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 [1], [2]
Aprobarbital Drug Info Approved Insomnia; Anesthesia [3], [4]
Barbiturate Drug Info Approved Anaesthesia [5]
Bromazepam Drug Info Approved Anxiety disorder; Panic attacks [6]
Desflurane Drug Info Approved Anesthesia [7], [8]
Dihydroergotoxine Drug Info Approved Alzheimer disease [9]
Enflurane Drug Info Approved Anesthesia [10], [11]
Fospropofol disodium Drug Info Approved Monitored anaesthesia care sedation [12], [13]
Halothane Drug Info Approved Anesthesia [14], [15]
Heptabarbital Drug Info Approved Anesthesia [16]
Isoflurane Drug Info Approved Anesthesia [5], [17]
Lindane Drug Info Approved Infestations of lice and scabies [18]
Sevoflurane Drug Info Approved Anesthesia [5], [19]
Zopiclone Drug Info Approved Insomnia [20], [21]
FASORACETAM Drug Info Phase 3 Cognitive disorders [22]
CX-516 Drug Info Phase 2/3 Schizophrenia; Pervasive developmental disorder [23], [24]
AZD7325 Drug Info Phase 2 Anxiety disorder [25], [26]
Coluracetam Drug Info Phase 2 Alzheimer disease [27]
CX-1739 Drug Info Phase 2 Attention deficit hyperactivity disorder [28]
Mibampator Drug Info Phase 2 Alzheimer disease [29]
Selurampanel Drug Info Phase 2 Epilepsy [30]
Talampanel Drug Info Phase 2 Epilepsy; Parkinson's disease [31], [32]
TRO-19622 Drug Info Phase 2 Chemotherapy-induced peripheral neuropathy [33], [34]
AZD-8418 Drug Info Phase 1 Schizophrenia [35]
Muscimol Drug Info Phase 1 Discovery agent [36], [37]
NBQX Drug Info Phase 1 Neurological disease [38]
TAK-137 Drug Info Phase 1 Psychiatric disorder [39]
ZK-200775 Drug Info Phase 1 Coronary artery disease [40], [41]
CX-1501 Drug Info Preclinical Alzheimer disease [42]
CX-717 Drug Info Preclinical Alzheimer disease [43], [42]
GYKI-47261 Drug Info Preclinical Parkinson's disease [44]
TP-023 Drug Info Preclinical Anxiety disorder [45]
TPT-43 Drug Info Preclinical Alzheimer disease [46]
Becampanel Drug Info Discontinued in Phase 2 Epilepsy [31]
ELB-139 Drug Info Discontinued in Phase 2 Anxiety disorder [47]
IPENOXAZONE Drug Info Discontinued in Phase 2 Alzheimer disease [48]
S-18986 Drug Info Discontinued in Phase 2 Alzheimer disease [49], [50]
YM-90K Drug Info Discontinued in Phase 2 Convulsions [51]
GSK729327 Drug Info Discontinued in Phase 1 Schizophrenia [52]
S-1746 Drug Info Discontinued in Phase 1 Cerebrovascular ischaemia [53]
ACEA-2085 Drug Info Terminated Pain [54]
GYKI-52466 Drug Info Terminated Alzheimer disease [55], [56]
GYKI-53655 Drug Info Terminated Discovery agent [57], [58]
IDRA-21 Drug Info Terminated Alzheimer disease [59], [60]
L-698544 Drug Info Terminated Alzheimer disease [61]
NS-257 Drug Info Terminated Cerebrovascular ischaemia [62]
NS-377 Drug Info Terminated Alzheimer disease [63]
PNQX Drug Info Terminated Cerebrovascular ischaemia [64]
ZONAMPANEL Drug Info Terminated Discovery agent [65]
Inhibitor (R,S)-AMPA Drug Info [66]
(S)-AMPA Drug Info [67]
(S)-WILLARDIINE Drug Info [68]
2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) Drug Info [69]
6-cyano-7-nitroquinoxaline-2,3-dione Drug Info [70]
7-chloro-3-hydroxyquinazoline-2,4-dione Drug Info [71]
DNQX Drug Info [72]
GLUTAMATE Drug Info [69]
GYKI-52466 Drug Info [73]
GYKI-53655 Drug Info [74]
KAINATE Drug Info [66]
N-(4-hydroxyphenylpropanyl)-spermine Drug Info [75]
NBQX Drug Info [76]
Piriqualone Drug Info [77]
RPR-118723 Drug Info [78]
YM-90K Drug Info [79]
ZK-200775 Drug Info [80]
ZONAMPANEL Drug Info [79]
Agonist 4,5,6,7-tetrahydroisoxazolo-[5,4-c]-pyridin-3-ol Drug Info [81]
Acamprosate Drug Info [82]
AZD7325 Drug Info [83]
Barbiturate Drug Info [5]
CX-1739 Drug Info [84]
Dihydroergotoxine Drug Info [9]
Isoflurane Drug Info [85], [86]
Isoguvacine Drug Info [87]
Mibampator Drug Info [88]
Muscimol Drug Info [87]
Antagonist ACEA-2085 Drug Info [54]
Becampanel Drug Info [89], [31]
Bicuculline Drug Info [90]
Desflurane Drug Info [91]
GYKI-47261 Drug Info [92]
Halothane Drug Info [93]
Heptabarbital Drug Info [16]
L-698544 Drug Info [94]
Lindane Drug Info [95]
N-methylbicuculline Drug Info [96]
NS-257 Drug Info [97]
NS-377 Drug Info [98]
PNQX Drug Info [99]
S-1746 Drug Info [100]
Selurampanel Drug Info [101]
Sevoflurane Drug Info [102]
Talampanel Drug Info [89], [31], [103]
TRO-19622 Drug Info [33]
Binder Aprobarbital Drug Info [3]
Bromazepam Drug Info [104]
Zopiclone Drug Info [105], [106], [107]
Modulator AZD-8418 Drug Info [108]
Coluracetam Drug Info [109]
CX-1501 Drug Info [110]
CX-516 Drug Info [24]
CX-717 Drug Info [111]
ELB-139 Drug Info [89]
FASORACETAM Drug Info [4]
Fospropofol disodium Drug Info [4]
GSK729327 Drug Info [112]
IDRA-21 Drug Info [60]
IPENOXAZONE Drug Info [4]
LY-392098 Drug Info [113]
S-18986 Drug Info [89]
TAK-137 Drug Info [4]
