MDL-105519 - iGluR 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMDL 105519Cat. No.: HY-15085CAS No.: 161230-88-2分式: CHClNO分量: 376.19作靶點: iGluR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 17 mg/

2、mL (45.19 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6582 mL 13.2912 mL 26.5823 mL5 mM 0.5316 mL 2.6582 mL 5.3165 mL10 mM 0.2658 mL 1.3291 mL 2.6582 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 MDL 105519有效和選擇性的氨酸與 NMDA 受體結(jié)合的拮抗劑。體外研究M

3、DL 105519 is a potent and selective ligand for the glycine recognition site that completely inhibit the bindingof 3Hglycine to rat brain membranes with a Ki value of 10.9 nM. MDL 105519 is approximately 10,000-foldselective for the glycine recognition site relative to the other receptor types invest

4、igated. MDL 105519 inhibitsNMDA-dependent responses, such as elevations of 3HTCP binding in brain membranes, cyclic GMPaccumulation in brain slices, and alterations in cytosolic Ca2+ and Na+-Ca2+ currents in cultured neurons.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEInhibition is non-competit

5、ive with respect to NMDA and could be nullified with D-serine 1.體內(nèi)研究 MDL 105519 is an NMDA receptor antagonist in vivo. Intravenously administration of MDL 105519 preventsharmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDAreceptor antagonism in viv

6、o. This antagonism is associated with anticonvulsant activity in genetically based,chemically induced, and electrically mediated seizure models. Anxiolytic activity is observed in the ratseparation-induced vocalization model, but muscle-relaxant activity is apparent at lower doses. Higher dosesimpai

7、r rotorod performance, but are without effect on mesolimbic dopamine turnover or prepulse inhibition ofthe startle reflex 1.PROTOCOLAnimal Adult, male, CD rats are administered MK-801 (n=4, 2 mg/kg, i.p.) or MDL 105519 (n=4, 2 mg/kg, i.p.) andAdministration 1 extracellular dopamine concentrations ar

8、e measured using in vivo microdialysis 1.Mice: Mice adult male CD-1 are injected with various doses of MDL 105519 (8, 16, 32, 64, 128 mg/kg)intraperitoneally and 30 min later are administered harmaline 50 mg/kg. Sixty minutes after the first injection,the mice are killed and cerebellar cGMP content

9、is measured by radioimmunoassay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Baron BM, et al. Pharmacological characterization of MDL 105,519, an NMDA receptor glycine site antagonist. Eur J Pharmacol. 1997Apr 4;323(2-3):181-92.McePdfHeightCaution: Product has not been fully validated for medic