Target Information

Target General Information

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Target ID

T28722 (Former ID: TTDI01774)

Target Name

GABA(A) receptor gamma-3 (GABRG3)

Synonyms

GABRG3

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Gene Name

GABRG3

Target Type

Successful target

[1]

Disease

[+] 9 Target-related Diseases

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

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

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

Epilepsy/seizure [ICD-11: 8A61-8A6Z]

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

Intentional self-harm [ICD-11: PC91]

Labour/delivery anaesthesia complication [ICD-11: JB0C]

Mental/behavioural/neurodevelopmental disorder [ICD-11: 6E20-6E8Z]

Mood/affect symptom [ICD-11: MB24]

Function

Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functionsas receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand- gated chloride channel.

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BioChemical Class

Ligand-gated ion channel

UniProt ID

GBRG3_HUMAN

Sequence

MAPKLLLLLCLFSGLHARSRKVEEDEYEDSSSNQKWVLAPKSQDTDVTLILNKLLREYDK
KLRPDIGIKPTVIDVDIYVNSIGPVSSINMEYQIDIFFAQTWTDSRLRFNSTMKILTLNS
NMVGLIWIPDTIFRNSKTAEAHWITTPNQLLRIWNDGKILYTLRLTINAECQLQLHNFPM
DEHSCPLIFSSYGYPKEEMIYRWRKNSVEAADQKSWRLYQFDFMGLRNTTEIVTTSAGDY
VVMTIYFELSRRMGYFTIQTYIPCILTVVLSWVSFWIKKDATPARTALGITTVLTMTTLS
TIARKSLPRVSYVTAMDLFVTVCFLFVFAALMEYATLNYYSSCRKPTTTKKTTSLLHPDS
SRWIPERISLQAPSNYSLLDMRPPPTAMITLNNSVYWQEFEDTCVYECLDGKDCQSFFCC
YEECKSGSWRKGRIHIDILELDSYSRVFFPTSFLLFNLVYWVGYLYL

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

Drugs and Modes of Action

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Approved Drug(s)

[+] 12 Approved Drugs

Allopregnanolone

Drug Info

Approved

Postpartum depression

[2], [3]

Bentazepam

Drug Info

Approved

Anxiety disorder

[4]

Clobazam - Lundbeck

Drug Info

Approved

Anxiety disorder

[5], [6]

Etomidate

Drug Info

Approved

Anaesthesia

[7], [8]

Flumazenil

Drug Info

Approved

Benzodiazepine overdose

[9], [10]

Mebutamate

Drug Info

Approved

Anxiety disorder

[4]

Metharbital

Drug Info

Approved

Epilepsy

[11], [12]

Remimazolam

Drug Info

Approved

Procedural sedation

[13]

Stiripentol

Drug Info

Approved

Dravet syndrome

[14]

Talbutal

Drug Info

Approved

Irritability

[15]

Thiamylal

Drug Info

Approved

Anaesthesia

[16], [17]

Zolpidem

Drug Info

Approved

Insomnia

[4], [18]

Clinical Trial Drug(s)

[+] 11 Clinical Trial Drugs

Arbaclofen placarbil

Drug Info

Phase 3

Fragile X syndrome

[19]

Clomethiazole

Drug Info

Phase 3

Stroke

[20]

SAGE-217

Drug Info

Phase 3

Postpartum depression

[21]

Pagoclone

Drug Info

Phase 2/3

Anxiety disorder

[22]

Etazolate

Drug Info

Phase 2

Neurodegenerative disorder

[23], [24]

EVT-201

Drug Info

Phase 2

Insomnia

[25]

SARIPIDEM

Drug Info

Phase 2

Anxiety disorder

[26]

T-2007

Drug Info

Phase 2

Epilepsy

[27]

AZD-3043

Drug Info

Phase 1

Anaesthesia

[28]

NSD-788

Drug Info

Phase 1

Anxiety disorder

[29]

Org-25435

Drug Info

Phase 1

Epilepsy

[30]

