D-Amino Acid Oxidase Inhibitor II, CBIO

A cell-permeable benzisoxazolone compound that potently inhibits D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) activity (IC₅₀ = 90 and 150/188 nM 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 (30 mg/kg, p.o.) markedly prolongs the half-life of orally administered D-serine (30 mg/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 (ED₅₀ =60 ng) or after (ED₅₀ = 170 ng) subcutaneous formalin injection (50 µl 5% solution) greatly alleviates formalin-induced late phase tonic pain (E_max =67%), but not early phase acute nociception in rats in vivo.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

It is recommended to prepare a stock solution for 6 month use each time and store the unreconstituted material in solid form, protected from moisture and preferably under inert gas, for best long-term stability during storage.

Gong, N., et al. 2011. J. Pharmacol. Exp. Ther.336, 282.
Ferraris, D., et al. 2008. J. Med. Chem.51, 3357.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Irritant (B)