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GABAA Receptors
More Information »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 GABAC receptors. They are pentameric proteins, consisting of 5 subunits belonging to different families.
GABAA Receptor Products
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 |
| 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 | |
| 0770 | GBLD 345 |
| High affinity benzodiazepine agonist | |
| 2174 | Hispidulin |
| Partial positive allosteric modulator at the benzodiazepine receptor | |
| 1327 | L-655,708 |
| 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 | |
| 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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