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10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
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 ified with D-serine. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Isomeric SMILES | C1=CC=C(C=C1)/C(=C\C2=C(NC3=C2C(=CC(=C3)Cl)Cl)C(=O)O)/C(=O)O |
|---|---|
| Alternate CAS | 161230-88-2 |
| PubChem CID | 6603913 |
| MeSH Entry Terms | 3-(2-phenyl-2-carboxyethenyl)-4,6-dichloro-1H-indole-2-carboxylic acid;MDL 105,519;MDL 105519;MDL-105519 |
| Molecular Weight | 376.19 |
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