Bombesin receptor antagonist that inhibits bombesin binding to rat brain with an IC50 value of 2 μM. Inhibits amylase release in vitro (IC50 = 4 μM) and attenuates bombesin-mediated suppression of food intake in vivo.
Broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. In
Highly potent and selective OX2 receptor agonist; displays 400-fold selectivity over OX1 receptors. EC50 values are 0.13 and 52 nM for human OX2 and OX1 receptors respectively.