cj-042794 and Pain

cj-042794 has been researched along with Pain* in 3 studies

Other Studies

3 other study(ies) available for cj-042794 and Pain

ArticleYear
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.
    Bioorganic & medicinal chemistry letters, 2010, Jun-15, Volume: 20, Issue:12

    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.
    Journal of medicinal chemistry, 2010, Mar-11, Volume: 53, Issue:5

    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.
    European journal of pharmacology, 2008, Feb-02, Volume: 580, Issue:1-2

    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