gaba receptor inhibitors (inhibitors, agonists and modulators) · 2020. 9. 30. · gaba receptor...
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GABA Receptor Inhibitors
(inhibitors, agonists and modulators)
GABA is a chemical messenger that is widely distributed in the brain. GABA’s natural function is to reduce the activity of the neurons
to which it binds. GABA receptors are probably the most common kind in the mammalian nervous system. It is estimated that close to
40% of the synapses in the human brain work with GABA and therefore have GABA receptors.
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Nefiracetam - CAS 77191-36-7
Catalog Number: B0084-076916 Price: $398/1 g
Molecular Weight: 246.3 Molecular Formula: C14H18N2O2
Description: Nefiracetam is a GABAergic, cholinergic, and monoaminergic neuronal system
enhancer for Ro 5-4864-induced convulsions.
Baicalin - CAS 21967-41-9
Catalog Number: B0084-087689 Price: $239/50 g
Molecular Weight: 446.364 Molecular Formula: C21H18O11
Description: Baicalin is a flavone found in several species in the genus Scutellaria, including
Scutellaria baicalensis and Scutellaria lateriflora. Baicalin is a positive allosteric modulator of the
benzodiazepine site and/or a non-benzodiazepine site of the GABA receptor.
(S)-(-)-4-Amino-2-hydroxybutyric acid - CAS 40371-51-5
Catalog Number: B0084-091852 Price: $198/200 g
Molecular Weight: 119.12 Molecular Formula: C4H9NO3
Description: (S)-(-)-4-Amino-2-hydroxybutyric acid is an analogue of γ-aminobutyric acid (GABA)
that exhibits potential inhibitory activity on GABA binding and uptake by brain.
(R)-baclofen - CAS 69308-37-8
Catalog Number: B0084-097120 Price: $499/5 g
Molecular Weight: 213.66 Molecular Formula: C10H12ClNO2
Description: (R)-baclofen a selective GABAB agonist.
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CGP 52432 - CAS 139667-74-6
Catalog Number: B0084-211080 Price: $238/20 mg
Molecular Weight: 384.24 Molecular Formula: C15H24Cl2NO4P
Description: CGP52432 is a potent and selective GABAB receptor antagonist with IC50 value of 85
nM.
AWD 131-138 - CAS 188116-07-6
Catalog Number: B0084-244924 Price: $248/10 mg
Molecular Weight: 279.724 Molecular Formula: C13H14ClN3O2
Description: AWD 131-138 is a partial agonist of GABAA receptor with low affinity for the
benzodiazepine binding site. AWD 131-138 exhibits potent anticonvulsant and anxiolytic properties
in rodent models. It is used as an antiepileptic drug for the treatment of canine idiopathic epilepsy.
2-{3-[5-(2-Hydroxypropan-2-yl)-1H-1,3-benzodiazol-1-yl]phenyl}benzamide - CAS 951654-29-8
Catalog Number: B0084-284807 Price: $198/10 mg
Molecular Weight: 371.44 Molecular Formula: C23H21N3O2
Description: A GABAA receptor modulator that effects against anxiety.
Piperine - CAS 94-62-2
Catalog Number: B0084-291161 Price: $389/250 g
Molecular Weight: 285.34 Molecular Formula: C17H19NO3
Description: Piperine (1-Piperoylpiperidine) is an alkaloid isolated from black pepper, activating
transient receptor potential vanilloid type 1 receptor (TRPV1; EC50 = 38 µM) and modulates GABAA
receptors (EC50s = 43-60 µM). It is used in some traditional medicines.
Supplement in health care products.
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Thiocolchicoside - CAS 602-41-5
Catalog Number: B0084-464811 Price: $199/500 mg; $299/1 g
Molecular Weight: 563.618 Molecular Formula: C27H33NO10S
Description: Thiocolchicoside is a semi-synthetic derivative of colchicine, an anti-inflammatory
glycoside extracted from the flower seeds of superba gloriosa. Thiocolchicoside acts as a GABAA
receptor antagonist exhibiting anti-inflammatory and analgesic activity. It is used as a muscle
relaxant.
Baclofen - CAS 1134-47-0
Catalog Number: B0084-474356 Price: $198/100 g
Molecular Weight: 213.66 Molecular Formula: C10H12ClNO2
Description: Baclofen, an agonist of GABAB receptor, could be effective as a skeletal muscle
relaxant and has been also found to have antispastic effect.
BAR-501 - CAS 1632118-69-4
Catalog Number: B0084-482211 Price: $198/10 mg
Molecular Weight: 406.651 Molecular Formula: C26H46O3
Description: BAR-501, a UDCA derivative, is a selective GPBAR1 agonist devoid of any FXR
agonistic activity. BAR-501 effectively transactivates GPBAR1 in HEK293 cells overexpressing a
CRE along with GPBAR1, with a EC50 of 1 μM. Besides, protects against development of portal
hypertension in rodent models of liver injury and endothelial dysfunction.
Ganaxolone - CAS 38398-32-2
Catalog Number:
Molecular Weight: 332.53 Molecular Formula: C22H36O2
Description: Ganaxolone is a positive allosteric modulator of GABAA receptors with
anticonvulsive anxiolytic properties. Ganaxolone enhances GABA-evoked chloride currents in
Xenopus oocytes expressing GABAA receptors (EC50= 94, 122 and 213 nM for α2β1γ2L, α3β1γ2L and
α1β1γ2L receptors, respectively). It acts via inhibiting GABAA receptor-chloride channel ligand
binding and enhancing ligand binding at the benzodiazepine site.
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(-)-Bicuculline methochloride - CAS 53552-05-9
Catalog Number:
Molecular Weight: 417.85 Molecular Formula: C21H20ClNO6
Description: (-)-Bicuculline methochloride is the methochloride salt of (+)-bicuculline, which is a
potent antagonist of GABAA receptors.
