Target Information

Target General Information

Top

Target ID

T54128 (Former ID: TTDS00121)

Target Name

Glutamate receptor AMPA (GRIA)

Synonyms

Glutamate receptor ionotropic, AMPA; Glutamate receptor; AMPA selective glutamate receptor; AMPA receptor

Click to Show/Hide

Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 11 Target-related Diseases

Alzheimer disease [ICD-11: 8A20]

Anxiety disorder [ICD-11: 6B00-6B0Z]

Appearance/behaviour symptom [ICD-11: MB23]

Corneal disease [ICD-11: 9A76-9A78]

Depression [ICD-11: 6A70-6A7Z]

Insomnia [ICD-11: 7A00-7A0Z]

Malaria [ICD-11: 1F40-1F45]

Monitored anaesthesia care [ICD-11: N.A.]

Neuropathy [ICD-11: 8C0Z]

Pediculosis [ICD-11: 1G00]

Substance abuse [ICD-11: 6C40]

BioChemical Class

Chloride channel

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 16 Approved Drugs

Acamprosate

Drug Info

Approved

Alcohol dependence

[2], [3]

Aprobarbital

Drug Info

Approved

Anaesthesia

[4], [5]

Artemisinin SP

Drug Info

Approved

Malaria

[6]

Barbiturate

Drug Info

Approved

Depression

[7]

Bromazepam

Drug Info

Approved

Panic attacks

[8]

Desflurane

Drug Info

Approved

Anaesthesia

[9], [10]

Dihydroergotoxine

Drug Info

Approved

Alzheimer disease

[11]

E-2007

Drug Info

Approved

Diabetic neuropathy

[12], [13]

Enflurane

Drug Info

Approved

Anaesthesia

[14], [15]

Fospropofol disodium

Drug Info

Approved

Monitored anaesthesia care

[16], [17]

Halothane

Drug Info

Approved

Anaesthesia

[18], [19]

Heptabarbital

Drug Info

Approved

Anaesthesia

[20]

Isoflurane

Drug Info

Approved

Anaesthesia

[21], [22]

Lindane

Drug Info

Approved

Infestations of lice and scabies

[23]

Sevoflurane

Drug Info

Approved

Anaesthesia

[22], [24]

Zopiclone

Drug Info

Approved

Insomnia

[25], [26]

Clinical Trial Drug(s)

[+] 18 Clinical Trial Drugs

FASORACETAM

Drug Info

Phase 3

Cognitive impairment

[27]

CX-516

Drug Info

Phase 2/3

Pervasive developmental disorder

[28], [29]

BIIB104

Drug Info

Phase 2a

Cognitive impairment

[30]

AZD7325

Drug Info

Phase 2

Anxiety disorder

[31], [32]

Coluracetam

Drug Info

Phase 2

Alzheimer disease

[33]

CX-1739

Drug Info

Phase 2

Attention deficit hyperactivity disorder

[34]

CX-717

Drug Info

Phase 2

Spinal cord injury

[35]

CX1789

Drug Info

Phase 2

Obstructive sleep apnea

[35]

Mibampator

Drug Info

Phase 2

Alzheimer disease

[36]

PF-04958242

Drug Info

Phase 2

Schizophrenia

[30], [37]

Selurampanel

Drug Info

Phase 2

Epilepsy

[38]

TAK-653

Drug Info

Phase 2

Depression

[30]

Talampanel

Drug Info

Phase 2

Parkinson disease

[39], [40]

TRO-19622

Drug Info

Phase 2

Peripheral neuropathy

[41], [42]

AZD-8418

Drug Info

Phase 1

Schizophrenia

[43]

NBQX

Drug Info

Phase 1

Neurological disorder

[44]

TAK-137

Drug Info

Phase 1

Psychiatric disorder

[45]

ZK-200775

Drug Info

Phase 1

Coronary artery disease

[46], [47]

Discontinued Drug(s)

[+] 14 Discontinued Drugs

Becampanel

Drug Info

Discontinued in Phase 2

Epilepsy

[40]

ELB-139

Drug Info

Discontinued in Phase 2

Anxiety disorder

[48]

IPENOXAZONE

Drug Info

Discontinued in Phase 2

Alzheimer disease

[49]

S-18986

Drug Info

Discontinued in Phase 2

Alzheimer disease

[50], [51]

