V1a/V2 antagonist 1 (Compound 18j) is an orally active dual-target antagonist of V1a and V2 receptors, exhibiting high binding affinity toward these receptors [Ki values are hV1a: 0.13 nM, hV2: 0.53 nM, and mV1a: 0.5 nM; IC50 for hV1a is 2.2 nM]. This compound can inhibit oxytocin-induced scratching behavior in mice.

V1a receptor (human):0.13 nM (Ki), V1a receptor (human):2.2 nM, V2 receptor (human):0.53 nM (Ki)

V1a/V2 antagonist 1 (1 μM) 显示出优良的肝微粒体代谢稳定性，其 Cl int (h/r/m) (μL/min/mg) 分别为15.9/36.9/27.1。该化合物与 hERG 无相互作用 (IC 50 ：>30 μM)，且其 PDR 值为 0.91 (VB-Caco-2 渗透性试验) [1] 。

V1a/V2 antagonist 1（0.1-3 mg/kg，口服，60 min 预处理）能够显著抑制由 Oxytocin 诱发的小鼠抓挠行为。