Potent neuropeptide Y (NPY) Y1 receptor antagonist (pA2 = 10 and 10.5 at rY1 and hY1, receptors respectively). Also a potent and selective NPY Y4 receptor agonist (pEC50 values are 6.0, 8.6 and 6.1 for rY2, hY4 and rY5 receptors respectively). Suppresses food intake in rats in vivo. Also has affinity for neuropeptide FF (NPFF) receptors in vitro (Ki = 43-73 nM).

Selective galanin GAL2 receptor antagonist (Ki values are 13.1 and 420 nM for GAL2 and GAL1 receptors respectively). Blocks the pro-nociceptive effect of GAL2 receptor agonists.

AC-099 hydrochloride (化合物 3) 是一种选择性的 NPFF2R 完全激动剂 (EC50=1189 nM)，也是 NPFF1R 部分激动剂 (EC50=2370 nM)。AC-099 hydrochloride 能减弱脊神经结扎诱导的大鼠超敏性。