GI-181771X

GI-181771X is a potent, orally bioavailable small molecule agonist of the cholecystokinin 1 (CCK1) receptor, belonging to the benzodiazepine class. Developed by GlaxoSmithKline, it was investigated primarily for the treatment of obesity and related metabolic disorders. The drug acts as a full agonist at peripheral CCK1 receptors—particularly on vagal afferent fibers and pyloric sphincter—modulating gastric emptying, increasing fasting gastric volumes, and promoting satiation. Unlike classic benzodiazepines, it does not exhibit sedative or anxiolytic effects. In clinical studies in humans and preclinical models in rodents, GI‑181771X reduced food intake but did not consistently reduce body weight in human trials; gastrointestinal side effects were more common than with placebo. Morphological changes in the pancreas were observed in rodents but not confirmed in monkeys or humans[1][3][5].

Other names

305366-98-7UNII-6YF0SHR37TUNII6YF0SHR37TUNII 6YF0SHR37TCHEMBL1269257CHEMBL-1269257CHEMBL 1269257