| GABAA Receptor Agonists, Antagonists, Modulators |
| Cat. No. |
Product |
Activity |
| 2503 |
(-)-Bicuculline methiodide |
GABAA antagonist; more water soluble
version of (+)-bicuculline (Cat. No. 0130) |
| 0109 |
(-)-Bicuculline methobromide |
GABAA antagonist; more water soluble
version of (+)-bicuculline (Cat. No. 0130) |
| 0131 |
(-)-Bicuculline methochloride |
GABAA antagonist; more water soluble
version of (+)-bicuculline (Cat. No. 0130) |
| 0130 |
(+)-Bicuculline |
Potent GABAA antagonist |
| 2681 |
17-PA |
Antagonist of neurosteroid potentiation and direct gating of
GABAA |
| 3972 |
AA 29504 |
Positive allosteric modulator of GABAA receptors |
| 3653 |
Allopregnanolone |
Positive allosteric modulator of GABAA receptors |
| 3679 |
DS2 |
Positive allosteric modulator of GABAA receptors; displays subunit selectivity |
| 3113 |
Etifoxine hydrochloride |
GABAA potentiator;
anxiolytic |
| 1471 |
Etomidate |
GABA-mimetic; selectively interacts with β2- and β3-subunit
containing GABAA receptors |
| 2867 |
Flupirtine maleate |
GABAA modulator;
also indirect NMDA antagonist and Kv7 channel activator |
| 3109 |
Furosemide |
GABAA antagonist;
also Na+/2Cl-/K+ cotransporter blocker |
| 0344 |
GABA |
Endogenous agonist |
| 2531 |
Ganaxolone |
Potent positive allosteric modulator of GABAA receptors |
| 0235 |
Isoguvacine hydrochloride |
Selective GABAA agonist |
| 3250 |
L-838,417 |
GABAA partial
agonist; displays subtype selectivity |
| 1295 |
Loreclezole hydrochloride |
Subtype-selective GABAA modulator |
| 4949 |
MaxiPost |
Negative modulator of GABAA receptors; also potassium channel modulator |
| 4415 |
MK 0343 |
GABAA partial
agonist; displays subtype selectivity |
| 3817 |
MRK 016 |
α5-selective GABAA inverse
agonist |
| 0289 |
Muscimol |
Potent GABAA agonist;
also GABAA-ρ partial
agonist |
| 4410 |
Ocinaplon |
GABAA modulator;
anxiolytic |
| 2738 |
Org 20599 |
Positive allosteric modulator of GABAA receptors; direct agonist at higher concentrations |
| 4466 |
PHP 501 trifluoroacetate |
Potent GABAA antagonist |
| 1128 |
Picrotoxin |
GABAA antagonist |
| 3652 |
Pregnanolone |
Postitive allosteric modulator of GABAA receptors |
| 5376 |
Pregnenolone sulfate sodium salt |
GABAA inhibitor;
displays some subunit selectivity; NMDA potentiator; also activates TRPM3
channels |
| 6192 |
PZ-II-029 |
α6β3γ2-selective GABAA positive allosteric modulator |
| 4709 |
RuBi GABA trimethylphosphine |
Caged GABA; inhibits neural activity |
| 1512 |
SB 205384 |
GABAA modulator;
slows current decay |
| 2143 |
SCS |
Potent GABAA antagonist;
β1-subunit selective |
| 1262 |
SR 95531 hydrobromide |
Competitive and selective GABAA antagonist |
| 0181 |
TACA |
GABAA agonist;
also GABA-T substrate and GABA uptake inhibitor |
| 2905 |
TB 21007 |
α5-selective GABAA inverse
agonist |
| 6334 |
THDOC |
Positive modulator of GABAA receptors; endogenous neurosteroid |
| 0807 |
THIP hydrochloride |
GABAA agonist |
| 3620 |
Topiramate |
Positive allosteric modulator of GABAA receptors; GluK1 antagonist; also inhibits carbonic
