General description

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

50 mg in Glass bottle

Reconstitution

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.

Warning

Toxicity: Irritant (B)