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Asimadoline hydrochloride

CAS No. : 185951-07-9

MCE 站：Asimadoline hydrochloride

产品活性：Asimadoline (EMD-61753) hydrochloride 是一种口服有效的，选择性的，具有周边活性的 κ-opioid 激动剂，对豚鼠和人重组 κ-opioid 的 IC₅₀s 分别为 5.6 nM 和 1.2 nM。Asimadoline hydrochloride 对血脑屏障的渗透性低，具有外周抗炎作用。Asimadoline hydrochloride 可改善糖尿病大鼠的异常性疼痛，并具有用于肠易激综合征 (IBS) 研究的潜力。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

In Vitro: Asimadoline (EMD-61753) hydrochloride has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC₅₀ for Asimadoline hydrochloride binding to μ-opioid receptors is 3 ?M and to δ-opioid receptors is 0.7 ?M. The IC₅₀ values for D1, D2, kainate, σ, PCP/NMDA, H1, α1, α2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2, 5HT3, AMPA and kainate/AMPA receptors are all >10 ?M.
Asimadoline hydrochloride has affinity to sodium and L type Ca²⁺ ion channels at IC₅₀ concentrations 150 to 800 fold the IC₅₀ for the κ receptors.
At high concentrations, Asimadoline hydrochloride demonstrates spasmolytic action against 400 ?M barium chloride in the rat duodenum (IC₅₀=4.2 ?M), suggesting that Asimadoline hydrochloride may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified.

In Vivo: Asimadoline (EMD-61753 hydrochloride; 1, 5, 15 mg/kg; s.c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.
The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. The metabolism of Asimadoline hydrochloride is rapid and appears similar in animals and man. Asimadoline hydrochloride has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels.
Treatment with Asimadoline hydrochloride (5 mg/kg/day; i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes.

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