Target Validation Information
Target ID T69494
Target Name NMDA receptor
Target Type
Successful
Drug Potency against Target L-Glutamic Acid Drug Info EC50 = 10~20 uM [552549]
Magnesium Sulfate Drug Info IC50 = 420000 nM [552251]
Orphenadrine Drug Info IC50 = 16200 nM [553233]
Ketamine Drug Info IC50 = 310 nM [552920]
EAA-090 Drug Info IC50 = 30 nM [552601]
D-cycloserine Drug Info EC50 = 2900 nM [553021]
Action against Disease Model Orphenadrine IC50 on mitochondrial membrane potential decrease evoked by NMDA: 11600nM [552183] Drug Info
References
Ref 552183In vitro and in vivo protective effect of orphenadrine on glutamate neurotoxicity. Neuropharmacology. 1999 May;38(5):671-7.
Ref 552549Targeting the metabotropic glutamate receptor mGluR4 for the treatment of diseases of the central nervous system. Curr Top Med Chem. 2005;5(9):885-95.
Ref 552251Modulation of NMDA receptor function by ketamine and magnesium: Part I. Anesth Analg. 2001 May;92(5):1173-81.
Ref 553233Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237-46.
Ref 552920Mg2+ imparts NMDA receptor subtype selectivity to the Alzheimer's drug memantine. J Neurosci. 2009 Mar 4;29(9):2774-9. doi: 10.1523/JNEUROSCI.3703-08.2009.
Ref 552601N-methyl-D-aspartate receptor (NMDA) antagonists as potential pain therapeutics. Curr Top Med Chem. 2006;6(8):749-70.
Ref 553021Structural determinants of D-cycloserine efficacy at the NR1/NR2C NMDA receptors. J Neurosci. 2010 Feb 17;30(7):2741-54. doi: 10.1523/JNEUROSCI.5390-09.2010.

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