Discontinued Drug(s)

[+] 21 Discontinued Drugs

Suriclone

Drug Info

Discontinued in Preregistration

Anxiety disorder

[31]

Ocinaplon

Drug Info

Discontinued in Phase 3

Generalized anxiety disorder

[32], [33]

Pazinaclone

Drug Info

Discontinued in Phase 3

Anxiety disorder

[34]

Y-23684

Drug Info

Discontinued in Phase 3

Anxiety disorder

[35]

LORECLEZOLE

Drug Info

Discontinued in Phase 2

Epileptic seizures

[36], [37]

NGD 91-3

Drug Info

Discontinued in Phase 2

Anxiety disorder

[38]

RESEQUINIL

Drug Info

Discontinued in Phase 2

Epilepsy

[39]

RO-48-6791

Drug Info

Discontinued in Phase 2

Anxiety disorder

[40]

SL-65.1498

Drug Info

Discontinued in Phase 2

Anxiety disorder

[41]

Suritozole

Drug Info

Discontinued in Phase 2

Major depressive disorder

[42]

CCD-3693

Drug Info

Discontinued in Phase 1

Anxiety disorder

[43]

CTP-354

Drug Info

Discontinued in Phase 1

Pain

[44]

Org-21465

Drug Info

Discontinued in Phase 1

Anaesthesia

[45]

RO-48-8684

Drug Info

Discontinued in Phase 1

Anxiety disorder

[46]

Co-152791

Drug Info

Terminated

Epilepsy

[48]

Girisopam

Drug Info

Terminated

Anxiety disorder

[49]

NSD-721

Drug Info

Terminated

Anxiety disorder

[50]

Ro-19-8022

Drug Info

Terminated

Anxiety disorder

[51]

RU-33965

Drug Info

Terminated

Alzheimer disease

[52]

ZK-91296

Drug Info

Terminated

Alzheimer disease

[53]

ZK-93426

Drug Info

Terminated

Alzheimer disease

[54], [55]

Preclinical Drug(s)

[+] 1 Preclinical Drugs

RWJ-51204

Drug Info

Preclinical

Anxiety disorder

[47]

Mode of Action

[+] 5 Modes of Action

Modulator

[+] 48 Modulator drugs

Allopregnanolone

Drug Info

[3], [56]

Bentazepam

Drug Info

[1], [4]

Clobazam - Lundbeck

Drug Info

[57]

Etomidate

Drug Info

[57]

Mebutamate

Drug Info

[57]

Metharbital

Drug Info

[57]

Stiripentol

Drug Info

[4], [59]

Talbutal

Drug Info

[57]

Thiamylal

Drug Info

[57]

Clomethiazole

Drug Info

[60]

SAGE-217

Drug Info

[3], [56]

Pagoclone

Drug Info

[61]

Etazolate

Drug Info

[24]

EVT-201

Drug Info

[58]

SARIPIDEM

Drug Info

[26]

AZD-3043

Drug Info

[62]

NSD-788

Drug Info

[58]

Org-25435

Drug Info

[63]

Suriclone

Drug Info

[64]

Ocinaplon

Drug Info

[65]

Pazinaclone

Drug Info

[66]

Y-23684

Drug Info

[67]

LORECLEZOLE

Drug Info

[68]

RO-48-6791

Drug Info

[71]

Suritozole

Drug Info

[73]

CCD-3693

Drug Info

[74]

CTP-354

Drug Info

[75]

Org-21465

Drug Info

[76]

RO-48-8684

Drug Info

[77]

RWJ-51204

Drug Info

[78]

Co-152791

Drug Info

[79]

Girisopam

Drug Info

[80]

NSD-721

Drug Info

[58]

Ro-19-8022

Drug Info

[81]

RU-33965

Drug Info

[82], [83], [84]

ZK-91296

Drug Info

[85]

ZK-93426

Drug Info

[86]

AA-29504

Drug Info

[58]

C-21191

Drug Info

[58]

CP-409092

Drug Info

[87]

DOV-51892

Drug Info

[58]