CGP 13501 - CAS 56189-68-5
Catalog Number:
Molecular Weight: 290.44 Molecular Formula: C19H30O2
Description: CGP 13501 is a positive allosteric modulator of GABAB receptors, potentiating the
effects of GABA at this receptor type.
Guvacine hydrochloride - CAS 6027-91-4
Catalog Number:
Molecular Weight: 163.6 Molecular Formula: C6H9NO2.HCl
Description: Guvacine hydrochloride is a specific GABA uptake inhibitor (IC50 = 14, 58, 119 and 1870
μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1, respectively). Guvacine may be beneficial for the
treatment of neuropsychiatric disorders.
(-)-Bicuculline methobromide - CAS 73604-30-5
Catalog Number:
Molecular Weight: 462.3 Molecular Formula: C21H20BrNO6
Description: (-)-Bicuculline methobromide is the methobromide salt of (+)-bicuculline, which is a
potent antagonist of GABAA receptors.
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FG 7142 - CAS 78538-74-6
Catalog Number:
Molecular Weight: 225.25 Molecular Formula: C13H11N3O
Description: FG 7142 is a benzodiazepine inverse agonist and anxiogenic agent. FG 7142 increases
tyrosine hydroxylation and upregulates β-adrenoceptors in mouse cerebral cortex.
CGP 46381 - CAS 123691-14-5
Catalog Number:
Molecular Weight: 219.26 Molecular Formula: C10H22NO2P
Description: CGP 46381 is a selective GABAB receptor antagonist (IC50 = 4.9 μM).
SKF 97541 - CAS 127729-35-5
Catalog Number:
Molecular Weight: 137.12 Molecular Formula: C4H12NO2P
Description: SKF 97541 is a highly potent GABAB agonist, and also acts as a GABAA-ρ antagonist.
SKF 97541 exhibits sedative effects in mammals and has the potential to be used in the treatment
of various addictions due to neurochemical imbalances.
FGIN-1-43 - CAS 145040-29-5
Catalog Number:
Molecular Weight: 487.51 Molecular Formula: C28H36Cl2N2O
Description: FGIN-1-43 is a potent and specific ligand for the mitochondial DBI receptor (MDR).
CGP 55845 hydrochloride - CAS 149184-22-5
Catalog Number:
Molecular Weight: 438.71 Molecular Formula: C18H22Cl2NO3P.HCl
Description: CGP 55845 hydrochloride is a potent and selective GABAB receptor antagonist (IC50
= 5 nM), which prevents agonist binding (pKi = 8.35) and inhibits release of GABA and glutamate
(pEC50 = 8.08 and 7.85, respectively).
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CP 615003 mesylate - CAS 1259477-42-3
Catalog Number:
Molecular Weight: 469.53 Molecular Formula: C20H24FN3O3.CH4O3S
Description: CP 615003 mesylate is a potent and selective GABAA receptor partial agonist
potentially useful in treating generalized anxiety disorder.
Primidone - CAS 125-33-7
Catalog Number: 125-33-7
Molecular Weight: 218.25 Molecular Formula: C12H14N2O2
Description: Primidone, a pyrimidinedione derivative, could be used as an anticonvulsant agent
especially against epilepsy unspecified.
Pagoclone - CAS 133737-32-3
Catalog Number:
Molecular Weight: 407.89 Molecular Formula: C23H22ClN3O2
Description: Pagoclone, an active (+)-enantiomer of the racemate RP 59037, is a ubtype selective
partial agonist at GABAA receptor and used for the treatment of panic and anxiety disorders.
Ginkgolide A - CAS 15291-75-5
Catalog Number: 15291-75-5
Molecular Weight: 408.4 Molecular Formula: C20H24O9
Description: Ginkgolide A is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA)
antagonist with a Ki of 14.5 μM.
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Afloqualone - CAS 56287-74-2
Catalog Number: 56287-74-2
Molecular Weight: 283.3 Molecular Formula: C16H14FN3O
Description: Afloqualone is a agonist of GABA receptor has sedative and muscle-relaxant effects.
Bemegride - CAS 64-65-3
Catalog Number: 64-65-3
Molecular Weight: 155.19 Molecular Formula: C8H13NO2
Description: Bemegride is a central nervous system stimulant and antidote for barbiturate
poisoning.
Acamprosate calcium - CAS 77337-73-6
Catalog Number: 77337-73-6
Molecular Weight: 400.48 Molecular Formula: C10H20CaN2O8S2
Description: Acamprosate calcium is a gamma-aminobutyric acid(GABA)agonist and modulator
of glutamatergic systems. It has been used in alcohol dependence treatments and may be an
effective augmentation therapy in patients with treatment-resistant anxiety. It has low
bioavailability, but also has an excellent tolerability and safety profile. It is unique in that it is not
metabolized by the liver and is also not impacted by alcohol use, so it can be administered to
patients with hepatitis or liver disease and to patients who continue drinking alcohol. It was
approved for use in the therapy of alcohol dependence and abuse in the United States in 2004.
CI 966 hydrochloride - CAS 110283-66-4
Catalog Number:
Molecular Weight: 509.87 Molecular Formula: C23H21F6NO3.HCl
Description: The hydrochloride salt form of CI 966, which is an inhibitor of the GABA transporter
and could be used as anticonvulsive as well as neuroprotective agent.
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SB 205384 - CAS 160296-13-9
Catalog Number:
Molecular Weight: 330.4 Molecular Formula: C17H18N2O3S
Description: SB 205384 is a GABAA receptor modulator. SB 205384 potentiates α6, α3 and α5-
subunit-containing receptors (EC50 = 280, 695 and 730 nM, respectively). It exhibits little effect on
receptors which contains α1 or α2 subunits.
Emamectin Benzoate - CAS 155569-91-8
Catalog Number: 155569-91-8
Molecular Weight: 1008.24 Molecular Formula: C56H81NO15
Description: Emamectin Benzoate is the Emamectin derivative. Emamectin, also called as
Proclaim, is widely used as an insecticide because of its chloride channel activation properties.
