Ro 61-8048

Ro 61-8048 is a **potent and selective kynurenine 3-monooxygenase (KMO) inhibitor** developed by **Roche**. It competitively inhibits KMO with Ki = 4.8 nM and IC50 = 37 nM, preventing conversion of L-kynurenine to 3-hydroxy-L-kynurenine. The compound increases kynurenic acid levels to concentrations that antagonize the glycine site of NMDA receptors. It is **blood-brain barrier permeable** and exhibits **antidystonic, anticonvulsant, and neuroprotective activities**. Structural studies reveal it binds in an **allosteric manner** by occupying a unique tunnel structure near the substrate-binding pocket. Preclinical studies demonstrated efficacy in models of dystonia, neuropathic pain, nicotine/cocaine addiction, inflammation-induced hypotension, and intracerebral hemorrhage.

Other names

3,4-Dimethoxy-N-[4-(3-nitrophenyl)-2-thiazolyl]benzenesulfonamide