| 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 552183 | In vitro and in vivo protective effect of orphenadrine on glutamate neurotoxicity. Neuropharmacology. 1999 May;38(5):671-7. | ||||
| Ref 552549 | 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 552251 | Modulation of NMDA receptor function by ketamine and magnesium: Part I. Anesth Analg. 2001 May;92(5):1173-81. | ||||
| Ref 553233 | 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. | ||||
| Ref 552920 | Mg2+ 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 552601 | N-methyl-D-aspartate receptor (NMDA) antagonists as potential pain therapeutics. Curr Top Med Chem. 2006;6(8):749-70. | ||||
| Ref 553021 | Structural 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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