bms453 and Pain

bms453 has been researched along with Pain* in 1 studies

Other Studies

1 other study(ies) available for bms453 and Pain

ArticleYear
Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design.
    Bioorganic & medicinal chemistry letters, 2016, 07-15, Volume: 26, Issue:14

    A series of triaryl pyrazoles were identified as potent pan antagonists for the retinoic acid receptors (RARs) α, β and γ. X-ray crystallography and structure-based drug design were used to improve selectivity for RARγ by targeting residue differences in the ligand binding pockets of these receptors. This resulted in the discovery of novel antagonists which maintained RARγ potency but were greater than 500-fold selective versus RARα and RARβ. The potent and selective RARγ antagonist LY2955303 demonstrated good pharmacokinetic properties and was efficacious in the MIA model of osteoarthritis-like joint pain. This compound demonstrated an improved margin to RARα-mediated adverse effects.

    Topics: Dose-Response Relationship, Drug; Drug Design; Humans; Models, Molecular; Molecular Structure; Osteoarthritis; Pain; Piperazines; Pyrazoles; Receptors, Retinoic Acid; Retinoic Acid Receptor gamma; Structure-Activity Relationship

2016