Antiarthritic activity in CII-induced DBA/1J mouse arthritic model assessed as decrease in chronic inflammation at 50 mg/kg, ip measured 10 days post second CII booster by Hematoxylin and eosin staining relative to CII-treated control
Antiarthritic activity in CII-induced DBA/1J mouse arthritic model assessed as decrease in abcess formation at 50 mg/kg, ip measured 10 days post second CII booster by Hematoxylin and eosin staining relative to CII-treated control
Antiarthritic activity in CII-induced DBA/1J mouse arthritic model assessed as decrease in fibrosis at 50 mg/kg, ip measured 10 days post second CII booster by Hematoxylin and eosin staining relative to CII-treated control
Antiarthritic activity in CII-induced DBA/1J mouse arthritic model assessed as decrease in periarticular erosion at 50 mg/kg, ip measured 10 days post second CII booster by Hematoxylin and eosin staining relative to CII-treated control
Downregulation of COX-2 expression in ankle tissue of CII-induced DBA/1J mouse arthritic model at 25 to 50 mg/kg, ip measured 10 days post second CII booster by immunoblot analysis
Downregulation of iNOS expression in ankle tissue of CII-induced DBA/1J mouse arthritic model at 25 to 50 mg/kg, ip measured 10 days post second CII booster by immunoblot analysis
Competitive antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromide uptake at 0.1 to 1 uM after 2 hrs by fluorescence assay in presence of BzATP
Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromide uptake after 2 hrs by fluorescence assay
Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA
Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release at 1 uM preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA relative to control
Antagonist activity at recombinant mouse P2X1 receptor overexpressed in Xenopus oocytes assessed as inhibition of ATP-induced ion current at 10 uM preincubated for 20 mins followed by ATP induction by two-electrode voltage clamping method relative to control
Antagonist activity at recombinant human P2X3 receptor overexpressed in Xenopus oocytes assessed as inhibition of ATP-induced ion current at 10 uM preincubated for 20 mins followed by ATP induction by two-electrode voltage clamping method relative to control
Antagonist activity at P2X7 receptor in neuropathic rat dorsal horn assessed as inhibition of long term potentiation-induced neropathic pain at 20 uM relative to control