Butabindide is a potent inhibitor of cholecystokinin-inactivating peptidase/tripeptidyl peptidase 2 (CCK-inactivating peptidase/TPP-2; K = 7 nM). It is selective for CCK-inactivating peptidase/TPP-2 over a panel of serine proteases (Ks = >1 μM) as well as CCK receptors (Ks = >0.1 mM). Butabindide (0.1-100 μM) increases levels of CCK octapeptide in depolarized rat cerebral cortex slices. In vivo, butabindide inhibits CCK-inactivating peptidase/TPP-2 in mouse liver and brain (IDs = 1.1 and 6.8 mg/kg, respectively). It also enhances CCK octapeptide-induced delay in gastric emptying and reduces food intake in mice.
Butabindide (oxalate) is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide (oxalate) inhibits TPP II to protect CCK-8 against inactivation.
IC50&Target
IC50: 7 nM (TPP II) and 10 μM (TPP I)
体外研究
Butabindide (UCL-1397; 0-24 nM; membranes of rat cerebral cortex) oxalate inhibits TPP II activity in the meninges.
体内研究
Butabindide (UCL-1397; 10 mg/kg; intravenous injection; Oxalate inhibits the breakdown of CCK-8 in the gastrointestinal tract for 20 minutes and increases satiety in mice.
Animal Model:
Mice (25-30 g)
Dosage:
10 mg/kg
Administration:
Intravenous injection; for 20 minutes
Result:
Reduces food intake and elicits other behavioral concomitants of satiation.