Target Information

Target General Infomation
Target ID
T54128
Former ID
TTDS00121
Target Name
Glutamate receptor AMPA subtype
Synonyms
AMPA receptor; AMPA selective glutamate receptor; GluR; Glutamate receptor; Glutamate receptor ionotropic, AMPA
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Anaesthesia [ICD9: 338; ICD10: R52, G89]
Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Anesthesia [ICD9: 338; ICD10: R20.0]
Anxiety disorder; Panic attacks [ICD9: 300; ICD10: F40-F42]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Chemotherapy-induced peripheral neuropathy [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Coronary artery disease [ICD9: 410-414, 429.2; ICD10: I20-I25]
Convulsions [ICD9: 780.3; ICD10: R56.0]
Epilepsy; Parkinson's disease [ICD9: 332, 345; ICD10: F02.3, G20, G40]
Epilepsy [ICD10: G40]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Insomnia; Anesthesia [ICD9:307.41, 307.42, 327.0, 780.51, 780.52, 338; ICD10: F51.0, G47.0, R20.0]
Infestations of lice and scabies [ICD9: 132.0, 133.0; ICD10: B85.0, B86]
Monitored anaesthesia care sedation [ICD9: 338; ICD10: R52, G89]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Psychiatric disorder [ICD9: 290-319; ICD10: F01-F99]
Parkinson's disease [ICD9: 332; ICD10: G20]
Schizophrenia [ICD9: 295; ICD10: F20]
Schizophrenia; Pervasive developmental disorder [ICD9: 295, 299; ICD10: F20, F84]
BioChemical Class
Chloride channel
Target Validation
T54128
UniProt ID
P14867||P47869||P47870
Drugs and Mode of Action
Drug(s) Acamprosate Drug Info Approved Alcohol use disorders [537176], [542113]
Aprobarbital Drug Info Approved Insomnia; Anesthesia [535467], [551871]
Barbiturate Drug Info Approved Anaesthesia [536300]
Bromazepam Drug Info Approved Anxiety disorder; Panic attacks [550705]
Desflurane Drug Info Approved Anesthesia [538538], [542164]
Dihydroergotoxine Drug Info Approved Alzheimer disease [534844]
Enflurane Drug Info Approved Anesthesia [538275], [542185]
Fospropofol disodium Drug Info Approved Monitored anaesthesia care sedation [526010], [529941]
Halothane Drug Info Approved Anesthesia [537886], [539530]
Heptabarbital Drug Info Approved Anesthesia [538013]
Isoflurane Drug Info Approved Anesthesia [536300], [539627]
Lindane Drug Info Approved Infestations of lice and scabies [538370]
Sevoflurane Drug Info Approved Anesthesia [536300], [542316]
Zopiclone Drug Info Approved Insomnia [538566], [542453]
FASORACETAM Drug Info Phase 3 Cognitive disorders [545408]
CX-516 Drug Info Phase 2/3 Schizophrenia; Pervasive developmental disorder [467505], [536120]
AZD7325 Drug Info Phase 2 Anxiety disorder [522519], [542687]
Coluracetam Drug Info Phase 2 Alzheimer disease [522235]
CX-1739 Drug Info Phase 2 Attention deficit hyperactivity disorder [548779]
Mibampator Drug Info Phase 2 Alzheimer disease [522580]
Selurampanel Drug Info Phase 2 Epilepsy [523372]
Talampanel Drug Info Phase 2 Epilepsy; Parkinson's disease [536498], [543034]
TRO-19622 Drug Info Phase 2 Chemotherapy-induced peripheral neuropathy [536447], [543190]
AZD-8418 Drug Info Phase 1 Schizophrenia [522881]
Muscimol Drug Info Phase 1 Discovery agent [467594], [522693]
NBQX Drug Info Phase 1 Neurological disease [467600]
TAK-137 Drug Info Phase 1 Psychiatric disorder [524799]
ZK-200775 Drug Info Phase 1 Coronary artery disease [527708], [542619]
CX-1501 Drug Info Preclinical Alzheimer disease [547144]
CX-717 Drug Info Preclinical Alzheimer disease [542783], [547144]
GYKI-47261 Drug Info Preclinical Parkinson's disease [536285]
TP-023 Drug Info Preclinical Anxiety disorder [544186]
TPT-43 Drug Info Preclinical Alzheimer disease [532302]
Becampanel Drug Info Discontinued in Phase 2 Epilepsy [536498]
ELB-139 Drug Info Discontinued in Phase 2 Anxiety disorder [547900]
IPENOXAZONE Drug Info Discontinued in Phase 2 Alzheimer disease [545366]
