CVT-10216 is a Potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50: 29 nM). CVT-10216 also has inhibitory effect of ALDH-1 (IC50: 1.3 μM). CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.

ALDH2:29 nM

CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 that reduces excessive alcohol drinking.?Anxiety plays a role in alcoholism. As reflected in social interaction behavior in four unrelated rodent models: endogenous anxiety-like behavior in na?ve Fawn-Hooded rats, repeated alcohol-withdrawal-induced anxiety, restraint stress-induced anxiety and drug-induced anxiety.?CVT-10216 counteracted anxiety in all models except that produced by the 5-HT(2C) agonist, mCPP.?CVT-10216 exhibited both acute and prophylactic inhibitions of repeated alcohol-withdrawal-induced anxiety.?Importantly, anxiogenic behavior induced by the benzodiazepine receptor inverse agonist, DMCM, was counteracted dose-dependently by CVT-10216.CVT-10216 (intraperitoneal injection; 3.75 or 15 mg/kg) are determined 5 h into the third withdrawal, it has the anxiolytic effect of 15 mg/kg CVT-10216 in this model. ?However it has no significant effects on locomotor activity. CVT-10216 (intraperitoneal injection; 3.75, 7.5, or 15 mg/kg) shows a increase in social interaction as a dose-dependent manner, punctuated by a 2-fold increase in social interaction after 15 mg/kg in Fawn-Hooded rats[1].