliary Muscle ◽  
Cell Permeability ◽  
Schlemm’S Canal ◽  
Schlemm's Canal ◽  
Ep2 Receptor ◽  
Mlc Phosphorylation ◽  
Related Proteins ◽  
Outflow Pathway

AbstractThis study investigated the effects of omidenepag (OMD), a novel selective EP2 receptor agonist, on human trabecular meshwork (HTM) cells, monkey Schlemm’s canal endothelial (SCE) cells, and porcine ciliary muscle (CM) to clarify the mechanism of intraocular pressure (IOP) reduction involving conventional outflow pathway. In HTM and SCE cells, the effects of OMD on transforming growth factor-β2 (TGF-β2)-induced changes were examined. The expression of actin cytoskeleton and extracellular matrix (ECM) proteins, myosin light chain (MLC) phosphorylation in HTM cells were evaluated using real-time quantitative PCR, immunocytochemistry, and western blotting. The expression of barrier-related proteins, ZO-1 and β-catenin, and permeability of SCE cells were evaluated using immunocytochemistry and transendothelial electrical resistance. The CM contraction was determined by contractibility assay. OMD significantly inhibited expression of TGF-β2 induced mRNA, protein, and MLC-phosphorylation on cytoskeletal and ECM remodeling in the HTM dose dependently. In SCE cells, OMD suppressed TGF-β2-induced expression of the barrier-related proteins and decreased SCE monolayer permeability. OMD at 3 µM significantly inhibited CM contraction, however, the effect was not significant at lower concentrations. IOP lowering effect of OMD through conventional outflow pathway is exerted by increasing outflow facilities with the modulation of TM cell fibrosis and SCE cell permeability.

Functional characterization of basolateral and luminal dopamine receptors in rabbit CCD

2001 ◽  
Vol 281 (1) ◽  
pp. F114-F122 ◽  
Author(s):  
Osamu Saito ◽  
Yasuhiro Ando ◽  
Eiji Kusano ◽  
Yasushi Asano
Keyword(s):  
Receptor Agonist ◽  
Collecting Duct ◽  
Functional Characterization ◽  
Receptor Subtypes ◽  
Cortical Collecting Duct ◽  
Basolateral Side ◽  
Skf 81297 ◽  
Transepithelial Voltage ◽  
Specific Antagonist

Previous studies reported the existence of both D1- and D2-like receptors in the cortical collecting duct (CCD). However, especially with regard to natriuresis, it remains controversial. In the present study, rabbit CCD was perfused to characterize the receptor subtypes responsible for the tubular actions. Basolateral dopamine (DA) induced a dose-dependent depolarization of transepithelial voltage. Basolateral domperidone, a D2-like receptor antagonist, abolished depolarization, whereas SKF-81297, a D1-like receptor agonist, showed no significant change. In addition, bromocriptine, a D2-like receptor agonist, also caused depolarization, whereas SKF-81297, a D1-like receptor agonist, did not depolarize significantly. Moreover, RBI-257, a D4-specific antagonist, reversed the basolateral DA-induced depolarization. In contrast to the basolateral side, luminal DA caused depolarization via a D1-like receptor; however the change was less than that for basolateral DA. For further evaluation, 22Na+ flux ( J Na) was measured to confirm the effect of DA on Na+ transport. Basolateral DA also caused a suppression of J Na, and this reaction was abolished by domperidone. These results suggested that the basolateral D2-like receptor is mainly responsible for the natriuretic action of DA in rabbit CCD.

W1390 Characterization of a Novel, Potent, and Selective Small Molecule Motilin Receptor Agonist, RQ-00201894

2010 ◽  
Vol 138 (5) ◽  
pp. S-713 ◽  
Author(s):  
Nobuyuki Takahashi ◽  
Naomi Koba ◽  
Toshinori Yamamoto ◽  
Masaki Sudo
Keyword(s):  
Small Molecule ◽  
Receptor Agonist ◽  
Motilin Receptor
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