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- Dana Ferraris, Bridget Duvall, Yao-Sen Ko, Ajit G Thomas, Camilo Rojas, Pavel Majer, Kenji Hashimoto, and Takashi Tsukamoto.
- MGI Pharma, Inc.
- J. Med. Chem. 2008 Jun 26; 51 (12): 3357-9.
AbstractD-amino acid oxidase (DAAO) catalyzes the oxidation of D-amino acids including d-serine, a full agonist at the glycine site of the NMDA receptor. A series of benzo[ d]isoxazol-3-ol derivatives were synthesized and evaluated as DAAO inhibitors. Among them, 5-chloro-benzo[ d]isoxazol-3-ol (CBIO) potently inhibited DAAO with an IC50 in the submicromolar range. Oral administration of CBIO in conjunction with d-serine enhanced the plasma and brain levels of d-serine in rats compared to the oral administration of d-serine alone.
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