Asimadoline hydrochloride (EMD-61753 hydrochloride) is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline hydrochloride has also been shown to be used in the treatment of irritable bowel syndrome.

κ opioid (Guinea pig):5.6 nM (EC50), κ opioid (human recombinant):1.2 nM (EC50)

Asimadoline对μ-阿片受体的IC50为3μM，对δ-阿片受体的IC50为0.7μM。高浓度下，Asimadoline对大鼠十二指肠中400μM氯化钡显示出痉挛解除作用（IC50：4.2μM），表明Asimadoline可能通过尚未确定的机制阻断氯化钡对平滑肌的直接刺激效应[1]。

Asimadoline的代谢在动物和人类中快速且相似。口服后的吸收率在大鼠中为80%，在狗和猴子中超过90%。Asimadoline具有部分通过增加关节液中substance P水平[1]来介导的周围抗炎作用。使用Asimadoline (5 mg/kg/day i.p.)治疗，在所有三个时间方案下都能显著（且持续）减轻疾病[2]。

Asimadoline (5 mg/kg/day, n=10 per group) or vehicle (2 mL/kg/day, n=10) is administered to DA rats by i.p. injection twice daily (i) during the primary inflammatory phase (days 1–3); (ii) once the disease is established (days 13–21); or (iii) throughout the entire time course (days 1-21). Non-arthritic control animals receive Asimadoline (5 mg/kg/day, n=5) or vehicle (2 mL/kg/day, n=5) by i.p. injection twice daily. In all cases, disease parameters are assessed. In this experiment, the SP content of joint tissue is assessed only after the rats are killed (day 21)[2].