ICI 216140 is a GRP/bombesin receptor 2 antagonist (IC50: 2 nM in vitro). At 2 mg/kg, it can decrease bombesin-stimulated pancreatic amylase secretion in rats. At 1 mM, it has been proved to attenuate bombesin-stimulated increases in blood pressure in rat
Potent bombesin receptor agonist (IC50 values are 0.26, 1.55 and 2.52 nM for BB1, BB2 and BB3 respectively). Enhances glucose transport in obese and diabetic primary myocytes. Also stimulates NCI-H1299 lung cancer cell proliferation in vitro.