Target Information

Target General Infomation
Target ID
T69494
Former ID
TTDS00135
Target Name
NMDA receptor
Target Type
Successful
Disease Anaesthesia; Anxiety disorder [ICD9:338, 300, 311; ICD10: R52, G89, F32, F40-F42]
Anesthesia [ICD9: 338; ICD10: R20.0]
Acute ischemic stroke [ICD9: 434.91; ICD10: I61-I63]
Acute pain [ICD9: 338,780; ICD10: R52, G89]
Alzheimer disease [ICD9: 331; ICD10: G30]
Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Cancer pain [ICD9: 140-229, 338,780; ICD10: R52, G89]
Cerebral infarction [ICD10: I63]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Dementia [ICD9: 290-294; ICD10: F01-F07]
Depression [ICD9: 311; ICD10: F30-F39]
Exogenous obesity [ICD10: E66]
Epileptic seizures; Alzheimer disease [ICD9:345.9, 780.3, 331; ICD10: G40, P90, R56, G30]
Epilepsy [ICD10: G40]
Epileptic seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Neuropathy [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Neurodegenerative disease [ICD9: 330-337; ICD10: G30-G32]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Obsessive compulsive disorder [ICD9: 300.3; ICD10: F42]
Parkinson's disease [ICD9: 332; ICD10: G20]
Painful diabetic neuropathy [ICD9: 250.6,338,780; ICD10: E10.4, E11.4, E13.4, G89, R52]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Suicidal ideation [ICD10: R45.8]
Schizophrenia [ICD9: 295; ICD10: F20]
Schizophrenia; Indigestion [ICD9:295; ICD10: F20, K30]
Traumatic brain injury [ICD9: 800.0-801.9, 803.0-804.9, 850.0-854.1; ICD10: S06]
BioChemical Class
Ion transport
Target Validation
T69494
Drugs and Mode of Action
Drug(s) Benzphetamine Drug Info Approved Exogenous obesity [551871]
D-cycloserine Drug Info Approved Bacterial infections [536854]
Felbamate Drug Info Approved Epilepsy [536756], [540874]
Huperzine A Drug Info Approved Epileptic seizures; Alzheimer disease [544707], [551871]
Ketamine Drug Info Approved Anesthesia [467569], [536308]
L-Glutamic Acid Drug Info Approved Schizophrenia; Indigestion [536838], [538847], [551871]
Magnesium Drug Info Approved Acute ischemic stroke [537116]
Magnesium Sulfate Drug Info Approved Acute pain [537116]
Memantine Drug Info Approved Alzheimer disease [467588], [528380]
Nitrous oxide Drug Info Approved Anaesthesia; Anxiety disorder [536300], [551871]
Orphenadrine Drug Info Approved Parkinson's disease [538173], [542269]
Amitriptyline+ketamine Drug Info Phase 3 Neuropathic pain [544412]
Dexanabinol Drug Info Phase 3 Traumatic brain injury [537115]
Remacemide Drug Info Phase 3 Pain [534082]
AV-101 Drug Info Phase 2 Neuropathic pain [525245]
CHF-3381 Drug Info Phase 2 Neuropathic pain [529017], [536374]
CNS-5161 Drug Info Phase 2 Neuropathic pain [536374]
D-cycloserine Drug Info Phase 2 Obsessive compulsive disorder [536854]
Dextromethorphan+quinidine Drug Info Phase 2 Painful diabetic neuropathy [536078]
Dimiracetam Drug Info Phase 2 Neuropathic pain [523061]
MDL-27192 Drug Info Phase 2 Epileptic seizures [546020]
Neramexane Drug Info Phase 2 Cancer pain [536058]
NRX-1074 Drug Info Phase 2 Major depressive disorder [524651]
TRAXOPRODIL MESYLATE Drug Info Phase 2 Neurological disease [521688]
ADCI Drug Info Phase 1 Epileptic seizures [525718]
ASP-0777 Drug Info Phase 1 Alzheimer disease [523568]
AZD6423 Drug Info Phase 1 Suicidal ideation [524408]
AD-529 Drug Info Preclinical Neuropathic pain [548142]
ADX-2 series Drug Info Preclinical Schizophrenia [536463]
ED-1812 Drug Info Preclinical Pain [548142]
Midafotel Drug Info Discontinued in Phase 3 Cognitive disorders [545291]
Selfotel Drug Info Discontinued in Phase 3 Cerebrovascular ischaemia [467500], [544835]
