Description

• A cell-permeable benzisoxazolone compound that potently inhibits D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) activity (IC 50 = 90 and 150/188nM against rat spinal cord and porcine kidney DAO, respectively) in a reversible and D-serine-competitive ( K i = 100 nM) manner
• Upon co-administration, CBIO (30mg/kg, p.o.) markedly prolongs the half-life of orally administered D-serine (30mg/kg) in plasma, resulting in enhanced rat brain D-serine level (60% vs
• 25% above basal, respectively, with vs
• without CBIO)
• Direct intrathecal/spinal CBIO injection either before (ED 50 =60 ng) or after (ED 50 = 170 ng) subcutaneous formalin injection (50μl 5% solution) greatly alleviates formalin-induced late phase tonic pain (E max =67%), but not early phase acute nociception in rats in vivo .