A cell-permeable thienopyrrole compound that potently inhibits the cellular activity of transfected D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) in CHO cells (IC50 against human and rat DAO = 145 and 114 nM, respectively), while exhibiting no activity towards D-aspartate oxidase (DDO; IC50 >5 µM), P450 enzymes CYP3A4/2D6/3C9 (IC50 >10 µM), and a panel of over 150 other enzymes, receptors, and ion channels. Although in vivo treatment of Compound 8 (200 mg/kg, i.p.) is shown to effectively inhibit DAO activity in rat brain and kidney (by 96% and 80%, respectively), the resulting D-serine concentration increase in the periphery and central nervous system appears to be far from sufficient to produce adequate antipsychotic and cognitive enhancing effects.
Packaging
Packaged under inert gas
Warning
Toxicity: Harmful (C)
Reconstitution
Unstable in solution; reconstitute just prior to use.
Other Notes
Smith, S.M., et al. 2009. J. Pharmacol. Exp. Ther.328, 921. Sparey, T., et al. 2008. Bioorg. Med. Chem. Lett.18, 3386.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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