Butabindide is a potent inhibitor of cholecystokinin-inactivating peptidase/tripeptidyl peptidase 2 (CCK-inactivating peptidase/TPP-2; Ki = 7 nM). It is selective for CCK-inactivating peptidase/TPP-2 over a panel of serine proteases (Kis = >1 μM) as well as CCK receptors (Kis = >0.1 mM). Butabindide (0.1-100 μM) increases levels of CCK octapeptide (Item Nos. 24404 | 23371) in depolarized rat cerebral cortex slices. In vivo, butabindide inhibits CCK-inactivating peptidase/TPP-2 in mouse liver and brain (ID50s = 1.1 and 6.8 mg/kg, respectively). It also enhances CCK octapeptide-induced delay in gastric emptying and reduces food intake in mice.