S-18986 Drug Info Discontinued in Phase 2 Alzheimer disease [467644], [546269]
YM-90K Drug Info Discontinued in Phase 2 Convulsions [545107]
GSK729327 Drug Info Discontinued in Phase 1 Schizophrenia [548489]
S-1746 Drug Info Discontinued in Phase 1 Cerebrovascular ischaemia [547450]
ACEA-2085 Drug Info Terminated Pain [525844]
GYKI-52466 Drug Info Terminated Alzheimer disease [467544], [545950]
GYKI-53655 Drug Info Terminated Discovery agent [467543], [546685]
IDRA-21 Drug Info Terminated Alzheimer disease [467553], [527059]
L-698544 Drug Info Terminated Alzheimer disease [545425]
NS-257 Drug Info Terminated Cerebrovascular ischaemia [545132]
NS-377 Drug Info Terminated Alzheimer disease [545922]
PNQX Drug Info Terminated Cerebrovascular ischaemia [546736]
ZONAMPANEL Drug Info Terminated Discovery agent [546621]
Inhibitor (R,S)-AMPA Drug Info [529714]
(S)-AMPA Drug Info [527890]
(S)-WILLARDIINE Drug Info [534502]
2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) Drug Info [530863]
6-cyano-7-nitroquinoxaline-2,3-dione Drug Info [528135]
7-chloro-3-hydroxyquinazoline-2,4-dione Drug Info [528453]
DNQX Drug Info [534261]
GLUTAMATE Drug Info [530863]
GYKI-52466 Drug Info [527792]
GYKI-53655 Drug Info [534085]
KAINATE Drug Info [529714]
N-(4-hydroxyphenylpropanyl)-spermine Drug Info [530651]
NBQX Drug Info [528721]
Piriqualone Drug Info [525977]
RPR-118723 Drug Info [525816]
YM-90K Drug Info [527219]
ZK-200775 Drug Info [526053]
ZONAMPANEL Drug Info [527219]
Agonist 4,5,6,7-tetrahydroisoxazolo-[5,4-c]-pyridin-3-ol Drug Info [535801]
Acamprosate Drug Info [537464]
AZD7325 Drug Info [550288]
Barbiturate Drug Info [536300]
CX-1739 Drug Info [531966]
Dihydroergotoxine Drug Info [534844]
Isoflurane Drug Info [535407], [536041]
Isoguvacine Drug Info [535527]
Mibampator Drug Info [544383]
Muscimol Drug Info [535527]
Antagonist ACEA-2085 Drug Info [525844]
Becampanel Drug Info [536166], [536498]
Bicuculline Drug Info [535600]
Desflurane Drug Info [535164]
GYKI-47261 Drug Info [536923]
Halothane Drug Info [536495]
Heptabarbital Drug Info [538013]
L-698544 Drug Info [533941]
Lindane Drug Info [536870]
N-methylbicuculline Drug Info [535280]
NS-257 Drug Info [533631]
NS-377 Drug Info [534702]
PNQX Drug Info [545986]
S-1746 Drug Info [528007]
Selurampanel Drug Info [532519]
Sevoflurane Drug Info [537113]
Talampanel Drug Info [536166], [536498], [537081]
TRO-19622 Drug Info [536447]
Binder Aprobarbital Drug Info [535467]
Bromazepam Drug Info [536992]
Zopiclone Drug Info [535660], [535995], [537160]
Modulator AZD-8418 Drug Info [549032]
Coluracetam Drug Info [529446]
CX-1501 Drug Info [528840]
CX-516 Drug Info [536120]
CX-717 Drug Info [531632]
ELB-139 Drug Info [536166]
FASORACETAM Drug Info [551871]
Fospropofol disodium Drug Info [551871]
GSK729327 Drug Info [550963]
IDRA-21 Drug Info [527059]
IPENOXAZONE Drug Info [551871]
LY-392098 Drug Info [467585]
S-18986 Drug Info [536166]
TAK-137 Drug Info [551871]
TP-023 Drug Info [536166]
TPT-43 Drug Info [536166]
Suppressor Enflurane Drug Info [535053]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
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Ref 526010General anesthetic potencies of a series of propofol analogs correlate with potency for potentiation of gamma-aminobutyric acid (GABA) current at the GABA(A) receptor but not with lipid solubility. JPharmacol Exp Ther. 2001 Apr;297(1):338-51.
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 527708The AMPA antagonist ZK 200775 in patients with acute ischaemic stroke: a double-blind, multicentre, placebo-controlled safety and tolerability study. Cerebrovasc Dis. 2005;20(5):304-9. Epub 2005 Aug30.
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Ref 538013A computer program using disposition decomposition analysis in pharmacodynamics. Biopharm Drug Dispos. 1997 Jan;18(1):9-15.
