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Cat. No. Name Size Price Add Cart
KI3743MDL299515 mg$490

Chemical Characteristic

Product NameMDL29951
CAS No.130798-51-5
Molecular Weight 302.11
FormulaC12H9Cl2NO4
Chemical Name2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid
Smiles[nH]1c(c(c2c(cc(cc12)Cl)Cl)CCC(=O)O)C(=O)O
Chemical Structure

Biological activities

MDL-29951 is a novel glycine antagonist of NMDA receptor activation (Ki=0.14 mM, [3H]glycine binding) [1]. MDL-29951 completely inhibited the use-dependent binding of [3H]N-[1-(2-thienyl) cyclohexyl]-piperidine, and it was noncompetitive, glycine-reversible inhibitor of both NMDA-induced biochemical and electrophysiological responses in brain slice preparations . 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].

References

[1] Baron BM, Harrison BL, McDonald IA, et al. Potent indole- and quinoline-containing N-methyl-D-aspartate antagonists acting at the strychnine-insensitive glycine binding site. J Pharmacol Exp Ther. 1992,262(3):947-956.
[2] Wright SW, Carlo AA, Danley DE, et al. 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. Bioorg Med Chem Lett. 2003,13(12):2055-2058.
[3] Harden TK. Enigmatic GPCR finds a stimulating drug. Sci Signal. 2013,6(298):34.

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