YM-90K

Drug Info

Discontinued in Phase 2

Convulsion

[52]

GSK729327

Drug Info

Discontinued in Phase 1

Schizophrenia

[53]

S-1746

Drug Info

Discontinued in Phase 1

Cerebrovascular ischaemia

[54]

ACEA-2085

Drug Info

Terminated

Pain

[60]

GYKI-52466

Drug Info

Terminated

Alzheimer disease

[61], [62]

IDRA-21

Drug Info

Terminated

Alzheimer disease

[63], [64]

L-698544

Drug Info

Terminated

Alzheimer disease

[65]

NS-257

Drug Info

Terminated

Cerebrovascular ischaemia

[66]

NS-377

Drug Info

Terminated

Alzheimer disease

[67]

PNQX

Drug Info

Terminated

Cerebrovascular ischaemia

[68]

Preclinical Drug(s)

[+] 5 Preclinical Drugs

BIIR-777

Drug Info

Preclinical

Neurological disorder

[55]

CX-1501

Drug Info

Preclinical

Alzheimer disease

[56]

GYKI-47261

Drug Info

Preclinical

Parkinson disease

[57]

TP-023

Drug Info

Preclinical

Anxiety disorder

[58]

TPT-43

Drug Info

Preclinical

Alzheimer disease

[59]

Mode of Action

[+] 7 Modes of Action

Agonist

[+] 11 Agonist drugs

Acamprosate

Drug Info

[69]

Artemisinin SP

Drug Info

[70]

Barbiturate

Drug Info

[22]

Dihydroergotoxine

Drug Info

[11]

Isoflurane

Drug Info

[75], [76]

AZD7325

Drug Info

[81]

CX-1739

Drug Info

[83]

CX1789

Drug Info

[35]

Mibampator

Drug Info

[85]

4,5,6,7-tetrahydroisoxazolo-[5,4-c]-pyridin-3-ol

Drug Info

[107]

Muscimol

Drug Info

[70]

Binder

[+] 3 Binder drugs

Aprobarbital

Drug Info

[4]

Bromazepam

Drug Info

[71]

Zopiclone

Drug Info

[1], [79], [80]

Antagonist

[+] 18 Antagonist drugs

Desflurane

Drug Info

[72]

Halothane

Drug Info

[74]

Heptabarbital

Drug Info

[20]

Lindane

Drug Info

[77]

Sevoflurane

Drug Info

[78]

Selurampanel

Drug Info

[86]

Talampanel

Drug Info

[40], [87], [88]

TRO-19622

Drug Info

[42]

Becampanel

Drug Info

[40], [88]

S-1746

Drug Info

[94]

GYKI-47261

Drug Info

[97]

ACEA-2085

Drug Info

[60]

L-698544

Drug Info

[100]

NS-257

Drug Info

[101]

NS-377

Drug Info

[102]

PNQX

Drug Info

[103]

Bicuculline

Drug Info

[109]

N-methylbicuculline

Drug Info

[114]

Modulator

[+] 19 Modulator drugs

E-2007

Drug Info

[13]

Fospropofol disodium

Drug Info

[5]

FASORACETAM

Drug Info

[5]

CX-516

Drug Info

[29]

Coluracetam

Drug Info

[82]

CX-717

Drug Info

[84]

AZD-8418

Drug Info

[89]

TAK-137

Drug Info

[5]

ELB-139

Drug Info

[88]

IPENOXAZONE

Drug Info

[5]

S-18986

Drug Info

[88]

GSK729327

Drug Info

[93]

BIIR-777

Drug Info

[95]

CX-1501

Drug Info

[96]

TP-023

Drug Info

[88]

TPT-43

Drug Info

[88]

IDRA-21

Drug Info

[64]

LY-314657

Drug Info

[111]

LY-392098

Drug Info

[112]

Suppressor

[+] 1 Suppressor drugs

Enflurane

Drug Info

[73]

Activator

[+] 3 Activator drugs

BIIB104

Drug Info

[30]

PF-04958242

Drug Info

[30]

TAK-653

Drug Info

[30]

Inhibitor

[+] 16 Inhibitor drugs

NBQX

Drug Info

[90]

ZK-200775

Drug Info

[91]

YM-90K

Drug Info

[92]

GYKI-52466

Drug Info

[98]

GYKI-53655

Drug Info

[99]

Zonampanel

Drug Info

[92]