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Ref 525816J Med Chem. 2000 Jun 15;43(12):2371-81.Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
Ref 525844Interaction among NMDA receptor-, NMDA glycine site- and AMPA receptor antagonists in spinally mediated analgesia. Can J Anaesth. 2000 Jul;47(7):693-8.
Ref 525977Bioorg Med Chem Lett. 2001 Jan 22;11(2):177-81.Atropisomeric quinazolin-4-one derivatives are potent noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists.
Ref 526053Bioorg Med Chem Lett. 2001 May 7;11(9):1205-10.Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.
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 527219Bioorg Med Chem Lett. 2004 Oct 18;14(20):5107-11.Synthesis and AMPA receptor antagonistic activity of a novel 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl groupand improved its good physicochemical properties by introduced CF3 group.
Ref 527792Bioorg Med Chem Lett. 2006 Jan 1;16(1):167-70. Epub 2005 Oct 10.New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists.
Ref 527890J Med Chem. 2005 Dec 1;48(24):7867-81.Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
Ref 5280071,026 experimental treatments in acute stroke. Ann Neurol. 2006 Mar;59(3):467-77.
Ref 528135J Med Chem. 2006 Apr 20;49(8):2579-92.Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
Ref 528453J Med Chem. 2006 Oct 5;49(20):6015-26.Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
Ref 528721J Med Chem. 2007 Apr 5;50(7):1558-70. Epub 2007 Mar 10.Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
Ref 528840Pharmacology of ampakine modulators: from AMPA receptors to synapses and behavior. Curr Drug Targets. 2007 May;8(5):583-602.
Ref 529446MKC-231, a choline uptake enhancer: (2) Effect on synthesis and release of acetylcholine in AF64A-treated rats. J Neural Transm. 2008 Jul;115(7):1027-35.
Ref 529714J Med Chem. 2008 Oct 23;51(20):6614-8. Epub 2008 Sep 24.1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.
Ref 530651Bioorg Med Chem. 2010 Feb 15;18(4):1381-7. Epub 2010 Jan 6.Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
Ref 530863J Med Chem. 2010 May 27;53(10):4110-8.4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
Ref 531632Acute sleep deprivation: the effects of the AMPAKINE compound CX717 on human cognitive performance, alertness and recovery sleep. J Psychopharmacol. 2012 Aug;26(8):1047-57.
Ref 531966AMPAKINE enhancement of social interaction in the BTBR mouse model of autism. Neuropharmacology. 2013 Jan;64:268-82.
Ref 532519BGG492 (selurampanel), an AMPA/kainate receptor antagonist drug for epilepsy. Expert Opin Investig Drugs. 2014 Jan;23(1):107-13.
Ref 533631Characterization of the binding of [3H]NS 257, a novel competitive AMPA receptor antagonist, to rat brain membranes and brain sections. J Neurochem. 1995 Sep;65(3):1264-73.
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 534085J Med Chem. 1996 Jan 19;39(2):343-6.Substituted 1,2-dihydrophthalazines: potent, selective, and noncompetitive inhibitors of the AMPA receptor.
Ref 534261J Med Chem. 1996 Oct 25;39(22):4430-8.Synthesis of chiral 1-(2'-amino-2'-carboxyethyl)-1,4-dihydro-6,7-quinoxaline-2,3-diones: alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor agonists and antagonists.
Ref 534502J Med Chem. 1997 Oct 24;40(22):3645-50.Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.
Ref 534702In vivo and in vitro evaluation of AMPA receptor antagonists in rat hippocampal neurones and cultured mouse cortical neurones. Eur J Pharmacol. 1998 Jul 24;353(2-3):159-67.
Ref 534844Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97.
Ref 535053Enflurane directly depresses glutamate AMPA and NMDA currents in mouse spinal cord motor neurons independent of actions on GABAA or glycine receptors. Anesthesiology. 2000 Oct;93(4):1075-84.
Ref 535164Modulation of NMDA receptor function by ketamine and magnesium. Part II: interactions with volatile anesthetics. Anesth Analg. 2001 May;92(5):1182-91.
Ref 535280GABA receptors modulate trigeminovascular nociceptive neurotransmission in the trigeminocervical complex. Br J Pharmacol. 2001 Oct;134(4):896-904.
Ref 535407Effects of GABAergic agents on anesthesia induced by halothane, isoflurane, and thiamylal in mice. Pharmacol Biochem Behav. 2002 May;72(1-2):111-6.
Ref 535467Determination of zidovudine/lamivudine/nevirapine in human plasma using ion-pair HPLC. J Pharm Biomed Anal. 2002 Jun 1;28(5):903-8.
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