MDL 29951 2-Carboxy-4,6-dichloro-1H-indole-3-propionic acid;3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid;2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid;MDL-29951 2-Carboxy-4,6-dichloro-1H-indo 130798-51-5
MDL-29951 is a novel glycine antagonist of NMDA receptor activation (Ki=0.14 mM, [3H]glycine binding) in vitro and in vivo.
IC50 value: 0.14 mM ([3H]glycine binding) [1].
Target: NMDA receptor
in vitro: MDL-29951 was approximately 2000-fold selective for the glycine binding site relative to the glutamate recognition sites. MDL-29951 completely inhibited the use-dependent binding of [3H]N-[1-(2-thienyl) cyclohexyl]-piperidine and was noncompetitive, glycine-reversible inhibitor of both NMDA-induced biochemical and electrophysiological responses in brain slice preparations [1]. MDL-29951, an antagonist of the glycine site of the NMDA receptor, has been found to be an allosteric inhibitor of the enzyme fructose 1,6-bisphosphatase [2]. MDL29951 did not activate any of the known uracil or adenine nucleotide-activated P2Y receptors or cysteinyl leukotriene receptors [3].
in vivo: MDL-29951 produced parallel rightward shifts in the glycine requirement for demonstration of NMDA-stimulated elevations in cytosolic calcium in cultured neuronal preparations. The glycine antagonists were potent anticonvulsants after their i.c.v. administration to audiogenic seizure-susceptible DBA/2J mice[1]. MDL29951 diminished myelination in primary oligodendrocytes isolated from heterozygous mice but had no effect on myelination in oligodendrocytes from GPR17 knockout mice [3].
About|Contact|Cas|Product Name|Molecular|Country|Encyclopedia
Message|New Cas|MSDS|Service|Advertisement|CAS DataBase|Article Data|Manufacturers | Chemical Catalog
©2008 LookChem.com,License: ICP
NO.:Zhejiang16009103
complaints:service@lookchem.com Desktop View