GABAA Receptors

More Information »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.

GABAA Receptor Products

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
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
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
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

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