TP-023 Drug Info [89]
TPT-43 Drug Info [89]
Suppressor Enflurane Drug Info [114]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
REF 1The effects of acamprosate on alcohol-cue reactivity and alcohol priming in dependent patients: a randomized controlled trial. Psychopharmacology (Berl). 2009 Jul;205(1):53-62. Epub 2009 Mar 25.
REF 2(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: 7106).
REF 3Determination of zidovudine/lamivudine/nevirapine in human plasma using ion-pair HPLC. J Pharm Biomed Anal. 2002 Jun 1;28(5):903-8.
REF 4Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 5Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79.
REF 6Drug information of Bromazepam, 2008. eduDrugs.
REF 7FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020118.
REF 8(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: 7156).
REF 9Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97.
REF 10FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074396.
REF 11(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: 7175).
REF 12General 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 132008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
REF 14Benzodiazepine utilisation in Australia: report from a new pharmacoepidemiological database. Aust J Public Health. 1993 Dec;17(4):345-9.
REF 15(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: 2401).
REF 16A computer program using disposition decomposition analysis in pharmacodynamics. Biopharm Drug Dispos. 1997 Jan;18(1):9-15.
REF 17(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: 2505).
REF 18FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 088190.
REF 19(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: 7296).
REF 20FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021476.
REF 21(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: 7430).
REF 22Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003134)
REF 23(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: 4165).
REF 24Autism spectrum disorders: emerging pharmacotherapy. Expert Opin Emerg Drugs. 2005 Aug;10(3):521-36.
REF 25ClinicalTrials.gov (NCT00807937) Proof of Concept in Patients With Generalized Anxiety Disorder (GAD)AZD7325. U.S. National Institutes of Health.
REF 26(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: 7712).
REF 27ClinicalTrials.gov (NCT00621270) Safety and Effectiveness Study of BCI-540 Versus Placebo in the Treatment of Major Depressive Disorder With Concomitant Anxiety. U.S. National Institutes of Health.
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028722)
REF 29ClinicalTrials.gov (NCT00843518) Treatment for Aggression and Agitation in Patients With Alzheimer's Disease. U.S. National Institutes of Health.
REF 30ClinicalTrials.gov (NCT01302873) Study of BGG492 in Patients With Chronic Subjective Tinnitus. U.S. National Institutes of Health.
REF 31Emerging drugs for epilepsy. Expert Opin Emerg Drugs. 2007 Sep;12(3):407-22.
REF 32(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: 8279).
REF 33Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
REF 34(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: 8542).
REF 35ClinicalTrials.gov (NCT01027234) This Study Will Assess the Safety and Tolerability of AZD8418 After Single Increasing Oral Doses. U.S. National Institutes of Health.
REF 36(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: 4259).
REF 37ClinicalTrials.gov (NCT00921128) Convection-Enhanced Delivery to Study the Pathophysiology Underlying the Clinical Features of Parkinson s Disease. U.S. National Institutes of Health.
REF 38(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: 4264).
REF 39ClinicalTrials.gov (NCT02163915) Safety, Tolerability, and Pharmacokinetics of Multiple Rising Doses of TAK-137 in Adults With Attention-Deficit/Hyperactivity Disorder. U.S. National Institutes of Health.
REF 40The 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.
REF 41(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: 7636).
REF 42Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013391)
REF 43(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: 7842).
REF 44Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54.
REF 45Use of multicomponent reactions in developing small-molecule tools to study GABAA receptor mechanism and function. Future Med Chem. 2011 February; 3(2): 243-250.
REF 46Clinical trials with pegylated liposomal Doxorubicin in the treatment of ovarian cancer. J Drug Deliv. 2013;2013:898146.
REF 47Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020261)
REF 48Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003027)
REF 49(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: 4304).