Indiplon - CAS 325715-02-4
Catalog Number: 325715-02-4
Molecular Weight: 376.43 Molecular Formula: C20H16N4O2S
Description: Indiplon acts as a high-affinity positive and orally active allosteric modulator of the
GABAA receptor (Ki=1.2 nM in rat frontal cortex and Ki=1.7 nM and in cerebellum).
Valerenic acid - CAS 3569-10-6
Catalog Number:
Molecular Weight: 234.33 Molecular Formula: C15H22O2
Description: Valerenic acid is a positive allosteric modulator of GABAA receptors displaying
selectivity for receptors containing β2 or β3 subunits. Valerenic acid exhibits sedative,
anticonvulsant and anxiolytic effects in vivo. Valerenic acid also acts as a partial agonist of 5-
HT5A receptors.
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(+)-Bicuculline - CAS 485-49-4
Catalog Number: 485-49-4
Molecular Weight: 367.35 Molecular Formula: C20H17NO6
Description: (+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also
blocks Ca(2+)-activated potassium channels.
Progabide - CAS 62666-20-0
Catalog Number: 62666-20-0
Molecular Weight: 334.77 Molecular Formula: C17H16ClFN2O2
Description: Progabide is a gamma-aminobutyric acid (GABA) antagonist. It has agonistic
activity for both the GABAA and GABAB receptors. It has antiepileptic activity and is commonly
used in the treatment of epilepsy. It also has been used for many diseases, including
schizophrenia, Parkinson's disease, clinical depression and anxiety disorder with varying success.
SCS - CAS 3232-36-8
Catalog Number:
Molecular Weight: 256.26 Molecular Formula: C14H12N2O3
Description: SCS is a potent and selective partial inhibitor of β1-containing GABAA receptors (IC50
= 4.5, 5.3 and 7.9 nM at α2β1γ1θ, α2β1γ1 and α2β1γ2s GABAA receptors, respectively).
L-Cycloserine - CAS 339-72-0
Catalog Number: 339-72-0
Molecular Weight: 102.09 Molecular Formula: C3H6N2O2
Description: L-Cycloserine is excitatory amino acid, an antibiotic effective against
Mycobacterium tuberculosis.
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TACA - CAS 38090-53-8
Catalog Number:
Molecular Weight: 101.1 Molecular Formula: C4H7NO2
Description: TACA, the trans-isomer of CACA, is a potent GABAA and GABAC agonist, GABA
uptake inhibitor and substrate for GABA-T. It also acts as a GABAA-ρ agonist.
Ro 19-4603 - CAS 99632-94-7
Catalog Number:
Molecular Weight: 319.38 Molecular Formula: C15H17N3O3S
Description: Ro 19-4603 is a novel potent partial inverse agonist of benzodiazepine (BZ) receptors.
Ro19-4603 binds with high affinity to both diazepam-sensitive (DS) and diazepam-insensitive (DI)
GABAA receptors (Ki values are ~ 0.2 and ~ 2.6 nM for DS and DI receptors respectively).
DMCM hydrochloride - CAS 1215833-62-7
Catalog Number:
Molecular Weight: 350.8 Molecular Formula: C17H18N2O4.HCl
Description: DMCM hydrochloride is a benzodiazepine inverse agonist exhibiting anxiogenic and
potent convulsant activity.
CGP 36216 hydrochloride - CAS 123691-29-2
Catalog Number:
Molecular Weight: 187.6 Molecular Formula: C5H14NO2P.HCl
Description: CGP 36216 hydrochloride is a selective GABAB antagonist that is active to
presynaptic receptors but inactive to postsynaptic receptors.
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L-838,417 - CAS 286456-42-6
Catalog Number:
Molecular Weight: 399.40 Molecular Formula: C19H19F2N7O
Description: L-838,417 is a subtype-selective GABAA receptor partial agonist. It selectively binds
to α2, α3 and α5 subunits with Ki values of 0.67, 0.67 and 2.25 nM respectively, but it shows no
efficacy at α1 (α1-sparing). It shows non-sedative antinociceptive, anxiolytic and anti-
inflammatory activity in vivo. It was developed by Merck.
CGP7930 - CAS 57717-80-3
Catalog Number: 57717-80-3
Molecular Weight: 292.46 Molecular Formula: C19H32O2
Description: CGP7930 is a positive allosteric modulator at the GABAB receptor. It has anxiolytic
effects in animal studies, and has a synergistic effect with GABAB agonists such as baclofen and
GHB. It increases the potency and efficacy of GABA at both native and recombinant GABAB
receptors with EC50 values of 5.37 and 4.60μM respectively. It also enhances the inhibitory effect
of the agonist L-baclofen in cultured cortical neurons. It reduces operant self-administration of
ethanol and cocaine in rats.
Chlormethiazole hydrochloride - CAS 6001-74-7
Catalog Number:
Molecular Weight: 198.11 Molecular Formula: C6H9Cl2NS
Description: Chlormethiazole hydrochloride is the hydrochloride salt of chlormethiazole, which is
a GABAA agonist. It is a useful research chemical and is used in the study of effects of thiazole
methiodide and hydrochloride fractions of thiamine upon the neuromuscular system. It is
neuroprotective in a number of animal models and is used as a sedative and anticonvulsant. It
prevents the degeneration of serotonergic nerve terminals induced by MDMA.
DS2 - CAS 374084-31-8
Catalog Number:
Molecular Weight: 353.83 Molecular Formula: C18H12ClN3OS
Description: DS2 has been found to be a positive allosteric modulator of δ-GABAA receptors and
could probably be useful against analgesics as well as sleep disorders.
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TCS 1105 - CAS 185391-33-7
Catalog Number:
Molecular Weight: 296.3 Molecular Formula: C17H13FN2O2
Description: TCS 1105 is a GABAA benzodiazepine receptor (BZR) ligand that acts as an agonist
at α2 and antagonist at α1 benzodiazepine receptors (Ki = 118 and 245 nM, respectively).
