Asimadoline-EMD-61753-DataSheet-生命科學(xué)試劑-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作靶點(diǎn): Opioid Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) 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. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.03 mM); Suspended solution; Need ultrasonic3. 請(qǐng)依序添加每種溶劑： 10% DM

3、SO 90% corn oilSolubility: 2.5 mg/mL (6.03 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Asimadoline種有效的 opioid 受體激動(dòng)劑，對(duì)于豚和類(lèi)重 組 opioid受體的 IC50 值分別為5.6和1.2nM。IC50 & Target IC50: 5.6 nM (guinea pig opioid), 1.2 nM (human recombinant opioid) 1體外研究 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.體內(nèi)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