83731-80-0Relevant academic research and scientific papers
Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activity
Yau, Mei-Kwan,Liu, Ligong,Lim, Junxian,Lohman, Rink-Jan,Cotterell, Adam J.,Suen, Jacky Y.,Vesey, David A.,Reid, Robert C.,Fairlie, David P.
, p. 986 - 991 (2016/06/28)
Activation of protease activated receptor 2 (PAR2) has been implicated in inflammatory and metabolic disorders and its inhibition may yield novel therapeutics. Here, we report a series of PAR2 antagonists based on C-terminal capping of 5-isoxazolyl-l-cyclohexylalanine-l-isoleucine, with benzylamine analogues being effective new PAR2 antagonists. 5-Isoxazolyl-l-cyclohexylalanine-l-isoleucine-2-methoxybenzylamine (10) inhibited PAR2-, but not PAR1-, induced release of Ca2+(IC500.5 μM) in human colon cells, IL-6 and TNFα secretion (IC501-5 μM) from human kidney cells, and was anti-inflammatory in acute rat paw inflammation (ED505 mg/kg sc). These findings show that new benzylamide antagonists of PAR2 have anti-inflammatory activity.
