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.
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