AZD6765 Drug Info Discontinued in Phase 2 Major depressive disorder [542661], [548584]
EAA-090 Drug Info Discontinued in Phase 2 Painful diabetic neuropathy [536374]
SGS-111 Drug Info Discontinued in Phase 2 Cognitive disorders [547578]
CGP-37849 Drug Info Discontinued in Phase 1 Neurological disease [467499], [546401]
Delucemine Drug Info Discontinued in Phase 1 Depression [546633]
S-1746 Drug Info Discontinued in Phase 1 Cerebrovascular ischaemia [547450]
ACEA-1011 Drug Info Terminated Cerebral infarction [546400]
ACEA-1031 Drug Info Terminated Cerebrovascular ischaemia [546460]
ACEA-1328 Drug Info Terminated Cancer pain [546357]
ACEA-1416 Drug Info Terminated Cerebrovascular ischaemia [546407]
CNS-1531 Drug Info Terminated Neuropathy [545051]
CNS-5788 Drug Info Terminated Cerebrovascular ischaemia [547184]
Dextrorphan Drug Info Terminated Acute ischemic stroke [546637]
FR-115427 Drug Info Terminated Cerebrovascular ischaemia [546642]
GPI-3000 Drug Info Terminated Cerebrovascular ischaemia [544990]
IDRA-21 Drug Info Terminated Alzheimer disease [467553], [527059]
L-689560 Drug Info Terminated Neurodegenerative disease [467573], [544995]
L-698544 Drug Info Terminated Alzheimer disease [545425]
LY-274614 Drug Info Terminated Dementia [544875]
M-241247 Drug Info Terminated Cerebrovascular ischaemia [545475]
NPS-1392 Drug Info Terminated Cerebrovascular ischaemia [547110]
PD-158473 Drug Info Terminated Cerebrovascular ischaemia [546428]
PD-159913 Drug Info Terminated Cerebrovascular ischaemia [546429]
Modulator ACEA-1011 Drug Info [533995]
ACEA-1031 Drug Info [533702]
ACEA-1416 Drug Info [534653]
ACPC Drug Info [533815], [551871]
ADCI Drug Info [525718]
ASP-0777 Drug Info [551922]
CGP-37849 Drug Info [530393]
CNS-1531 Drug Info [550138]
Delucemine Drug Info [525692]
FR-115427 Drug Info [533718]
GPI-3000 Drug Info [534607]
IDRA-21 Drug Info [527059]
L-689560 Drug Info [526795]
L-698544 Drug Info [533941]
LY-274614 Drug Info [533610]
MDL-27192 Drug Info [534392], [551871]
Memantine Drug Info [526721], [551871]
Midafotel Drug Info [531509]
PD-158473 Drug Info [526459]
PD-159913 Drug Info [550138]
SGS-111 Drug Info [544121]
TRAXOPRODIL MESYLATE Drug Info [527945], [551871]
Antagonist ACEA-1328 Drug Info [536058]
AD-529 Drug Info [550138]
ADX-2 series Drug Info [536463]
Amitriptyline+ketamine Drug Info [536374]
Aptiganel HCl Drug Info [535658]
AV-101 Drug Info [551769]
AZD6423 Drug Info [543994]
AZD6765 Drug Info [550288]
Benzphetamine Drug Info [535378]
C-101,606 Drug Info [535404]
CHF-3381 Drug Info [536374]
CNS-5161 Drug Info [536374]
CNS-5788 Drug Info [525990]
Dexanabinol Drug Info [537115]
Dextromethorphan+quinidine Drug Info [536374]
Dextrorphan Drug Info [535658]
Dimiracetam Drug Info [532652]
EAA-090 Drug Info [536374]
ED-1812 Drug Info [550138]
Felbamate Drug Info [536399], [536617], [536643]
Huperzine A Drug Info [536934]
Ketamine Drug Info [536166], [537586], [537702]
L-Glutamic Acid Drug Info [536888]
M-241247 Drug Info [545476]
Magnesium Drug Info [537116]
Magnesium Sulfate Drug Info [536484]
Neramexane Drug Info [536058]
Nitrous oxide Drug Info [536300]
NPS-1392 Drug Info [525561]
Orphenadrine Drug Info [537076], [538036]
S-1746 Drug Info [528007]
Selfotel Drug Info [535658]
Agonist D-cycloserine Drug Info [536773], [536854]
NRX-1074 Drug Info [532574]
Remacemide Drug Info [535658], [536166]
References
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Ref 467500(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4155).
Ref 467553(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4219).