(S)-AMPA

Drug Info

[104]

(S)-WILLARDIINE

Drug Info

[105]

2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX)

Drug Info

[106]

7-chloro-3-hydroxyquinazoline-2,4-dione

Drug Info

[108]

DNQX

Drug Info

[110]

N-(4-hydroxyphenylpropanyl)-spermine

Drug Info

[113]

Piriqualone

Drug Info

[115]

RPR-118723

Drug Info

[116]

[3H]CNQX

Drug Info

[117]

[3H]kainate

Drug Info

[118]

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

Target QSAR Model

References

Top

REF 1

Eszopiclone: its use in the treatment of insomnia. Neuropsychiatr Dis Treat. 2007 Aug;3(4):441-453.

REF 2

URL: 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 3

The 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.

REF 4

Determination of zidovudine/lamivudine/nevirapine in human plasma using ion-pair HPLC. J Pharm Biomed Anal. 2002 Jun 1;28(5):903-8.

REF 5

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 6

The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71.

REF 7

DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.

REF 8

Drug information of Bromazepam, 2008. eduDrugs.

REF 9

REF 10

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020118.

REF 11

Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97.

REF 12

REF 13

Nat Rev Drug Discov. 2013 Feb;12(2):87-90.

REF 14

REF 15

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074396.

REF 16

2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.

REF 17

General 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 18

REF 19

Benzodiazepine utilisation in Australia: report from a new pharmacoepidemiological database. Aust J Public Health. 1993 Dec;17(4):345-9.

REF 20

A computer program using disposition decomposition analysis in pharmacodynamics. Biopharm Drug Dispos. 1997 Jan;18(1):9-15.

REF 21

REF 22

Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79.

REF 23

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 088190.

REF 24

REF 25

REF 26

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021476.

REF 27

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003134)

REF 28

REF 29

Autism spectrum disorders: emerging pharmacotherapy. Expert Opin Emerg Drugs. 2005 Aug;10(3):521-36.

REF 30

Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.

REF 31

REF 32

ClinicalTrials.gov (NCT00807937) Proof of Concept in Patients With Generalized Anxiety Disorder (GAD)AZD7325. U.S. National Institutes of Health.

REF 33

ClinicalTrials.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 34

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028722)

REF 35

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 36

ClinicalTrials.gov (NCT00843518) Treatment for Aggression and Agitation in Patients With Alzheimer's Disease. U.S. National Institutes of Health.

REF 37

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 38

ClinicalTrials.gov (NCT01302873) Study of BGG492 in Patients With Chronic Subjective Tinnitus. U.S. National Institutes of Health.

REF 39

REF 40

Emerging drugs for epilepsy. Expert Opin Emerg Drugs. 2007 Sep;12(3):407-22.

REF 41

REF 42

Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.

REF 43

ClinicalTrials.gov (NCT01027234) This Study Will Assess the Safety and Tolerability of AZD8418 After Single Increasing Oral Doses. U.S. National Institutes of Health.

REF 44

REF 45

ClinicalTrials.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 46

REF 47

The 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.

REF 48

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020261)

REF 49

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003027)

REF 50

REF 51

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007184)

REF 52

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002155)

REF 53

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025967)

REF 54

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016496)

REF 55

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025224)

REF 56

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013391)

REF 57

Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54.

REF 58

Use 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 59

Clinical trials with pegylated liposomal Doxorubicin in the treatment of ovarian cancer. J Drug Deliv. 2013;2013:898146.

REF 60

Interaction among NMDA receptor-, NMDA glycine site- and AMPA receptor antagonists in spinally mediated analgesia. Can J Anaesth. 2000 Jul;47(7):693-8.

REF 61

REF 62

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005470)

REF 63

REF 64

IDRA-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 65

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003218)

REF 66

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002246)

REF 67

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005356)

REF 68

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010041)

REF 69

Predicting the effect of naltrexone and acamprosate in alcohol-dependent patients using genetic indicators. Addict Biol. 2009 Jul;14(3):328-37.

REF 70

GABA(A) receptor ligands and their therapeutic potentials. Curr Top Med Chem. 2002 Aug;2(8):817-32.

REF 71

Glutamatergic and GABAergic modulations of ultrasonic vocalizations during maternal separation distress in mouse pups. Psychopharmacology (Berl). 2009 May;204(1):61-71.