GIDAZEPAM

Drug Info

[88]

HZ-166

Drug Info

[58]

NGD 96-3

Drug Info

[58]

PNU 101017

Drug Info

[89]

Ro-15-3505

Drug Info

[90]

UC-2024

Drug Info

[58]

UC-2029

Drug Info

[58]

Modulator (allosteric modulator)

[+] 10 Modulator (allosteric modulator) drugs

Flumazenil

Drug Info

[58]

Zolpidem

Drug Info

[58]

alpha3IA

Drug Info

[58]

alpha5IA

Drug Info

[58]

DMCM

Drug Info

[58]

tetrahydrodeoxycorticosterone

Drug Info

[58]

TP003

Drug Info

[58]

[18F]fluoroethylflumazenil

Drug Info

[58]

[3H]CGS8216

Drug Info

[58]

[3H]Ro154513

Drug Info

[58]

Agonist

[+] 9 Agonist drugs

Remimazolam

Drug Info

[13]

Arbaclofen placarbil

Drug Info

[3]

T-2007

Drug Info

[58]

NGD 91-3

Drug Info

[69]

RESEQUINIL

Drug Info

[70]

SL-65.1498

Drug Info

[72]

isonipecotic acid

Drug Info

[58]

JM-1232(-)

Drug Info

[58]

piperidine-4-sulphonic acid

Drug Info

[58]

Blocker (channel blocker)

[+] 2 Blocker (channel blocker) drugs

TBPS

Drug Info

[58]

[35S]TBPS

Drug Info

[58]

Antagonist

[+] 1 Antagonist drugs

UC-1011

Drug Info

[58]

Cell-based Target Expression Variations

Top

Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function. Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006). Human Similarity Proteins Human Pathway Affiliation

Different Human System Profiles of Target

Top

Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.

Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).

Human Similarity Proteins

Human Pathway Affiliation

There is no similarity protein (E value < 0.005) for this target

KEGG Pathway	Pathway ID	Affiliated Target
Neuroactive ligand-receptor interaction	hsa04080	Affiliated Target
Class: Environmental Information Processing => Signaling molecules and interaction	Pathway Hierarchy
Retrograde endocannabinoid signaling	hsa04723	Affiliated Target
Class: Organismal Systems => Nervous system	Pathway Hierarchy
GABAergic synapse	hsa04727	Affiliated Target
Class: Organismal Systems => Nervous system	Pathway Hierarchy

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 Affiliated Biological Pathways

Top

KEGG Pathway

[+] 5 KEGG Pathways

Neuroactive ligand-receptor interaction

Retrograde endocannabinoid signaling

GABAergic synapse

Morphine addiction

Nicotine addiction

Reactome

[+] 2 Reactome Pathways

Ligand-gated ion channel transport

GABA A receptor activation

WikiPathways

[+] 3 WikiPathways

SIDS Susceptibility Pathways

Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell

Iron uptake and transport

References

Top

REF 1

Prodynorphin gene deletion increased anxiety-like behaviours, impaired the anxiolytic effect of bromazepam and altered GABAA receptor subunits gene expression in the amygdala. J Psychopharmacol. 2011Jan;25(1):87-96.

REF 2

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

REF 3

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

REF 4

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

REF 5

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: 7149).

REF 6

Drug information of Clobazam, 2008. eduDrugs.

REF 7

REF 8

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

REF 9

REF 10

ClinicalTrials.gov (NCT00997087) A Randomized, Double-Blind, Placebo-Controlled Trial of Flumazenil for the Treatment of Obsessive Compulsive Disorder. U.S. National Institutes of Health.

REF 11

REF 12

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 008322.

REF 13

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020

REF 14

The effects of stiripentol on GABA(A) receptors.Epilepsia. 2011 Apr;52 Suppl 2:76-8.

REF 15

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009410.

REF 16

REF 17

Drug information of Thiamylal, 2008. eduDrugs.

