Aldehyde dehydrogenase 2 (ALDH2) is a mitochondrial enzyme involved in the major oxidative pathway of alcohol metabolism. CVT-10216 is a reversible inhibitor of ALDH2 (IC50 = 29 nM) that demonstrates >40-fold selectivity for ALDH2 over the cytosolic isoform, ALDH1. CVT-10216 has been reported to reduce excessive alcohol drinking in alcohol-preferring rats and to prevent self-administration of alcohol in Long-Evans rats. This compound has also been shown to produce anxiolytic effects in four different rodent models, including a model of repeated alcohol withdrawal-induced anxiety. The efficacy of CVT-10216 has also been examined in rodent models of drug addiction or binge eating of high-fat or high-sugar diets.
