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CAS No.: 153205-46-0

Asimadoline/阿西马朵林 Catalog No. CSN21495

Synonyms: EMD-61753;阿西马朵林

Asimadoline is an agonist of κ-opioid receptor (KOR) with IC50 of 1.2 nM.

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技术信息

生物活性

描述Asimadoline is a potent kappa-opioid receptor agonist with a diaryl acetamide structure. It has high affinity for the kappa receptor, with IC(50) of 5.6 nmol L(-1) (guinea pig) and 1.2 nmol L(-1) (human recombinant), and high selectively with kappa : micro : delta binding ratios of 1 : 501 : 498 in human recombinant receptors. It acts as a complete agonist in in vitro assay. 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]. Treatment with Asimadoline (5 mg/kg/day; i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes^[2]. Asimadoline (EMD-61753; 1, 5, 15 mg/kg; s.c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats^[3]. Asimadoline was extremely effective in attenuating joint damage (by up to 80%) when administered parenterally (0.5 to 10 mg kg(-1) day(-1), i.p.) throughout the disease or during its early phase; treatment was less successful if confined to the latter stages^[4].
参考文献

[1] Camilleri M. Novel pharmacology: asimadoline, a kappa-opioid agonist, and visceral sensation. Neurogastroenterol Motil. 2008 Sep;20(9):971-9
[2] Binder W, Scott C, Walker JS. Involvement of substance P in the anti-inflammatory effects of the peripherally selective kappa-opioid asimadoline and the NK1 antagonist GR205171. Eur J Neurosci. 1999 Jun;11(6):2065-72
[3] Jolivalt CG, Jiang Y, Freshwater JD, Bartoszyk GD, Calcutt NA. Dynorphin A, kappa opioid receptors and the antinociceptive efficacy of asimadoline in streptozotocin-induced diabetic rats. Diabetologia. 2006 Nov;49(11):2775-85
[4] Binder W, Walker JS. Effect of the peripherally selective kappa-opioid agonist, asimadoline, on adjuvant arthritis. Br J Pharmacol. 1998 Jun;124(4):647-54

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4123 mL
- 12.0616 mL
- 24.1231 mL
- 5 mM
- 0.4825 mL
- 2.4123 mL
- 4.8246 mL
- 10 mM
- 0.2412 mL
- 1.2062 mL
- 2.4123 mL

技术信息

CAS号

153205-46-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H30N2O2

运输

蓝冰

分子量

414.54

别名

EMD-61753;阿西马朵林

溶解度

DMSO	103.3 mg/mL (249.2 mM)
Water	Insoluble

动物实验配方

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