REF 18

REF 19

ClinicalTrials.gov (NCT01325220) Efficacy and Safety Study of STX209 (Arbaclofen) for the Treatment of Social Withdrawal in Children With Fragile X Syndrome. U.S. National Institutes of Health.

REF 20

ClinicalTrials.gov (NCT02374567) Pharmacovigilance in Gerontopsychiatric Patients. U.S. National Institutes of Health.

REF 21

ClinicalTrials.gov (NCT04442503) A Study to Evaluate the Efficacy and Safety of SAGE-217 in Participants With Severe Postpartum Depression (PPD). U.S. National Institutes of Health.

REF 22

ClinicalTrials.gov (NCT00830154) A Study to Assess the Efficacy and Safety of Pagoclone for Adults With Stuttering. U.S. National Institutes of Health.

REF 23

REF 24

Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing. J Neurochem. 2008 Jul;106(1):392-404.

REF 25

ClinicalTrials.gov (NCT00380003) Efficacy Study of EVT 201 to Treat Insomnia. U.S. National Institutes of Health.

REF 26

Behavioural effects of novel benzodiazepine (omega) receptor agonists and partial agonists: increases in punished responding and antagonism of the pentylenetetrazole cue. Behav Pharmacol. 1995 Mar;6(2):116-126.

REF 27

ClinicalTrials.gov (NCT00939653) T2007-002 Clofarabine, Etoposide, Cyclophosphamide in Relapsed Acute Myelogenous Leukemia (AML). U.S. National Institutes of Health.

REF 28

ClinicalTrials.gov (NCT01086813) Phase I, Single Centre, Study to Assess Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of AZD3043. U.S. National Institutes of Health.

REF 29

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028006)

REF 30

ClinicalTrials.gov (NCT01062867) First Administration to Man Of Org 25435 a New Intravenous Anesthetic. U.S. National Institutes of Health.

REF 31

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000574)

REF 32

REF 33

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001407)

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 800000717)

REF 35

The pharmacological properties of Y-23684, a benzodiazepine receptor partial agonist.. Br J Pharmacol. 1994 April; 111(4): 1170-1178.

REF 36

REF 37

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007906)

REF 38

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011480)

REF 39

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010724)

REF 40

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007556)

REF 41

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014726)

REF 42

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001322)

REF 43

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006723)

REF 44

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038187)

REF 45

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006459)

REF 46

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007572)

REF 47

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015754)

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 800011029)

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 800005437)

REF 50

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010233)

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 800001584)

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 800001729)

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 800000552)

REF 54

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 800001474)

REF 56

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

REF 57

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

REF 58

REF 59

Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16.

REF 60

Electrophysiological actions of gamma-aminobutyric acid and clomethiazole on recombinant GABA(A) receptors. Eur J Pharmacol. 2002 Oct 11;452(3):255-62.

REF 61

Evaluation of the abuse potential of pagoclone, a partial GABAA agonist. J Clin Psychopharmacol. 2006 Jun;26(3):268-73.

REF 62

AZD-3043: a novel, metabolically labile sedative-hypnotic agent with rapid and predictable emergence from hypnosis. Anesthesiology. 2012 Jun;116(6):1267-77.

REF 63

First administration to man of Org 25435, an intravenous anaesthetic: A Phase 1 Clinical Trial. BMC Anesthesiol. 2010 Jun 29;10:10.

REF 64

The effect of cyclopyrrolones on GABAA receptor function is different from that of benzodiazepines. Naunyn Schmiedebergs Arch Pharmacol. 1994 Sep;350(3):294-300.

REF 65

Discriminative stimulus properties of GABAA receptor positive allosteric modulators TPA023, ocinaplon and NG2-73 in rats trained to discriminate chlordiazepoxide or zolpidem. Eur J Pharmacol. 2011 Oct 1;668(1-2):190-3.

REF 66

The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. Expert Opin Investig Drugs. 2005 May;14(5):601-18.

REF 67

The pharmacological properties of Y-23684, a benzodiazepine receptor partial agonist. Br J Pharmacol. 1994 Apr;111(4):1170-8.

