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 ǰȳ  Ű   Pharmacology

GABA Receptor Small molecules

GABA receptor ʿ Small molecules Ұմϴ.

TOCRIS
ǰ ϱ
μϱ




Inhibitors
Cat. No. Product Name / Activity
0206 β-Alanine
GABA uptake inhibitor (GAT-2 and -3); also glycine receptor agonist and MRGPRD agonist
1296 CI 966 hydrochloride
Selective inhibitor of GAT-1
0234 Guvacine hydrochloride
Specific GABA uptake inhibitor
2747 NNC 05-2090 hydrochloride
GABA uptake inhibitor; moderately BGT-1 selective
1779 NNC 711
Selective GAT-1 inhibitor
0768 Riluzole hydrochloride
GABA uptake inhibitor; also inhibits glutamate release and blocks NaV channels
1081 SKF 89976A hydrochloride
Potent GAT-1 inhibitor; brain penetrant
1561 (S)-SNAP 5114
GABA uptake inhibitor
0181 TACA
GABA uptake inhibitor; also GABAA agonist and substrate for GABA-T
4256 Tiagabine hydrochloride
Selective GAT-1 inhibitor; anticonvulsant



Agonists
Cat. No. Product Name / Activity
0344 GABA
Endogenous agonist
0235 Isoguvacine hydrochloride
Selective GABAA agonist
3250 L-838,417
GABAA partial agonist; displays subtype selectivity
4415 MK 0343
GABAA partial agonist; displays subtype selectivity
0289 Muscimol
Potent GABAA agonist; also GABAA-ρ partial 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
GABAA agonist; displays subtype selectivity
0807 THIP hydrochloride
GABAA agonist
0180 ZAPA sulfate
'Low affinity' GABAA agonist; also GABAA-ρ antagonist
Inverse Agonists
Cat. No. Product Name / Activity
3817 MRK 016
α5-selective GABAA inverse agonist
2905 TB 21007
α5-selective GABAA inverse agonist
Antagonists
Cat. No. Product Name / 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
3109 Furosemide
GABAA antagonist; also Na+/2Cl-/K+ cotransporter blocker
4466 PHP 501 trifluoroacetate
Potent GABAA antagonist
1128 Picrotoxin
GABAA antagonist
2143 SCS
Potent GABAA antagonist; β1-subunit selective
1262 SR 95531 hydrobromide
Competitive and selective GABAA antagonist
1472 Suramin hexasodium salt
Competitive α1β2γ2 GABAA antagonist; also non-selective P2 antagonist
2745 U 93631
GABAA 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 benzodiazepine partial agonist
0456 Chlormezanone
Positive allosteric modulator of benzodiazepine site
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 ligand for mitochondrial DBI receptor; GABAA receptor modulator
0659 FGIN-1-43
Potent ligand for mitochondrial DBI receptor; GABAA receptor modulator
1328 Flumazenil
Benzodiazepine antagonist
2174 Hispidulin
Partial positive allosteric modulator at the benzodiazepine site
3597 Indiplon
Positive allosteric modulator of GABAA; acts at benzodiazepine site
1327 L-655,708
Benzodiazepine inverse agonist; selective for α5-containing GABAA receptors
3087 Lorazepam
Ligand at benzodiazepine site
2832 Midazolam hydrochloride
Benzodiazepine agonist
1997 Ro 15-4513
Benzodiazepine partial inverse agonist
1995 Ro 19-4603
Benzodiazepine inverse agonist
3942 TCS 1105
GABAA α2 benzodiazepine agonist
4414 TP 003
GABAA partial agonist; acts at benzodiazepine site
3655 Zaleplon
Benzodiazepine site agonist
1994 ZK 93423 hydrochloride
Potent benzodiazepine agonist
1996 ZK 93426 hydrochloride
Potent and 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
Positive allosteric modulator of GABAA receptors
0881 Chlormethiazole hydrochloride
Potentiates GABAA receptor function
3679 DS2
Positive allosteric modulator of δ-containing GABAA receptors
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
2531 Ganaxolone
Potent positive allosteric modulator of GABAA receptors
1295 Loreclezole hydrochloride
Subtype-selective GABAA modulator
4949 MaxiPost
Negative modulator of GABAA receptors; also potassium channel modulator
4410 Ocinaplon
GABAA modulator; anxiolytic
2738 Org 20599
Positive allosteric modulator of GABAA receptors; direct agonist at higher concentrations
2681 17-PA
Antagonist of neurosteroid potentiation and direct gating of GABAA
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
0830 Primidone
Potentiates GABAA receptor function
6192 PZ-II-029
α6β3γ2-selective GABAA positive allosteric modulator
1512 SB 205384
GABAA modulator; slows current decay
6334 THDOC
Positive modulator of GABAA receptors; endogenous neurosteroid
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
2733 U 90042
GABAA ligand
3048 Valerenic acid
Positive allosteric modulator of GABAA receptors



Agonists
Cat. No. Product Name / Activity
0796 (R)-Baclofen
Selective GABAB agonist; active enantiomer of (RS)-Baclofen (Cat. No. 0417)
0417 (RS)-Baclofen
Selective GABAB agonist
0344 GABA
Endogenous agonist
3400 RuBi-GABA
Caged GABA; excitable at visible wavelengths
4709 RuBi GABA trimethylphosphine
Caged GABA; inhibits neural activity
0379 SKF 97541
Highly potent GABAB agonist; also GABAA-ρ antagonist
Antagonists
Cat. No. Product Name / Activity
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
0245 2-Hydroxysaclofen
Selective GABAB antagonist; more potent than Saclofen (Cat. No. 0246)
0178 Phaclofen
Selective GABAB antagonist
0246 Saclofen
Selective GABAB antagonist
0984 SCH 50911
Selective and competitive GABAB antagonist; orally bioavailable
Modulators
Cat. No. Product Name / Activity
3313 rac BHFF
Potent and selective postitive allosteric modulator of GABAB receptors
1514 CGP 13501
Positive allosteric modulator of GABAB receptors
1513 CGP 7930
Positive allosteric modulator of GABAB receptors
2001 GS 39783
Positive allosteric modulator of GABAB receptors
Other
Cat. No. Product Name / Activity
1814 N-ArachidonylGABA
Inhibits pain in vivo
0538 trans-4-Hydroxycrotonic acid
GHB receptor ligand
0386 3-Methyl-GABA
Activator of GABA amino-transferase
1811 Modafinil
Psychostimulant
0780 NCS-382
Antagonist of γ-hydroxybutyric acid
4579 Pentobarbital sodium salt
Enhances GABAergic activity
2687 Pentylenetetrazole
CNS stimulant
5518 UMB 68
GHB receptor ligand
2815 Valproic acid, sodium salt
Increases GABA levels; anticonvulsant
2625 Zonisamide
Modulates GABA neurotransmission; anticonvulsant


Inhibitors
Cat. No. Product Name / Activity
3888 VU 0240551
KCC2 inhibitor
4719 VU 0463271
Potent and selective KCC2 inhibitor
Activators
Cat. No. Product Name / Activity
5242 CLP 257
Selective KCC2 activator


Cat. No. Product Name / Activity
3400 RuBi-GABA
Caged GABA; excitable at visible wavelengths
4709 RuBi GABA trimethylphosphine
Caged GABA; inhibits neural activity