产品
编 号：F181163
分子式：C27H30N2O2
分子量：414.54
分子式：C27H30N2O2
分子量：414.54
产品类型
规格
价格
是否有货
结构图
CAS No: 153205-46-0
产品详情
生物活性：
Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).
体内研究：
Asimadoline (EMD-61753; 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 is rapid and appears similar in animals and man. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels. Treatment with Asimadoline (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.
体外研究：
Asimadoline (EMD-61753) has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC50 for Asimadoline binding to μ-opioid receptors is 3 μM and to δ-opioid receptors is 0.7 μM. 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 μM. Asimadoline 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 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.
Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).
体内研究：
Asimadoline (EMD-61753; 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 is rapid and appears similar in animals and man. Asimadoline has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels. Treatment with Asimadoline (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.
体外研究：
Asimadoline (EMD-61753) has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC50 for Asimadoline binding to μ-opioid receptors is 3 μM and to δ-opioid receptors is 0.7 μM. 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 μM. Asimadoline 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 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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备