[CAS NO. 161230-88-2] MDL105519
PRODUCTS SPECIFICATIONS [161230-88-2]
DESCRIPTION [161230-88-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 376.19 |
| Molecular Formula | C18H11Cl2NO4 |
| SMILES | O=C(O)C(N1)=C(/C=C(C2=CC=CC=C2)/C(O)=O)C3=C1C=C(Cl)C=C3Cl |
Summary
MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.
In Vitro
MDL 105519 is a potent and selective ligand for the glycine recognition site that completely inhibit the binding of [ 3 H]glycine to rat brain membranes with a K i value of 10.9 nM. MDL 105519 is approximately 10,000-fold selective for the glycine recognition site relative to the other receptor types investigated. MDL 105519 inhibits NMDA-dependent responses, such as elevations of [ 3 H]TCP binding in brain membranes, cyclic GMP accumulation in brain slices, and alterations in cytosolic Ca 2+ and Na + -Ca 2+ currents in cultured neurons. Inhibition is non-competitive with respect to NMDA and could be nullified with D-serine [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MDL 105519 is an NMDA receptor antagonist in vivo . Intravenously administration of MDL 105519 prevents harmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDA receptor antagonism in vivo . This antagonism is associated with anticonvulsant activity in genetically based, chemically induced, and electrically mediated seizure models. Anxiolytic activity is observed in the rat separation-induced vocalization model, but muscle-relaxant activity is apparent at lower doses. Higher doses impair rotorod performance, but are without effect on mesolimbic dopamine turnover or prepulse inhibition of the startle reflex [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 17 mg/mL ( 45.19 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6582 mL | 13.2912 mL | 26.5823 mL |
| 5 mM | 0.5316 mL | 2.6582 mL | 5.3165 mL |
| 10 mM | 0.2658 mL | 1.3291 mL | 2.6582 mL |
