Asimadoline hydrochloride 是一种 κ-阿片(κ-opioid)受体激动剂,对豚鼠和人重组 κ-opioid 的IC50值分别为 5.6 和 1.2 nM。它可改善糖尿病大鼠的异常性疼痛,具有外周抗炎作用,并有用于肠易激综合征的研究潜力。
产品描述
Asimadoline HCl is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline has also been shown to be used in the treatment of irritable bowel syndrome.
体外活性
The IC50 for Asimadoline binding to μ-opioid receptors is 3 μM and to δ-opioid receptors is 0.7 μM. At high concentrations, Asimadoline demonstrates spasmolytic action against 400 μM barium chloride in the rat duodenum (IC50: 4.2 μM), suggesting that Asimadoline may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified[1].
体内活性
The metabolism of Asimadoline is rapid and appears similar in animals and man. The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through an increase in joint fluid substance P levels[1]. Treatment with Asimadoline (5 mg/kg/day i.p.) produces marked (and sustained) attenuation of the disease with all three-time regimes[2].
动物实验
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].
Cas No.
185951-07-9
分子式
C27H31ClN2O2
分子量
451.01
别名
阿西马朵林盐酸盐;EMD-61753 hydrochloride
储存和溶解度
DMSO:5 mg/mL,warmed
Powder: -20°C for 3 years
In solvent: -80°C for 2 years