TCS 1205 - CAS 355022-97-8
Catalog Number:
Molecular Weight: 337.33 Molecular Formula: C18H15N3O4
Description: TCS 1205 is a GABAA α2 benzodiazepine receptor agonist and GABAA α1 partial
agonist in vitro (Ki = 14 and 121 nM, respectively). It displays non-sedative anxiolytic activity in vivo.
Pipequaline - CAS 77472-98-1
Catalog Number: 77472-98-1
Molecular Weight: 316.448 Molecular Formula: C22H24N2
Description: Pipequaline is a non-selective GABAA receptor partial agonist that is potentially used
as an anxiolytic drug of the nonbenzodiazepine class. It exhibits anxiolytic properties and very
little sedative, amnestic or anticonvulsant effects. Currently pipequaline is only used for research.
Bretazenil - CAS 84379-13-5
Catalog Number:
Molecular Weight: 418.28 Molecular Formula: C19H20BrN3O3
Description: Bretazenil is a partial agonist at the GABAA benzodiazepine site (EC50 = 10 nM at
α1β1γ2 receptors) that potentiates GABA responses on α4β3γ2 cells. Bretazenil is potentially used
for the treatment of anxiety disorders.
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Arbaclofen Hydrochloride - CAS 63701-55-3
Catalog Number: 63701-55-3
Molecular Weight: 250.12 Molecular Formula: C10H13Cl2NO2
Description: Arbaclofen, the R-enantiomer of baclofen, is a selective gamma-amino butyric acid
type B receptor agonist used for autism spectrum disorder and fragile X syndrome in randomized,
double blind, placebo controlled trials.
Ocinaplon - CAS 96604-21-6
Catalog Number:
Molecular Weight: 301.3 Molecular Formula: C17H11N5O
Description: Ocinaplon is a GABAA receptor modulator and it can be used for the treatment of
generalized anxiety disorder.
SR 95531 hydrobromide - CAS 104104-50-9
Catalog Number:
Molecular Weight: 368.23 Molecular Formula: C15H17N3O3.HBr
Description: SR 95531 hydrobromide is a competitive GABAA receptor antagonist. SR 95531 differs
from bicuculline that it selectively antagonizes GABA-induced Cl- currents but exhibits little
action on pentobarbitone-induced currents. SR 95531 also acts as a low affinity glycine receptor
antagonist.
Loreclezole hydrochloride - CAS 117857-45-1
Catalog Number:
Molecular Weight: 311 Molecular Formula: C10H6Cl3N3.HCl
Description: Loreclezole hydrochloride is a subtype-selective GABAA receptor modulator. It acts
as a positive allosteric modulator of β2 or β3-subunit containing receptors.
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L-655,708 - CAS 130477-52-0
Catalog Number: 130477-52-0
Molecular Weight: 341.36 Molecular Formula: C18H19N3O4
Description: L-655,708, an inverse agonist of α5 subunit involved in GABAA receptor, has been
found to exhibit cognitive performance improvement in biological studies.
U 90042 - CAS 134516-99-7
Catalog Number:
Molecular Weight: 352.78 Molecular Formula: C17H13ClN6O
Description: U 90042 is a GABAA receptor ligand binding to three receptor subtypes: α1β2γ2,
α3β2γ2 and α6β2γ2 (Ki = 7.8, 9.5 and 11.0 nM, respectively). U 90042 potentiates GABA-induced
chloride currents in α6β2γ2 receptors. U 90042 is used as a sedative/hypnotic.
Org 20599 - CAS 156685-94-8
Catalog Number:
Molecular Weight: 438.04 Molecular Formula: C25H40ClNO3
Description: Org 20599 is an anaesthetic steroid. It has modulatory effects on GABAA receptors.
Org 20599 is a potential theraputic for migraines and headaches.
NNC 05-2090 hydrochloride - CAS 184845-18-9
Catalog Number:
Molecular Weight: 451.01 Molecular Formula: C27H30N2O2.HCl
Description: NNC052090 is a GABA uptake inhibitor that displays selectivity for BGT-1 (mGAT-2)
transporters.
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DPNI-caged-GABA - CAS 927866-58-8
Catalog Number:
Molecular Weight: 499.30 Molecular Formula: C15H23N3O12P2
Description: DPNI-caged-GABA, a kind of neurotransmitter, has been found to be allowed optical
control of neural tissue with high spatial and temporal precision.
RuBi GABA trimethylphosphine
Catalog Number:
Molecular Weight: 904.56 Molecular Formula: C27H33N5O2PRu.PF6.NaPF6
Description: RuBi GABA trimethylphosphine is the modified version of RuBi-GABA, which inhibits
neural activity in vivo and is suitable for use as alternative for GABA agonists such as muscimol.
It suppresses cortical local field potential (LFP) activity in anesthetized mice after activation with
a blue laser pulse.
RuBi-GABA - CAS 1028141-88-9
Catalog Number:
Molecular Weight: 922.8 Molecular Formula: C42H39F6N5O2P2Ru
Description: RuBi-GABA, a ruthenium-bipyridine-triphenylphosphine caged GABA, is a
photolabile protecting group used for highly efficient visible light GABA uncaging.
PHP 501 trifluoroacetate - CAS 1236105-75-1
Catalog Number:
Molecular Weight: 433.42 Molecular Formula: C20H21N3O.CF3CO2H
Description: PHP 501 trifluoroacetate is potent GABAA antagonist (Ki = 0.0028 μM at rat GABAA
receptors; IC50 = 0.024 μM at human α1β2γ2 GABAA-expressing tsA201 cells), without disrupting
hGAT-1, hGAT-2, hGAT-3 or hBGT-1 GABA transporters.
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PZ-II-029 - CAS 164025-44-9
Catalog Number:
Molecular Weight: 321.33 Molecular Formula: C18H15N3O3
Description: PZ-II-029,a pyrazoloquinolinone, was reported as the first postitive modulator of
GABAA α6β3γ2 subtype functionally selective ligands to date.
