GABAA Receptors

GABAA receptors are members of the Cys-loop family of ligand-gated ion channels and, along with GABAB receptors, are responsible for mediating the inhibitory effects of GABA. They are pentameric proteins, consisting of five subunits belonging to different families.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
3618 Acamprosate calcium
GABA agonist and glutamatergic modulator
2991 DPNI-caged-GABA
Nitroindoline-caged GABA
0344 GABA
Endogenous agonist
0235 Isoguvacine hydrochloride
Selective GABAA agonist
3250 L-838,417
Subtype-selective GABAA partial agonist
4415 MK 0343
Subtype-selective GABAA receptor partial agonist
3817 MRK 016
α5-selective GABAA inverse agonist
0289 Muscimol
Potent GABAA agonist
4709 RuBi GABA trimethylphosphine
Caged GABA; inhibits neural activity
0181 TACA
GABAA agonist. Also GABA-T substrate and GABA uptake inhibitor
3941 TCS 1205
Subtype-selective GABAA receptor agonist
0807 THIP hydrochloride
GABAA agonist
4414 TP 003
Functionally selective GABAA receptor (α3 subtype) partial agonist
0180 ZAPA sulfate
Agonist at 'low affinity' GABAA receptor. More potent than GABA/muscimol

Antagonists

Cat No Product Name / Activity
2503 (-)-Bicuculline methiodide
Water-soluble GABAA antagonist
0109 (-)-Bicuculline methobromide
Water-soluble GABAA antagonist
0131 (-)-Bicuculline methochloride
Water-soluble GABAA antagonist
0130 (+)-Bicuculline
Potent GABAA antagonist
3109 Furosemide
GABAA receptor antagonist. Also Na+/2Cl-/K+ cotransporter blocker
4466 PHP 501 trifluoroacetate
Potent GABAA antagonist
1128 Picrotoxin
GABAA receptor antagonist
2143 SCS
Selective GABAA receptor antagonist; β1-subunit-selective
1262 SR 95531 hydrobromide
Selective, competitive GABAA receptor antagonist
2905 TB 21007
α5-selective GABAA inverse agonist
2745 U 93631
GABAA receptor antagonist

Benzodiazepines

Cat No Product Name / Activity
5281 AC 5216
Selective TSPO ligand
3568 Bretazenil
Benzodiazepine partial agonist
0405 β-CCB
Benzodiazepine inverse agonist, putative endogenous ligand
2467 CGS 20625
Selective central benzodiazepine receptor partial agonist
0456 Chlormezanone
Skeletal muscle relaxant
1709 CL 218872
Benzodiazepine agonist
2805 Diazepam
Acts at the benzodiazepine modulatory site
0505 Dihydroergotoxine mesylate
Binds to GABAA receptor Cl- channel; allosteric modulator of benzodiazepine site
3083 DMCM hydrochloride
Benzodiazepine inverse agonist
0554 FG 7142
Benzodiazepine inverse agonist
0658 FGIN-1-27
Potent, specific ligand for mitochondrial DBI receptor
0659 FGIN-1-43
Potent, specific ligand for mitochondrial DBI receptor
1328 Flumazenil
Benzodiazepine antagonist
4047 Flunitrazepam
Acts at the benzodiazepene modulatory site
2174 Hispidulin
Partial positive allosteric modulator at the benzodiazepine receptor
1327 L-655,708
Benzodiazepine inverse agonist; selective for α5-containing GABAA receptors
3087 Lorazepam
Acts at the benzodiazepine modulatory site
2832 Midazolam hydrochloride
Benzodiazepine agonist
0670 PK 11195
Antagonist at peripheral benzodiazepine receptors
1997 Ro 15-4513
Benzodiazepine partial inverse agonist
1995 Ro 19-4603
Benzodiazepine inverse agonist
3942 TCS 1105
GABAA α2 benzodiazepine receptor agonist
3655 Zaleplon
Benzodiazepine site agonist
1994 ZK 93423 hydrochloride
Potent benzodiazepine agonist
1996 ZK 93426 hydrochloride
Potent, competitive benzodiazepine antagonist
0655 Zolpidem
Benzodiazepine agonist
1094 Zopiclone
Benzodiazepine agonist

