Target Validation Information
TTD ID	T69494
Target Name	N-methyl-D-aspartate receptor (NMDAR)
Type of Target	Successful
Drug Potency against Target	Cycloserine	Drug Info	EC50 = 2900 nM	[6]
	Ketamine	Drug Info	IC50 = 310 nM	[5]
	L-Glutamic Acid	Drug Info	EC50 = 10~20 uM	[3]
	Magnesium Sulfate	Drug Info	IC50 = 420000 nM	[2]
	Orphenadrine	Drug Info	IC50 = 16200 nM	[7]
	EAA-090	Drug Info	IC50 = 30 nM	[4]
Action against Disease Model	Orphenadrine	Drug Info	IC50 on mitochondrial membrane potential decrease evoked by NMDA: 11600nM	[1]
References
REF 1	In vitro and in vivo protective effect of orphenadrine on glutamate neurotoxicity. Neuropharmacology. 1999 May;38(5):671-7.
REF 2	Modulation of NMDA receptor function by ketamine and magnesium: Part I. Anesth Analg. 2001 May;92(5):1173-81.
REF 3	Targeting 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 4	N-methyl-D-aspartate receptor (NMDA) antagonists as potential pain therapeutics. Curr Top Med Chem. 2006;6(8):749-70.
REF 5	Mg2+ imparts NMDA receptor subtype selectivity to the Alzheimer's drug memantine. J Neurosci. 2009 Mar 4;29(9):2774-9.
REF 6	Structural determinants of D-cycloserine efficacy at the NR1/NR2C NMDA receptors. J Neurosci. 2010 Feb 17;30(7):2741-54.
REF 7	Orphenadrine 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.

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