Tracazolate hydrochloride - CAS 1135210-68-2
Catalog Number:
Molecular Weight: 340.85 Molecular Formula: C16H24N4O2.HCl
Description: Tracazolate hydrochloride is a subtype-selective GABAA receptor modulator that
potentiates or inhibits recombinant GABAA function depending on subunit combination.
Tracazolate hydrochloride enhances native GABAA receptor function, and exhibits anxiolytic
activity following systemic administration in vivo.
TP 003 - CAS 628690-75-5
Catalog Number:
Molecular Weight: 407.39 Molecular Formula: C23H16F3N3O
Description: TP 003 is a selective GABAA receptor (α3 subtype) partial agonist with affinity for the
benzodiazepine binding site on human GABAA receptors. TP 003 exhibits anxiolytic-like effects
in rodent behavioral models of anxiety.
ZK 93426 hydrochloride - CAS 1216792-30-1
Catalog Number:
Molecular Weight: 348.82 Molecular Formula: C18H20N2O3.HCl
Description: ZK 93426 hydrochloride is a potent, selective and competitive benzodiazepine
receptor antagonist (IC50 = 0.4 and 0.7 nM for inhibition of [3H]-flunitrazepam binding to rat
cerebellum and hippocampus, respectively). ZK 93426 hydrochloride displays both anxiogenic
and anxiolytic effects.
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ZK 93423 hydrochloride - CAS 1216574-52-5
Catalog Number:
Molecular Weight: 426.9 Molecular Formula: C23H22N2O4.HCl
Description: ZK 93423 hydrochloride is a potent and non-selective benzodiazepine receptor
agonist (IC50 = 1 nM) (Ki = 4.1, 4.2, 6 and 4.5 nM for inhibition of [3H]Ro15-1788 binding to human
recombinant α1β3γ2, α2β3γ2, α3β3γ2 and α5β3γ2 receptors, respectively). ZK 93423 hydrochloride
acts as an anxiolytic following systemic administration in vivo.
ZAPA sulfate - CAS 371962-01-5
Catalog Number:
Molecular Weight: 244.24 Molecular Formula: C4H6N2O2S.H2SO4
Description: ZAPA sulfate acts as an agonist at low affinity GABAA receptors and is thus a useful
ligand to investigate GABA receptors linked to benzodiazepine receptors. ZAPA sulfate is also a
GABAA-ρ receptor antagonist.
U 89843A - CAS 157013-85-9
Catalog Number:
Molecular Weight: 321.85 Molecular Formula: C16H23N5.HCl
Description: U 89843A is a positive allosteric modulator of GABAA receptors. U 89843A potentiates
GABA-induced Cl- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 GABAA receptors. U 89843A exhibits
sedative activity following i.v. administration without losing "righting reflex" and also displays
antioxidant activity.
adipiplon - CAS 840486-93-3
Catalog Number: 840486-93-3
Molecular Weight: 351.39 Molecular Formula: C18H18FN7
Description: Adipiplon is GABAA receptor partial agonist. It can bind to the α3 subtype. Adipiplon
is one of the first drugs selected for clinical development which is able to discriminate between α2
and α3, as well as showing little affinity for the α1 or α5 subtypes .Adipiplon is being researched as
a potential medication for the treatment of anxiety and insomnia, and in 2008 it was being used
in Phase IIb trials. But these trials were suspended after next-day side effects were discovered.
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Nipecotic acid - CAS 60252-41-7
Catalog Number:
Molecular Weight: 129.16 Molecular Formula: C6H11NO2
Description: (±)-Nipecotic acid is a nonselective GAT inhibitor that also induces GABA release
through a process termed 'heteroexchange. IC50 = 8, 38, 106 and 2370 μM for hGAT-1, rGAT-2,
hGAT-3 and hBGT-1 respectively.
Ro 15-4513 - CAS 91917-65-6
Catalog Number:
Molecular Weight: 326.31 Molecular Formula: C15H14N6O3
Description: Ro 15-4513, a high affinity benzodiazepine ligand, acts as a competitive antagonist,
and can therefore be an antidote to the acute impairment caused by alcohol. Ki values are 3.1 and
5.3 nM for diazepam-insensitive (DI) and diazepam-sensitive (DS) benzodiazepine receptors
respectively.
N-ArachidonylGABA - CAS 128201-89-8
Catalog Number:
Molecular Weight: 389.58 Molecular Formula: C24H39NO3
Description: N-ArachidonylGABA is first isolated from bovine brain. It was also found to inhibit
normal responses to pain in vivo, but has not been fully characterized to date.
Pregnenolone sulfate sodium salt - CAS 1852-38-6
Catalog Number:
Molecular Weight: 418.52 Molecular Formula: C21H31NaO5S
Description: Pregnenolone sulfate, a metabolite of the natural steroid hormone pregnenolone, is
a neurosteroid that has been demonstrated to antagonize the GABAA receptor chloride channel.
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GS 39783 - CAS 39069-52-8
Catalog Number: 39069-52-8
Molecular Weight: 337.44 Molecular Formula: C15H23N5O2S
Description: GS 39783 is an allosteric positive modulator of GABAB receptors, decreases cocaine
self-administration, blocks the rewarding properties of nicotine and produces anxiolytic-like
activity without the side effects associated with baclofen or benzodiazepines.
CGP 54626 hydrochloride - CAS 149184-21-4
Catalog Number: 149184-21-4
Molecular Weight: 410.31 Molecular Formula: C18H28Cl2NO3P.HCl
Description: The hydrochloride salt form of CGP 54626, a dichloropheny derivative, has been
found to be a GABAB receptor antagonist that could probably be effective as an analgesic agent.
IC50: 4 nM.
THIP hydrochloride - CAS 85118-33-8
Catalog Number:
Molecular Weight: 176.6 Molecular Formula: C6H8N2O2.HCl
Description: THIP hydrochloride is a GABAA receptor agonist and GABAA-ρ receptor antagonist.
