cj-042794 has been researched along with Pain* in 3 studies
3 other study(ies) available for cj-042794 and Pain
| Article | Year |
|---|---|
Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.
The discovery of a highly potent and selective EP(4) antagonist MF-766 is discussed. This N-benzyl indole derivative exhibits good pharmacokinetic profile and unprecedented in vivo potency in the rat AIA model. Topics: Animals; Arthritis; Benzoates; Cells, Cultured; Dogs; Drug Discovery; Drug Stability; Hepatocytes; Humans; Indoles; Inflammation; Pain; Pharmacokinetics; Rats; Receptors, Prostaglandin E; Receptors, Prostaglandin E, EP4 Subtype; Structure-Activity Relationship | 2010 |
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
The discovery of highly potent and selective second generation EP(4) antagonist MK-2894 (34d) is discussed. This compound exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several animal models of pain/inflammation. It also shows favorable GI tolerability profile in rats when compared to traditional NSAID indomethacin. Topics: Analgesics; Animals; Benzoates; Cyclopropanes; Half-Life; Humans; Magnetic Resonance Spectroscopy; Male; Pain; Prostaglandin Antagonists; Rats; Rats, Sprague-Dawley; Receptors, Prostaglandin E; Structure-Activity Relationship; Thiophenes | 2010 |
Effect of prostanoid EP4 receptor antagonist, CJ-042,794, in rat models of pain and inflammation.
Recent study suggests that the proinflammatory and nociceptive effects of prostaglandin E(2) are mediated by prostanoid receptor subtype EP(4) and prostanoid EP(4) receptor may be a potential target for the treatment of inflammatory pain. Here we describe pharmacological characterization of a novel prostanoid EP(4) receptor antagonist, CJ-042,794 (4-{(1S)-1-[({5-chloro-2-[(4-fluorophenyl) oxy] phenyl} carbonyl) amino] ethyl} benzoic acid) in comparison with piroxicam (non-steroidal anti-inflammatory drug) or rofecoxib (cyclooxygenase-2 inhibitor). CJ-042,794 competitively antagonized cAMP accumulation with a pA(2) value of 8.7 in HEK293 cells overexpressing rat prostanoid EP(4) receptors. Orally administered CJ-042,794 dose-dependently inhibited carrageenan-induced mechanical hyperalgesia with an ED(50) value of 4.7 mg/kg (11 micromol/kg) and its maximal activity was somewhat less effective than that of 10 mg/kg piroxicam (30 micromol/kg p.o.). When CJ-042,794 and rofecoxib were administered to adjuvant-induced arthritis rats on Days 12-22 twice daily, both compounds reversed paw swelling to normal levels. These results suggest that a pharmacological blockade of the prostanoid EP(4) receptor may represent a new therapeutic strategy in signs and symptomatic relief of osteoarthritis and/or rheumatoid arthritis. Topics: Administration, Oral; Analgesics; Animals; Anti-Inflammatory Agents; Benzamides; Benzoates; Cell Line; Cyclic AMP; Disease Models, Animal; Dose-Response Relationship, Drug; In Vitro Techniques; Inflammation; Lactones; Male; Pain; Pain Measurement; Piroxicam; Rats; Rats, Inbred Lew; Receptors, Prostaglandin E; Receptors, Prostaglandin E, EP4 Subtype; Sulfones | 2008 |