Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM. Pentagastrin is a synthetic polypeptide that has effects like gastrin when given parenterally, which can cause the secretion and synthesis of salivary proteins.

Ceruletide is a ten amino acid oligopeptide that stimulates smooth muscle and increases digestive secretions.

Nastorazepide is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.

Loxiglumide is a cholecystokinin (CCK) receptor antagonist.

Gastrin I is an endogenous gastrointestinal peptide hormone that can bind to cholecystokinin (CCK) receptors.

Rebamipide is an inducer of endogenous prostaglandin, an oxygen-derived free radical scavenger, and a cholecystokinin type 1 (CCK1) receptor inhibitor for inhibiting [125I]BH-CCK-8S with IC50 of 37.7 μM.