THIP exhibits antinociceptive, anticonvulsant and sedative effects. It is used as a hypnotic agent
for the treatment of patients with insomnia.
CGS 20625 - CAS 111205-55-1
Catalog Number:
Molecular Weight: 309.36 Molecular Formula: C18H19N3O2
Description: CGS 20625 is a partial agonist for the benzodiazepine binding site of the GABAA
receptor used as an anti-anxiety drug. It acts as a central benzodiazepine receptor agonist (IC50
= 1.3 nM) with no affinity for other neurotransmitter receptor binding sites.
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3-Methyl-GABA - CAS 71424-95-8
Catalog Number:
Molecular Weight: 522.58 Molecular Formula: C5H11NO2
Description: 3-Methyl-GABA is an activator of GABA aminotransferase.
CL 218872 - CAS 66548-69-4
Catalog Number:
Molecular Weight: 278.24 Molecular Formula: C13H9F3N4
Description: CL 218872 has been found to be a benzodiazepine agonist and has been found to
exhibit anxiolytic and anticonvulsant activities.
Etifoxine Hydrochloride - CAS 56776-32-0
Catalog Number: 56776-32-0
Molecular Weight: 337.24 Molecular Formula: C17H18Cl2N2O
Description: Etifoxine Hydrochloride is Potentiator of GABAA receptor with anxiolytic and
anticonvulsant activity.
Isoguvacine hydrochloride - CAS 68547-97-7
Catalog Number:
Molecular Weight: 163.6 Molecular Formula: C6H10ClNO2
Description: Isoguvacine hydrochloride is a selective GABA receptor agonist with anticonvulsant
and antiepileptic effect, developed for Neuroscience research.
AA 29504 - CAS 945828-50-2
Catalog Number:
Molecular Weight: 327.42 Molecular Formula: C19H25N3O2
Description: AA 29504 is a positive allosteric modulator of GABAA receptors with anxiolytic
activity. It modulates both α4β3δ-containing extrasynaptic receptors and α1β3γ2S-containing
receptors in Xenopus oocytes. AA 29504 is potentially used for the treatment of schizophrenia.
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rac BHFF - CAS 123557-91-5
Catalog Number:
Molecular Weight: 330.34 Molecular Formula: C17H21F3O3
Description: BHFF is a positive allosteric modulator of GABAB receptor that increases the potency
and efficacy of GABA. BHFF displays anxiolytic activity in vivo.
MRK 016 - CAS 783331-24-8
Catalog Number: 783331-24-8
Molecular Weight: 368.40 Molecular Formula: C17H20N8O2
Description: MRK-016 is a selective α5 subunit-containing GABAA negative allosteric modulator
with EC50 value of 3 nM. It has nootropic properties. MRK-016 can produce rapid, ketamine-like
antidepressant effects in animal models of depression.
U-93631 - CAS 152273-12-6
Catalog Number:
Molecular Weight: 299.37 Molecular Formula: C17H21N3O2
Description: U 93631 is a ligand at the picrotoxin site of GABA(A) receptors, allosterically
antagonizing GABA-induced Cl- currents. U-93631 causes rapid decay of gamma-aminobutyric
acid-induced chloride currents in recombinant rat gamma-aminobutyric acid type A receptors.
Cardiazole - CAS 54-95-5
Catalog Number: 54-95-5
Molecular Weight: 138.17 Molecular Formula: C6H10N4
Description: Cardiazole is a GABA(A) receptor antagonist, causes alterations in excitatory and
inhibitory neurotransmitter systems.
Etomidate - CAS 33125-97-2
Catalog Number: 33125-97-2
Molecular Weight: 244.29 Molecular Formula: C14H16N2O2
Description: Etomidate is a GABAA receptor agonist, used as a short-acting anaesthetic agent or
sedative.
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Flumazenil - CAS 78755-81-4
Catalog Number: 78755-81-4
Molecular Weight: 303.29 Molecular Formula: C15H14FN3O3
Description: Flumazenil is a GABAA receptor antagonist and the only GABAA receptor antagonist
on the market today.
L-DABA - CAS 1758-80-1
Catalog Number:
Molecular Weight: 118.13 Molecular Formula: C4H10N2O2
Description: L-DABA, (L-2,4-Diaminobutyric acid) is a noncompetitive GABA transaminase
inhibitor (IC50> 500 μM) with antitumor activity in vivo and in vitro.
Pregnanolone - CAS 128-20-1
Catalog Number:
Molecular Weight: 318.49 Molecular Formula: C21H34O2
Description: Pregnanolone, also known as Kabi-2213, SKF 6455, Eltanolone, is a GABAA receptor
positive allosteric modulator potentially for the treatment of pain.
Phaclofen - CAS 114012-12-3
Catalog Number:
Molecular Weight: 249.63 Molecular Formula: C9H13ClNO3P
Description: Phaclofen, a phosphonic acid derivative of Baclofen, is a selective GABAB antagonist.
2-Hydroxysaclofen - CAS 117354-64-0
Catalog Number:
Molecular Weight: 265.71 Molecular Formula: C9H12ClNO4S
Description: 2-Hydroxysaclofen is a GABAB receptor antagonist.
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CGP 35348 - CAS 123690-79-9
Catalog Number:
Molecular Weight: 225.22 Molecular Formula: C8H20NO4P
Description: CGP 35348 is a selective and brain penetrant GABAB receptor antagonist (IC50 = 34
μM as measured in rat cortical membranes) with higher affinity for postsynaptic than presynaptic
receptors.
Saclofen - CAS 125464-42-8
Catalog Number:
Molecular Weight: 249.72 Molecular Formula: C9H12ClNO3S
Description: Saclofen is a selective antagonist at GABAB receptors.
