119295-94-2

A 65186 is a Type A Cholecystokinin (CCK) receptor antagonist. Cholecystokinin (CCK) is a peptide hormone which is found both in the gastrointestinal tract throughout the human small intestine and in the enteric and central nervous system. It has a potential therapeutic role as an appetite suppressor.

A-65186 is a CCK-A receptor antagonist with the activity of inhibiting CCK8-induced amylase secretion. A-65186 has high binding affinity for pancreatic CCK-A receptors, is more than 500 times more selective for CCK-A receptors than for CCK-B receptors, and can inhibit CCK8-induced amylase secretion.

[1] Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors DOI:10.1021/jm00116a002