Ref 467569(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4233).
Ref 467573(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4239).
Ref 467588(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4253).
Ref 521688ClinicalTrials.gov (NCT00163059) The Antidepressant Effects Of The NMDA Antagonist, CP-101,606, In Patients With MDD. U.S. National Institutes of Health.
Ref 523061ClinicalTrials.gov (NCT01135251) Safety and Preliminary Evidence of Efficacy of Escalating Doses of Dimiracetam in AIDS Patients With Painful Neuropathy. U.S. National Institutes of Health.
Ref 523568ClinicalTrials.gov (NCT01406145) A Study of the Safety and Tolerability of ASP0777 in Subjects With Alzheimer's Disease (AD) Taking a Stable Dose of Donepezil. U.S. National Institutes of Health.
Ref 524408ClinicalTrials.gov (NCT01926366) AZD6423 SAD/MAD Study in Healthy Volunteers. U.S. National Institutes of Health.
Ref 524651ClinicalTrials.gov (NCT02067793) Study of Intravenous NRX-1074 in Patients With Major Depressive Disorder. U.S. National Institutes of Health.
Ref 525245ClinicalTrials.gov (NCT02484456) Antidepressant Effects of the Glycine Receptor Antagonist AV-101 (4-chlorokynurenine) in Major Depressive Disorder.
Ref 525718The anticonvulsant SGB-017 (ADCI) blocks voltage-gated sodium channels in rat and human neurons: comparison with carbamazepine. Epilepsia. 2000 Mar;41(3):263-70.
Ref 527059IDRA-21, a positive AMPA receptor modulator, inhibits synaptic and extrasynaptic NMDA receptor mediated events in cultured cerebellar granule cells. Neuropharmacology. 2004 Jun;46(8):1105-13.
Ref 528380Treatment effect size of memantine therapy in Alzheimer disease and vascular dementia. Alzheimer Dis Assoc Disord. 2006 Jul-Sep;20(3):133-7.
Ref 529017Indantadol, a novel NMDA antagonist and nonselective MAO inhibitor for the potential treatment of neuropathic pain. IDrugs. 2007 Sep;10(9):636-44.
Ref 534082Block of the N-methyl-D-aspartate receptor by remacemide and its des-glycine metabolite. J Pharmacol Exp Ther. 1996 Jan;276(1):161-8.
Ref 536058Emerging analgesics in cancer pain management. Expert Opin Emerg Drugs. 2005 Feb;10(1):151-71.
Ref 536078Dextromethorphan/quinidine: AVP 923, dextromethorphan/cytochrome P450-2D6 inhibitor, quinidine/dextromethorphan. Drugs R D. 2005;6(3):174-7.
Ref 536300Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79.
Ref 536308Calcium channel blockers in the spectrum of antihypertensive agents. Expert Opin Pharmacother. 2006 Dec;7(17):2385-401.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536756Use of second-generation antiepileptic drugs in the pediatric population. Paediatr Drugs. 2008;10(4):217-54.
Ref 536838Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22.
Ref 536854Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6.
Ref 537115Emerging treatments for traumatic brain injury. Expert Opin Emerg Drugs. 2009 Mar;14(1):67-84.
Ref 537116Emerging drugs for acute ischemic stroke. Expert Opin Emerg Drugs. 2009 Mar;14(1):33-42.
Ref 538173FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040249.
Ref 538847(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1369).
Ref 540874(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5473).
Ref 542269(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7251).
Ref 542661(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7681).
Ref 544412A Phase III Randomized, Placebo-Controlled Study of Topical Amitriptyline and Ketamine for Chemotherapy-Induced Peripheral Neuropathy (CIPN): A University of Rochester CCOP Study of 462 Cancer Survivors. Support Care Cancer. 2014 July; 22(7): 1807-1814.
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Ref 527059IDRA-21, a positive AMPA receptor modulator, inhibits synaptic and extrasynaptic NMDA receptor mediated events in cultured cerebellar granule cells. Neuropharmacology. 2004 Jun;46(8):1105-13.
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Ref 532652Broad spectrum and prolonged efficacy of dimiracetam in models of neuropathic pain. Neuropharmacology. 2014 Jun;81:85-94.
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Ref 533702In vitro pharmacology of ACEA-1021 and ACEA-1031: systemically active quinoxalinediones with high affinity and selectivity for N-methyl-D-aspartate receptor glycine sites. Mol Pharmacol. 1995 Mar;47(3):568-81.
