中文名 | Asimadoline hydrochloride |
英文名 | Asimadoline hydrochloride |
别名 | 阿西马朵林盐酸盐 化合物ASIMADOLINE HYDROCHLORIDE |
英文别名 | Asimadoline-HCl EMD-61753 hydrochloride Asimadoline hydrochloride Asimadoline Hydrochlorine N-[(1S)-2-[(3S)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-N-methyl-2,2-diphenylacetamide |
CAS | 185951-07-9 |
化学式 | C27H31ClN2O2 |
分子量 | 451.01 |
存储条件 | -20°C |
体外研究 | Asimadoline (EMD-61753) hydrochloride has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC 50 for Asimadoline hydrochloride binding to μ-opioid receptors is 3 µM and to δ-opioid receptors is 0.7 µM. The IC 50 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 µM. Asimadoline hydrochloride has affinity to sodium and L type Ca 2+ ion channels at IC 50 concentrations 150 to 800 fold the IC 50 for the κ receptors. At high concentrations, Asimadoline hydrochloride demonstrates spasmolytic action against 400 µM barium chloride in the rat duodenum (IC 50 =4.2 µM), suggesting that Asimadoline hydrochloride may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified. |
体内研究 | 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. Animal Model: Adult female Sprague-Dawley rats Dosage: 1, 5, 15 mg/kg Administration: SC; single dose Result: Acutely ameliorated both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats. |
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