REF 50Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007184)
REF 51Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002155)
REF 52Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025967)
REF 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016496)
REF 54Interaction among NMDA receptor-, NMDA glycine site- and AMPA receptor antagonists in spinally mediated analgesia. Can J Anaesth. 2000 Jul;47(7):693-8.
REF 55(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: 4210).
REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005470)
REF 57(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: 4209).
REF 58Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009633)
REF 59(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 60IDRA-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 61Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003218)
REF 62Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002246)
REF 63Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005356)
REF 64Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010041)
REF 65Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009224)
REF 66J 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 67J Med Chem. 2005 Dec 1;48(24):7867-81.Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
REF 68J 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 69J 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 70J 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 71J 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 72J 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 73Bioorg 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 74J Med Chem. 1996 Jan 19;39(2):343-6.Substituted 1,2-dihydrophthalazines: potent, selective, and noncompetitive inhibitors of the AMPA receptor.
REF 75Bioorg 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 76J 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 77Bioorg 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 78J 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 79Bioorg 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 80Bioorg Med Chem Lett. 2001 May 7;11(9):1205-10.Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.
REF 81Reduction in potency of selective gamma-aminobutyric acidA agonists and diazepam in CA1 region of in vitro hippocampal slices from chronic flurazepam-treated rats. J Pharmacol Exp Ther. 1992 Jul;262(1):204-11.
REF 82Predicting the effect of naltrexone and acamprosate in alcohol-dependent patients using genetic indicators. Addict Biol. 2009 Jul;14(3):328-37.
REF 83Clinical pipeline report, company report or official report of AstraZeneca (2009).
REF 84AMPAKINE enhancement of social interaction in the BTBR mouse model of autism. Neuropharmacology. 2013 Jan;64:268-82.
REF 85Effects of GABAergic agents on anesthesia induced by halothane, isoflurane, and thiamylal in mice. Pharmacol Biochem Behav. 2002 May;72(1-2):111-6.
REF 86Transmembrane residues define the action of isoflurane at the GABAA receptor alpha-3 subunit. Brain Res. 2005 Jan 25;1032(1-2):30-5.
REF 87GABA(A) receptor ligands and their therapeutic potentials. Curr Top Med Chem. 2002 Aug;2(8):817-32.
REF 88Mibampator (LY451395) Randomized Clinical Trial for Agitation/Aggression in Alzheimer's disease. Int Psychogeriatr. 2013 May; 25(5): 707-719.
REF 89Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
REF 90Effects of subcutaneous administration of the gamma-aminobutyric acid(A) receptor agonist muscimol on water intake in water-deprived rats. Physiol Behav. 2002 Nov;77(2-3):445-50.
REF 91Modulation of NMDA receptor function by ketamine and magnesium. Part II: interactions with volatile anesthetics. Anesth Analg. 2001 May;92(5):1182-91.
REF 92Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.
REF 93Reduced inhibition of cortical glutamate and GABA release by halothane in mice lacking the K+ channel, TREK-1. Br J Pharmacol. 2007 Nov;152(6):939-45. Epub 2007 Sep 10.
REF 943-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 95NMDA-induced seizure intensity is enhanced in COX-2 deficient mice. Neurotoxicology. 2008 Nov;29(6):1114-20. Epub 2008 Sep 11.
REF 96GABA receptors modulate trigeminovascular nociceptive neurotransmission in the trigeminocervical complex. Br J Pharmacol. 2001 Oct;134(4):896-904.
REF 97Characterization 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 98In 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 99Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005697)
REF 1001,026 experimental treatments in acute stroke. Ann Neurol. 2006 Mar;59(3):467-77.
REF 101BGG492 (selurampanel), an AMPA/kainate receptor antagonist drug for epilepsy. Expert Opin Investig Drugs. 2014 Jan;23(1):107-13.
REF 102Effects of sevoflurane on carrageenan- and fentanyl-induced pain hypersensitivity in Sprague-Dawley rats. Can J Anaesth. 2009 Feb;56(2):126-35. Epub 2008 Dec 31.
REF 103Talampanel suppresses the acute and chronic effects of seizures in a rodent neonatal seizure model. Epilepsia. 2009 Apr;50(4):694-701. Epub 2009 Feb 12.
REF 104Glutamatergic and GABAergic modulations of ultrasonic vocalizations during maternal separation distress in mouse pups. Psychopharmacology (Berl). 2009 May;204(1):61-71. Epub 2008 Dec 20.
REF 105Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
REF 106The pharmacology and mechanisms of action of new generation, non-benzodiazepine hypnotic agents. CNS Drugs. 2004;18 Suppl 1:9-15; discussion 41, 43-5.
REF 107Eszopiclone: its use in the treatment of insomnia. Neuropsychiatr Dis Treat. 2007 Aug;3(4):441-453.
REF 108Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031633)
REF 109MKC-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 110Pharmacology of ampakine modulators: from AMPA receptors to synapses and behavior. Curr Drug Targets. 2007 May;8(5):583-602.
REF 111Acute 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 112Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
REF 113(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: 4251).
REF 114Enflurane 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.

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