REF 72

Modulation of NMDA receptor function by ketamine and magnesium. Part II: interactions with volatile anesthetics. Anesth Analg. 2001 May;92(5):1182-91.

REF 73

Enflurane 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 74

Reduced 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.

REF 75

Transmembrane residues define the action of isoflurane at the GABAA receptor alpha-3 subunit. Brain Res. 2005 Jan 25;1032(1-2):30-5.

REF 76

Effects of GABAergic agents on anesthesia induced by halothane, isoflurane, and thiamylal in mice. Pharmacol Biochem Behav. 2002 May;72(1-2):111-6.

REF 77

NMDA-induced seizure intensity is enhanced in COX-2 deficient mice. Neurotoxicology. 2008 Nov;29(6):1114-20.

REF 78

Effects of sevoflurane on carrageenan- and fentanyl-induced pain hypersensitivity in Sprague-Dawley rats. Can J Anaesth. 2009 Feb;56(2):126-35.

REF 79

The 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 80

Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.

REF 81

Clinical pipeline report, company report or official report of AstraZeneca (2009).

REF 82

MKC-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 83

AMPAKINE enhancement of social interaction in the BTBR mouse model of autism. Neuropharmacology. 2013 Jan;64:268-82.

REF 84

Acute 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 85

Mibampator (LY451395) Randomized Clinical Trial for Agitation/Aggression in Alzheimer's disease. Int Psychogeriatr. 2013 May; 25(5): 707-719.

REF 86

BGG492 (selurampanel), an AMPA/kainate receptor antagonist drug for epilepsy. Expert Opin Investig Drugs. 2014 Jan;23(1):107-13.

REF 87

Talampanel suppresses the acute and chronic effects of seizures in a rodent neonatal seizure model. Epilepsia. 2009 Apr;50(4):694-701.

REF 88

Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.

REF 89

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031633)

REF 90

Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil r... J Med Chem. 2007 Apr 5;50(7):1558-70.

REF 91

Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz. Bioorg Med Chem Lett. 2001 May 7;11(9):1205-10.

REF 92

Synthesis and AMPA receptor antagonistic activity of a novel 7-imidazolyl-6-trifluoromethyl quinoxalinecarboxylic acid with a substituted phenyl gr... Bioorg Med Chem Lett. 2004 Oct 18;14(20):5107-11.

REF 93

Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).

REF 94

1,026 experimental treatments in acute stroke. Ann Neurol. 2006 Mar;59(3):467-77.

REF 95

Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

REF 96

Pharmacology of ampakine modulators: from AMPA receptors to synapses and behavior. Curr Drug Targets. 2007 May;8(5):583-602.

REF 97

Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.

REF 98

New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists. Bioorg Med Chem Lett. 2006 Jan 1;16(1):167-70.

REF 99

Substituted 1,2-dihydrophthalazines: potent, selective, and noncompetitive inhibitors of the AMPA receptor. J Med Chem. 1996 Jan 19;39(2):343-6.

REF 100

3-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 101

Characterization 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 102

In 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 103

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005697)

REF 104

Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. J Med Chem. 2005 Dec 1;48(24):7867-81.

REF 105

Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes. J Med Chem. 1997 Oct 24;40(22):3645-50.

REF 106

4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological charact... J Med Chem. 2010 May 27;53(10):4110-8.

REF 107

Reduction 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 108

Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Syn... J Med Chem. 2006 Oct 5;49(20):6015-26.

REF 109

Effects 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 110

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 recep... J Med Chem. 1996 Oct 25;39(22):4430-8.

REF 111

The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.

REF 112

REF 113

Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands. Bioorg Med Chem. 2010 Feb 15;18(4):1381-7.

REF 114

GABA receptors modulate trigeminovascular nociceptive neurotransmission in the trigeminocervical complex. Br J Pharmacol. 2001 Oct;134(4):896-904.

REF 115

Atropisomeric quinazolin-4-one derivatives are potent noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antag... Bioorg Med Chem Lett. 2001 Jan 22;11(2):177-81.

REF 116

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. J Med Chem. 2000 Jun 15;43(12):2371-81.

REF 117

Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists. J Med Chem. 2006 Apr 20;49(8):2579-92.

REF 118

1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of pot... J Med Chem. 2008 Oct 23;51(20):6614-8.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.

Prof. Feng ZHU

Prof. Yuzong CHEN