別名

D-Amino Acid Oxidase Inhibitor - CAS 39793-31-2 - Calbiochem,4H-Thieno[3,2-b]pyrrole-5-carboxylic acid, D-AAO Inhibitor, Compound 8

一般描述

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.

重懸

Unstable in solution; reconstitute just prior to use.

其他說明

Smith, S.M., et al. 2009. J. Pharmacol. Exp. Ther.328, 921.
Sparey, T., et al. 2008. Bioorg. Med. Chem. Lett.18, 3386.