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MDL 105519

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Catalog No. T16032Cas No. 161230-88-2

MDL 105519 is an effective antagonist of glycine binding to the NMDA receptor.

MDL 105519

MDL 105519

😃Good
Catalog No. T16032Cas No. 161230-88-2
MDL 105519 is an effective antagonist of glycine binding to the NMDA receptor.
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2 mg$595 days
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Product Introduction

Bioactivity
Description
MDL 105519 is an effective antagonist of glycine binding to the NMDA receptor.
In vitro
MDL 105519 is approximately 10,000-fold selective for the glycine recognition site relative to the other receptor types investigated. MDL 105519 is an effective and selective ligand for the glycine recognition site that completely inhibit the binding of [3H]glycine to rat brain membranes (Ki: 10.9 nM). MDL 105519 inhibits NMDA-dependent responses, such as elevations of [3H]TCP binding in brain membranes, cyclic GMP accumulation in brain slices, and alterations in cytosolic Ca2+ and Na+-Ca2+ currents in cultured neurons. Its inhibition is non-competitive with respect to NMDA and could be nullified with D-serine.
In vivo
MDL 105519 acts as an NMDA receptor antagonist in vivo, effectively blocking harmaline-induced increases in cerebellar cyclic GMP levels through intravenous administration, demonstrating its biochemical antagonistic properties. It exhibits anxiolytic effects in rat separation-induced vocalization tests, with noticeable muscle-relaxant properties at reduced dosages. The compound's antagonism also correlates with anticonvulsant effects across various seizure models, including genetic, chemically induced, and electrically provoked. Although higher doses compromise rotorod performance, they do not influence mesolimbic dopamine turnover or affect prepulse inhibition of the startle reflex.
Chemical Properties
Molecular Weight376.19
FormulaC18H11Cl2NO4
Cas No.161230-88-2
Relative Density.1.594 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 17 mg/mL (45.19 mM), Sonication and heating are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6582 mL13.2912 mL26.5823 mL132.9116 mL
5 mM0.5316 mL2.6582 mL5.3165 mL26.5823 mL
10 mM0.2658 mL1.3291 mL2.6582 mL13.2912 mL
20 mM0.1329 mL0.6646 mL1.3291 mL6.6456 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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