Modulators

Cat No Product Name / Activity
3972 AA 29504
Positive allosteric modulator of GABAA receptors
3653 Allopregnanolone
GABAA receptor positive allosteric modulator
3046 Alphaxalone
Direct activator and potentiator of GABAA
0881 Chlormethiazole hydrochloride
Potentiates GABAA receptor function
3679 DS2
Positive allosteric modulator of δ-containing GABAA receptors
3113 Etifoxine hydrochloride
Potentiator of GABAA receptors; anxiolytic
1471 Etomidate
GABA mimetic and GABA modulatory agent
2867 Flupirtine maleate
Modulates GABAA receptors
2531 Ganaxolone
Potent, positive allosteric modulator of GABAA receptors
3597 Indiplon
Subtype-selective GABAA receptor positive allosteric modulator
1295 Loreclezole hydrochloride
Subtype-selective GABAA receptor modulator
4949 MaxiPost
Potassium channel modulator; negative modulator of GABAA receptors
4410 Ocinaplon
GABAA modulator; anxiolytic
2738 Org 20599
Positive allosteric modulator and direct agonist of GABAA receptors
2681 17-PA
Antagonist of neurosteroid potentiation and direct gating of GABAA
3652 Pregnanolone
GABAA receptor positive allosteric modulator
0830 Primidone
Potentiates GABAA receptor function
1512 SB 205384
GABAA receptor modulator; slows current decay
3620 Topiramate
GABAA receptor positive allosteric modulator. Also GluR5 antagonist
1558 Tracazolate hydrochloride
Subtype-selective GABAA allosteric modulator
2734 U 89843A
Positive allosteric modulator of GABAA receptors
2733 U 90042
GABAA receptor ligand
3048 Valerenic acid
Positive allosteric modulator of GABAA receptors

GABAA receptors are members of the Cys-loop family of ligand-gated ion channels, responsible for mediating the inhibitory effects of GABA alongside GABAB and GABAA-ρ receptors. They are heteromeric pentamers, consisting of five subunits belonging to different families (α1-6, β1-3, γ1-3, δ, π, ε, θ).

The most abundant GABAA receptor in the mammalian brain consists of two copies each of subunits α1 and β2 with a single γ2 subunit. GABAA receptors contain an integral chloride channel, and have modulatory sites for benzodiazepines, barbiturates, neurosteroids and ethanol.

External sources of pharmacological information for GABAA Receptors :

    Literature for GABAA Receptors

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    GABAA Receptor Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    GABAA α1 Human GABRA1 NM_001127645 P14867
    Mouse Gabra1 NM_010250 P62812
    Rat Gabra1 NM_183326 P62813
    GABAA α2 Human GABRA2 NM_000807 P47869
    Mouse Gabra2 NM_008066 P26048
    Rat Gabra2 L08491 P23576
    GABAA α3 Human GABRA3 NM_000808 P34903
    Mouse Gabra3 NM_008067 P26049
    Rat Gabra3 NM_017069 P20236
    GABAA α4 Human GABRA4 NM_000809 P48169
    Mouse Gabra4 NM_010251 Q9D6F4
    Rat Gabra4 NM_080587 P28471
    GABAA α5 Human GABRA5 XM_001123369 P31644
    Mouse Gabra5 NM_176942 Q8BHJ7
    Rat Gabra5 NM_017295 P19969
    GABAA α6 Human GABRA6 NM_000811 Q16445
    Mouse Gabra6 NM_001099641 P16305
    Rat Gabra6 NM_021841 P30191
    GABAA β1 Human GABRB1 NM_000812 P18505
    Mouse Gabrb1 NM_008069 P50571
    Rat Gabrb1 NM_012956 P15431
    GABAA β2 Human GABRB2 NM_021911 P47870
    Mouse Gabrb2 NM_008070 P63137
    Rat Gabrb2 NM_012957 P63138
    GABAA β3 Human GABRb3 NM_000814 P28472
    Mouse Gabrb3 NM_008071 P63080
    Rat Gabrb3 NM_017065 P63079
    GABAA γ1 Human GABRG1 NM_173536 Q8N1C3
    Mouse Gabrg1 NM_010252 Q9R0Y8
    Rat Gabrg1 NM_080586 P23574
    GABAA γ2 Human GABRG2 NM_198903 P18507
    Mouse Gabrg2 NM_177408 P22723
    Rat Gabrg2 NM_183327 P18508
    GABAA γ3 Human GABRG3 NM_033223 Q99928
    Mouse Gabrg3 NM_008074 P27681
    Rat Gabrg3 NM_024370 P28473
    GABAA δ Human GABRD NM_000815 O14764
    Mouse Gabrd NM_008072 P22933
    Rat Gabrd NM_017289 P18506
    GABAA ε Human GABRE NM_004961 P78334
    Mouse Gabre NM_017369 NP_059065
    Rat Gabre NM_023091 Q9ES14
    GABAA π Human GABRP NM_014211 O00591
    Mouse Gabrp NM_146017 Q8QZW7
    Rat Gabrp NM_031029 O09028
    GABAA θ Human GABRQ NM_018558 Q9UN88
    Mouse Gabrq NM_020488 Q9JLF1
    Rat Gabrq NM_031733 O09028