Ref 533718Non-competitive NMDA antagonists, FR115427 and MK801, enhance neuronal survival in primary culture. Neurosci Lett. 1995 Feb 9;185(2):107-10.
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Ref 5339413-Nitro-3,4-dihydro-2(1H)-quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors. J Med Chem. 1993 Oct 29;36(22):3397-408.
Ref 533995NMDA receptor antagonists, MK-801 and ACEA-1011, prevent the development of tonic pain following subcutaneous formalin. Brain Res. 1993 Jul 2;615(2):331-4.
Ref 534392Preclinical characterization of MDL 27,192 as a potential broad spectrum anticonvulsant agent with neuroprotective properties. Epilepsy Res. 1997 Apr;27(1):41-54.
Ref 534607Treatment with the competitive NMDA antagonist GPI 3000 does not improve outcome after cardiac arrest in dogs. Stroke. 1998 Apr;29(4):824-9.
Ref 534653Tolerance develops to the antinociceptive and motor impairing effects of ACEA-1416, a NMDA receptor antagonist, in the formalin and rotarod test in mice. Pharmacol Res. 1998 Apr;37(4):295-302.
Ref 535378Amphetamine inhibits the N-methyl-D-aspartate receptor-mediated responses by directly interacting with the receptor/channel complex. J Pharmacol Exp Ther. 2002 Mar;300(3):1008-16.
Ref 535404Current status of neuroprotective agents in the treatment of acute ischemic stroke. Curr Neurol Neurosci Rep. 2001 Jan;1(1):13-8.
Ref 535658Neuroprotective agents for the treatment of acute ischemic stroke. Curr Neurol Neurosci Rep. 2003 Jan;3(1):9-20.
Ref 536058Emerging analgesics in cancer pain management. Expert Opin Emerg Drugs. 2005 Feb;10(1):151-71.
Ref 536166Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
Ref 536300Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 536399Mechanisms of action of antiepileptic drugs. Int Rev Neurobiol. 2007;81:85-110.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536484Magnesium sulfate diminishes the effects of amide local anesthetics in rat sciatic-nerve block. Reg Anesth Pain Med. 2007 Jul-Aug;32(4):288-95.
Ref 536617Interactions of MRZ 2/576 with felbamate, lamotrigine, oxcarbazepine and topiramate in the mouse maximal electroshock-induced seizure model. Pharmacology. 2008;81(3):259-65. Epub 2008 Feb 4.
Ref 536643Molecular determinants of the anticonvulsant felbamate binding site in the N-methyl-D-aspartate receptor. J Med Chem. 2008 Mar 27;51(6):1534-45. Epub 2008 Feb 27.
Ref 536773How many modes of action should an antibiotic have? Curr Opin Pharmacol. 2008 Oct;8(5):564-73. Epub 2008 Jul 30.
Ref 536854Has nature already identified all useful antibacterial targets? Curr Opin Microbiol. 2008 Oct;11(5):387-92. Epub 2008 Oct 6.
Ref 536888Altered expression of genes involved in GABAergic transmission and neuromodulation of granule cell activity in the cerebellum of schizophrenia patients. Am J Psychiatry. 2008 Dec;165(12):1594-603. Epub 2008 Oct 15.
Ref 536934Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43. Epub 2008 Nov 12.
Ref 537076Involvement of voltage-gated sodium channels blockade in the analgesic effects of orphenadrine. Pain. 2009 Apr;142(3):225-35. Epub 2009 Feb 12.
Ref 537115Emerging treatments for traumatic brain injury. Expert Opin Emerg Drugs. 2009 Mar;14(1):67-84.
Ref 537116Emerging drugs for acute ischemic stroke. Expert Opin Emerg Drugs. 2009 Mar;14(1):33-42.
Ref 537586Ketamine Modulates Theta and Gamma Oscillations. J Cogn Neurosci. 2009 Jul 7.
Ref 537702Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat cerebral cortex. Br J Pharmacol. 1985 Feb;84(2):381-91.
Ref 538036Dopamine/glutamate interactions in Parkinson's disease. Neurosci Biobehav Rev. 1997 Jul;21(4):393-400.
Ref 543994Biology of the NMDA Receptor. Marie L. Blanke and Antonius M.J. VanDongen. 2009.
Ref 544121Molecular basis of pharmacotherapies for cognition in Down syndrome. Trends Pharmacol Sci. 2010 February; 31(2): 66.
Ref 545476Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003415)
Ref 550138WO patent application no. 2009,0164,86, Use of nmda receptor antagonists for treatment of urologic tumors.
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
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