FGIN-1-27 - CAS 142720-24-9
Catalog Number:
Molecular Weight: 436.61 Molecular Formula: C28H37FN2O
Description: FGIN-1-27 is a high affinity agonist of mitochondrial benzodiazepine receptors (PBR)
binding to benzodiazepine receptors on mitochondrial membranes. FGIN-1-27 indirectly
potentiates GABAA receptor signaling to exhibit anticonvulsant, anxiolytic, and sedative activity
in both animal and clinical models.
NNC 711 - CAS 145645-62-1
Catalog Number:
Molecular Weight: 386.88 Molecular Formula: C21H22N2O3.HCl
Description: NNC 711 is a GABA uptake inhibitor by GAT-1 with IC50 values of 0.04, 171, 1700 and
622 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1. NNC 711 is an anticonvulsantagent.
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(S)-SNAP 5114 - CAS 157604-55-2
Catalog Number:
Molecular Weight: 505.61 Molecular Formula: C30H35NO6
Description: (S)-SNAP 5114 is a GABA transport inhibitor, displaying selectivity for GAT-3 and GAT-
2 (IC50 = 5, 21 and 388 μM for hGAT-3, rGAT-2 and hGAT-1, respectively). (S)-SNAP 5114 was shown
to increase thalamic GABA levels, and acts as an anticonvulsant following systemic
administration in vivo.
TPMPA - CAS 182485-36-5
Catalog Number:
Molecular Weight: 161.14 Molecular Formula: C6H12NO2P
Description: TPMPA is a selective and competitive GABAA-ρ antagonist with 8-fold selectivity for
human recombinant ρ1 receptors over ρ2 receptors. TPMPA exhibits minimal effects on GABAA
and GABAB receptors (Kb = 2.1 μM (antagonist), 320 μM (antagonist) and EC50 ~ 500 μM (weak
agonist) for GABAA-ρ, GABAA and GABAB receptors, respectively).
(-)-Bicuculline methiodide - CAS 40709-69-1
Catalog Number:
Molecular Weight: 509.3 Molecular Formula: C21H20INO6
Description: (-)-Bicuculline methiodide is the methiodide salt of (+)-bicuculline, which is a potent
antagonist of GABAA receptors.
β-CCB - CAS 84454-35-3
Catalog Number:
Molecular Weight: 268.31 Molecular Formula: C16H16N2O2
Description: β-CCB is an endogenous benzodiazepine binding inhibitor with proconvulsant and
anxiogenic properties.
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TB 21007 - CAS 207306-50-1
Catalog Number: 207306-50-1
Molecular Weight: 339.5 Molecular Formula: C15H17NO2S3
Description: TB 21007, as a nootropic drug, is a GABAA receptor inverse agonist selective for the
α5-subtype (Ki values are 1.6, 16, 20 and 20 nM for α5, α2, α1 and α3 subtypes respectively).
Gaboxadol - CAS 64603-91-4
Catalog Number: 64603-91-4
Molecular Weight: 140.14 Molecular Formula: C6H8N2O2
Description: Gaboxadol is a GABA agonist. It was a non-opioid analgesic and a novel type of
hypnotic. It was first synthesized in 1977 by the Danish chemist Povl Krogsgaard-Larsen. It is an
experimental sleep aid drug developed by Lundbeck and Merck. It was used as an analgesic and
anxiolytic, as well as a treatment for tardive dyskinesia, Huntington's disease, Alzheimer's disease,
and spasticity. It was in clinic phase 3 trials, but now it was terminated.
SL 651498 - CAS 205881-86-3
Catalog Number:
Molecular Weight: 389.42 Molecular Formula: C23H20FN3O2
Description: SL 651498 is a GABAA agonist selectively for subtype α2, and has the potential for the
treatment of anxiety.
Arbaclofen placarbil - CAS 847353-30-4
Catalog Number: 847353-30-4
Molecular Weight: 399.87 Molecular Formula: C19H26ClNO6
Description: Arbaclofen placarbil is a prodrug of R-baclofen. It is a GABA B receptor agonist.
Arbaclofen was being developed as a potential treatment for patients with GERD and spasticity
due to multiple sclerosis. However, development was terminated because of unsuccessful results
in phase III clinical trials.
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NS 11394 - CAS 951650-22-9
Catalog Number: 951650-22-9
Molecular Weight: 353.42 Molecular Formula: C23H19N3O
Description: NS 11394 is a drug with selectivity for the α3 and α5 subtypes. It acts as a subtype-
selective positive allosteric modulator at GABAA receptors. It is used as an analgesic for use in
chronic or neuropathic pain. It is unique in having superior efficacy at alpha(3) receptors and low
efficacy at alpha(1) receptors in vitro. It has an excellent pharmacokinetic profile, which correlates
with pharmacodynamic endpoints, yielding a high level of confidence in deriving in vivo
conclusions anchored to an in vitro selectivity profile and allowing for translation to higher
species. It impairs memory in both rats and mice because of its efficacy at GABA(A)-alpha(5)
receptors. It is potent and highly effective in rodent anxiety models. It has a significantly reduced
side effect profile in rat and mouse, even at full CNS receptor occupancy.
Etomidate Hydrochloride - CAS 53188-20-8
Catalog Number: 53188-20-8
Molecular Weight: 280.75 Molecular Formula: C14H17ClN2O2
Description: Etomidate hydrochloride is a GABAA receptor agonist used for the induction of
general anaesthesia.
Remimazolam benzenesulfonat - CAS 1001415-66-2
Catalog Number: 1001415-66-2
Molecular Weight: 597.48 Molecular Formula: C27H25BrN4O5S
Description: Remimazolam, a novel Benzodiazepine derivatives, has potential use for anxiolytic,
sedative and hypnotic. For the reason that remimazolam's beding discontinued because of its
unknown metabolic profile in 2014, this water-soluble benzenesulfonateIt salt wa
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Etifoxine - CAS 21715-46-8
Catalog Number: 21715-46-8
Molecular Weight: 300.78 Molecular Formula: C17H17ClN2O
Description: Etifoxine, also called as HOE 36801 or Stresam, is a positive allosteric modulator of
GABAreceptors that produces anxiolytic effects by preferentially modulating GABAA receptors
containing β2 or β3 subunits over those bearing a β1 subunit.