REF 68

Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit. Neuropharmacology. 1996;35(12):1753-60.

REF 69

Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Curr Drug Targets CNS Neurol Disord. 2003 Aug;2(4):213-32.

REF 70

WO patent application no. 2010,0024,51, Naphthyridin derivatives.

REF 71

Integrated pharmacokinetics and pharmacodynamics of Ro 48-6791, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects. Br J Clin Pharmacol. 1997 Nov;44(5):477-86.

REF 72

WO patent application no. 2005,0749,31, Pharmaceutical combinations comprising (s) -pantoprazole.

REF 73

Chronic postinjury administration of MDL 26,479 (Suritozole), a negative modulator at the GABAA receptor, and cognitive impairment in rats following traumatic brain injury. J Neurosurg. 1995 Nov;83(5):878-83.

REF 74

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

REF 75

Clinical pipeline report, company report or official report of Concert Pharmaceuticals.

REF 76

Computer-controlled infusion of ORG 21465, a water soluble steroid i.v. anaesthetic agent, into human volunteers. Br J Anaesth. 1997 Oct;79(4):433-9.

REF 77

Integrated pharmacokinetics and pharmacodynamics of Ro 48-8684, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects. Br J Clin Pharmacol. 1997 Nov;44(5):487-93.

REF 78

5-ethoxymethyl-7-fluoro-3-oxo-1,2,3,5-tetrahydrobenzo[4,5]imidazo[1,2a]pyridine-4-N-(2-fluorophenyl)carboxamide (RWJ-51204), a new nonbenzodiazepine anxiolytic. J Pharmacol Exp Ther. 2002 Nov;303(2):777-90.

REF 79

Substituted 3beta-phenylethynyl derivatives of 3alpha-hydroxy-5alpha-pregnan-20-one: remarkably potent neuroactive steroid modulators of gamma-aminobutyric acidA receptors. J Pharmacol Exp Ther. 1998Oct;287(1):198-207.

REF 80

[(3)H]-girisopam, a novel selective benzodiazepine for the 2, 3-benzodiazepine binding site. Brain Res Brain Res Protoc. 1999 Jul;4(2):230-5.

REF 81

Partial agonist of benzodiazepine receptors Ro 19-8022 elicits withdrawal symptoms after short-term administration in immature rats. Physiol Res. 2012;61(3):319-23.

REF 82

Discriminative stimulus properties of RU 33965, a benzodiazepine receptor weak partial inverse agonist. Pharmacol Biochem Behav. 1992 Oct;43(2):583-8.

REF 83

The effects of RU 33965 and RU 34030, two new 3-cyclopropyl carbonyl imidazobenzodiazepines, on GABAA receptor-mediated synaptic transmission in ce... Gen Pharmacol. 1994 May;25(3):589-97.

REF 84

Effects of benzodiazepine receptor inverse agonists and nicotine on behavioral vigilance in senescent rats. J Gerontol A Biol Sci Med Sci. 1996 May;51(3):B225-31.

REF 85

Enhancement of gamma-aminobutyric acid binding by the anxiolytic beta-carbolines ZK 93423 and ZK 91296. J Neurochem. 1987 May;48(5):1355-8.

REF 86

Actions of the beta-carboline ZK 93426 in an animal test of anxiety and the holeboard: interactions with Ro 15-1788. J Neural Transm. 1986;65(2):103-14.

REF 87

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

REF 88

Discriminative effects of phenazepam and gidazepam in rats: comparison with other GABA-related drugs. Pharmacol Biochem Behav. 1999 Oct;64(2):397-401.

REF 89

Neuroprotective effects of the GABA(A) receptor partial agonist U-101017 in 3-acetylpyridine-treated rats. Neurosci Lett. 1997 May 30;228(1):45-9.

REF 90

Molecular structure and stereoelectronic properties of sarmazenil--a weak inverse agonist at the omega modulatory sites (benzodiazepine receptors):... Bioorg Med Chem. 1998 Oct;6(10):1745-57.

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