anhydrase (CA) II and IV |
| 1558 |
Tracazolate hydrochloride |
Allosteric modulator of GABAA receptors |
| 2734 |
U 89843A |
Positive allosteric modulator of GABAA receptors |
|
|
|
| Benzodiazepines |
|
| Cat. No. |
Product |
Activity |
| 3568 |
Bretazenil |
Benzodiazepine partial agonist |
| 0456 |
Chlormezanone |
Positive allosteric modulator of benzodiazepine site |
| 1709 |
CL 218872 |
Benzodiazepine agonist |
| 2805 |
Diazepam |
Acts at the benzodiazepine modulatory site |
| 3083 |
DMCM hydrochloride |
Benzodiazepine inverse agonist |
| 0554 |
FG 7142 |
Benzodiazepine inverse agonist |
| 0658 |
FGIN-1-27 |
Potent ligand for mitochondrial DBI receptor; GABAA receptor modulator |
| 1328 |
Flumazenil |
Benzodiazepine antagonist |
| 1327 |
L-655,708 |
Benzodiazepine inverse agonist; selective for α5-containing GABAA receptors |
| 2832 |
Midazolam hydrochloride |
Benzodiazepine agonist |
| 1997 |
Ro 15-4513 |
Benzodiazepine partial inverse agonist |
| 4414 |
TP 003 |
GABAA partial
agonist; acts at benzodiazepine site |
| 0405 |
β-CCB |
Benzodiazepine inverse agonist; putative endogenous ligand |
|
|
|
| GABAB Receptor
Agonists, Antagonists, Modulators |
| Cat. No. |
Product |
Activity |
| 0796 |
(R)-Baclofen |
Selective GABAB agonist; active
enantiomer of (RS)-Baclofen (Cat. No. 0417) |
| 0417 |
(RS)-Baclofen |
Selective GABAB agonist |
| 0245 |
2-Hydroxysaclofen |
Selective GABAB antagonist; more
potent than Saclofen (Cat. No. 0246) |
| 0386 |
3-Methyl-GABA |
Activator of GABA amino-transferase |
| 1514 |
CGP 13501 |
Positive allosteric modulator of GABAB receptors |
| 1245 |
CGP 35348 |
Selective GABAB antagonist;
brain penetrant |
| 3219 |
CGP 36216 hydrochloride |
GABAB antagonist;
displays activity at presynaptic receptors |
| 1247 |
CGP 46381 |
Selective GABAB antagonist;
brain penetrant |
| 1246 |
CGP 52432 |
Potent and selective GABAB antagonist |
| 1088 |
CGP 54626 hydrochloride |
Potent and selective GABAB antagonist |
| 1248 |
CGP 55845 hydrochloride |
Potent and selective GABAB antagonist |
| 1513 |
CGP 7930 |
Positive allosteric modulator of GABAB receptors |
| 0344 |
GABA |
Endogenous agonist |
| 2001 |
GS 39783 |
Positive allosteric modulator of GABAB receptors |
| 1811 |
Modafinil |
Psychostimulant |
| 4579 |
Pentobarbital sodium salt |
Enhances GABAergic activity |
| 2687 |
Pentylenetetrazole |
CNS stimulant |
| 3313 |
rac BHFF |
Potent and selective postitive allosteric modulator of GABAB receptors |
| 4709 |
RuBi GABA trimethylphosphine |
Caged GABA; inhibits neural activity |
| 3400 |
RuBi-GABA |
Caged GABA; excitable at visible wavelengths |
| 0246 |
Saclofen |
Selective GABAB antagonist |
| 0984 |
SCH 50911 |
Selective and competitive GABAB antagonist; orally bioavailable |
| 0379 |
SKF 97541 |
Highly potent GABAB agonist; also GABAA-ρ antagonist |
| 2815 |
Valproic acid, sodium salt |
Increases GABA levels; anticonvulsant |
| 2625 |
Zonisamide |
Modulates GABA neurotransmission; anticonvulsant |