Lorediplon - CAS 917393-39-6
Catalog Number: 917393-39-6
Molecular Weight: 394.42 Molecular Formula: C20H15FN4O2S
Description: Lorediplon is a hypnotic drug acting as a GABAA receptor modulator, differentially
active at the alpha1-subunit. It is a novel nonbenzodiazepine of the pyrazolopyrimidine family. It
is a drug for the treatment of insomnia. It demonstrated a dose-dependent improvement in sleep.
It has been successfully completed with a best-in-class efficacy profile in terms of maintaining
sleep and sleep quality. It demonstrates a minimum of 10-fold and 6-fold increase in potency in
the spontaneous motor activation studies. It was developed by Ferrer and has been in Cilinic
Phase 2.
CI966 - CAS 110283-79-9
Catalog Number: 110283-79-9
Molecular Weight: 473.41 Molecular Formula: C23H21F6NO3
Description: CI966 is a highly potent and selective blocker of the GABA transporter 1 (GAT-1) with
IC50 value of 0.26 µM acting as a central nervous system depressant. It has potential as a potential
anxiolytic, anticonvulsant and neuroprotective therapeutic but was discontinued during clinical
development due to the incidence of severe adverse effects at higher doses and hence was never
marketed. In a phase I human clinical trial it was developed for the treatment of epilepsy.
Basmisanil - CAS 1159600-41-5
Catalog Number: 1159600-41-5
Molecular Weight: 445.47 Molecular Formula: C21H20FN3O5S
Description: This active molecular is a highly selective inverse agonist/negative allosteric
modulator GABAAα5 receptors. It was developed by Roche to treat cognitive impairment
associated with Down syndrome. In Apr 2016, Roche completed the phase II in Down syndrome (In
adolescents, In adults) in USA, Argentina, Canada, France, Italy, Mexico, New Zealand, Singapore,
Spain and the UK. In Sep 2016, Phase-II clinical trials in Neurological disorders (In adults, In the
elderly) in Spain was on going.
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Eszopiclone - CAS 138729-47-2
Catalog Number: 138729-47-2
Molecular Weight: 388.81 Molecular Formula: C17H17ClN6O3
Description: Eszopiclone is an active stereoisomer of zopiclone with hypnotic and sedative
activity and without significant anxiolytic activity. Eszopiclone is a GABA A receptor agonist. It is
able to bind to and activate the omega-1 subtype of the alpha subunit of the GABA receptor
complex. This leads to the opening of chloride channels, causing hyperpolarization, inhibition of
neuronal firing, and enhancement of the inhibitory effect of GABA. Eszopiclone is an approved for
the treatment of insomnia. It is a controlled substance (depressant) in the US but not in Canada.
CP-409092 - CAS 194098-25-4
Catalog Number: 194098-25-4
Molecular Weight: 297.35 Molecular Formula: C17H19N3O2
Description: CP-409092 is a GABA(A) partial agonist developed for the treatment of General
Anxiety Disorder (GAD) and presents an interesting phenomenon of human pharmacokinetic
predictions. In vitro, CP-409092 was abroadly metabolized in rat and human systems
predominantly to acid metabolite formed by oxidative deamination of the N-methyl group of CP-
409092 mediated by MAO-A (as deduced from inhibition experiments).
CP-457920 - CAS 220860-50-4
Catalog Number: 220860-50-4
Molecular Weight: 323.35 Molecular Formula: C18H17N3O3
Description: CP-457920, also called as NGD 971, is a selective α5 GABAA receptor inverse agonist
(Ki of ~ 1 ng/mL). CP-457920 was progressed into clinical studies for the treatment of Vascular
dementia but discontinued.
MK 0343 - CAS 233275-76-8
Catalog Number: 233275-76-8
Molecular Weight: 397.38 Molecular Formula: C19H17F2N7O
Description: MK 0343, also known as MRK-409, is a subtype-selective GABAA partial agonist (Ki
values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively). MK-0343 is a non-sedating
anxiolytic in preclinical species but causes sedation in humans.
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TPA023 - CAS 252977-51-8
Catalog Number: 252977-51-8
Molecular Weight: 395.44 Molecular Formula: C20H22FN7O
Description: TPA023, also called as MK-0777, is a subtype-selective, mixed agonist-antagonist at
GABAA receptor with anxiolytic and anticonvulsant effects.
Lesogaberan - CAS 344413-67-8
Catalog Number: 344413-67-8
Molecular Weight: 141.03 Molecular Formula: C3H9FNO2P
Description: Lesogaberan is a potent and selective GABAB receptor agonist that limit the clinical
use of baclofen for the treatment of GERD.
PWZ-029 - CAS 164025-33-6
Catalog Number: 164025-33-6
Molecular Weight: 291.74 Molecular Formula: C14H14ClN3O2
Description: PWZ-029, a benzodiazepine derivative, has been found to be a GABAA receptors
inverse agonist that could probably improve memory and exhibit sedative effects at some extent
at higher doses.
SCH-50911 - CAS 733717-87-8
Catalog Number: 733717-87-8
Molecular Weight: 173.21 Molecular Formula: C8H15NO3
Description: CH-50911 is a selective GABA-B antagonist with IC50 value of 1.1 μM. It is developed
by Schering-Plough Corporation. CH-50911 is often used in pharmacology research and it also
acts as an anticonvulsant under normal conditions. Preclinical trials for Absence seizures and
Cognition disorders in USA were discontinued.
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Pipequaline HCl
Catalog Number:
Molecular Weight: 352.908 Molecular Formula: C22H25N2Cl
Description: The hydrochloride of pipequaline. Pipequaline is a non-selective GABAA receptor
partial agonist that is potentially used as an anxiolytic drug of the nonbenzodiazepine class. It
exhibits anxiolytic properties and very little sedative, amnestic or anticonvulsant effects.
Currently pipequaline is only used for research.