Asimadoline-EMD-61753-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAsimadolineCat. No.: HY-107384CAS No.: 153205-46-0Synonyms: EMD-61753分式: CHNO分量: 414.54作靶点: Opioid Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DM

2、SO : 103.3 mg/mL (249.19 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.03 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (6.03 mM); Suspended solution; Need ultrasonic3. 请依序添加每种溶剂： 10% DM

3、SO 90% corn oilSolubility: 2.5 mg/mL (6.03 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Asimadoline种有效的 opioid 受体激动剂，对于豚和类重 组 opioid受体的 IC50 值分别为5.6和1.2nM。IC50 & Target IC50: 5.6 nM (guinea pig opioid), 1.2 nM (human recombinant opioid) 1体外研究 The IC50 for Asimadoline binding to -opioid receptors is 3 M

4、 and to -opioid receptors is 0.7 M. The IC50values for D1, D2, kainate, , PCP/NMDA, H1, 1, 2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2,5HT3, AMPA and kainate/AMPA receptors are all 10 IC50, suggesting no relevant antihistaminergic,antiserotonergic or anticholinergic effects. At high concentrations,

5、 Asimadoline demonstrates spasmolyticaction against 400 M barium chloride in the rat duodenum (IC50=4.2 M), suggesting that Asimadoline mayblock the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified 1.体内研究 The absorption rate following oral administration

6、 is 80% in rats and 90% in dogs and monkeys. Themetabolism 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 1. Treatmentwith Asimadoline (5 mg/kg/day i.p.)

7、produces marked (and sustained) attenuation of the disease with all threetime regimes 2.PROTOCOLAnimal Rats: Asimadoline (5 mg/kg/day, n=10 per group) or vehicle (2 mL/kg/day, n=10) is administered to DA ratsAdministration 2 by i.p. injection twice daily (i) during the primary inflammatory phase (da

8、ys 13); (ii) once the disease isestablished (days 1321); or (iii) throughout the entire time course (days 1-21). Non-arthritic control animalsreceive Asimadoline (5 mg/kg/day, n=5) or vehicle (2 mL/kg/day, n=5) by i.p. injection twice daily. In allcases, disease parameters are assessed. In this expe

9、riment, the SP content of joint tissue is assessed onlyafter the rats are killed (day 21) 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Camilleri M, et al. Asimadoline, a -Opioid Agonist, and Visceral Sensation. Neurogastroenterol Motil. 2008 Sep; 20(9): 971979.2. Binder W, et al. Involvement of substance P in the anti-inflammatory effects of the peripherally selective kappa-opioid asimadoline andthe NK1 antagonist GR205171. Eur J Neurosci. 1999 Jun;11(6):2065-72.McePdfHeightCaution: Product has not been fully validat