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GABA Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S4700 4-Aminobutyric acid (GABA) 4-Aminobutyric acid (4-Aminobutanoic acid, GABA, Gamma-aminobutyric acid, Piperidic acid) is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.
Theranostics, 2023, 13(4):1355-1369
S4423 Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. This compound induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
Viruses, 2025, 17(2)220
S1969 Nefiracetam Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.
E1247 SR95531 Gabazine(SR95531) is a potent competitive and allosteric antagonist of the GABAA receptor, with an IC50 for the GABA receptor of 9 µM.
E3045 Chinese Arborvilea Seed Extract Chinese Arborvilea Seed Extract is extracted from the dried and mature seed kernels of Platycladus orientalis (L.)Franco, has obvious anti-anxiety effect, and its mechanism may be related to increasing GABA level and decreasing Glu level in hippocampus.
E2848 Afoxolaner Afoxolaner (NexGard) is a new insecticide/acaricide molecule from the isoxazoline family that acts on the insect gamma-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
S5131 Homotaurine Homotaurine (Tramiprosate, Alzhemed, 3-Amino-1-propanesulfonic acid) is a synthetic organic compound that has GABAergic activity by mimicking GABA. It is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy.
S3959 (+)-Borneol (+)-Borneol is one of enantiomers of borneol which is a valuable medical material, senior aromatic spice, and chemical material and has been used in food and also folk medicine.
S4840 Baclofen Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.
S2996 L-DAB HBR

L-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) is an inhibitor of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. This compound exhibits antitumor activity.
S3634 6-Hydroxyflavone (6-HF) 6-Hydroxyflavone, a naturally occurring flavonoid, binds to GABAA receptors with moderate affinity and acts as a partial agonist of GABAA receptors.
E2354 Valepotriate Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABAA, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.
S5596 (1S)-(-)-α-Pinene α-Pinene is found in the oils of many species of many coniferous trees, notably the pine and has insecticidal activity. (1S)-(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site.
S9249 Securinine Securinine, a major natural alkaloid product from the root of the plant Securinega suffruticosa, acts as a γ-amino butyric acid (GABA) receptor antagonist.
S4892 Phenibut Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA), a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
E6459New Phaclofen Phaclofen is a selective antagonist of GABAB receptor. Phaclofen is a peripheral and central baclofen antagonist that is used in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact.
E3607 Crateva nurvala Extract Crateva Nurvala Extract is extracted from the stem bark of Crataeva nurvala Buch.. Crateva nurvala, an important medicinal plant, has been studied mainly with the stem bark part for obstructive and nonobstructive uropathies. Crateva nurvala is also used for the treatment of prostate enlargement and bladder sensitivity.
E0599 Arecaidine hydrochloride Arecaidine hydrochloride, a constituent of the nut of Areca catechu, inhibits the uptake of GABA and beta-alanine, but not that of glycine.
E0101 AZD6280 AZD6280 is a selective GABAA (α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
S4961 3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.
E4920 Baclofen hydrochloride Baclofen hydrochloride is an agonist of the GABAB receptor that mimics the action of GABA, leading to slow presynaptic inhibition via the GABAB receptor. It improves the function of the ubiquitin-proteasome system (UPS) and enhances cell survival in both in vitro and in vivo models of Huntington's disease (HD).
S4661 Tiagabine hydrochloride Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S3663 Afloqualone Afloqualone (AFQ, HQ-495) is a quinazolinone family GABAergic drug with muscle-relaxant and sedative effects, showing the agonist activity at the β subtype of the GABAa receptor.
S4675 Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S6008 p-Hydroxybenzaldehyde p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol), which can be found in the orchids Gastrodia elata, Galeola faberi and vanilla, is a hydroxybenzaldehyde that reacts with NAD+ and H2O to produce 4-hydroxybenzoate, NADH, and 2 protons. This compound at 101.7 μM can significantly reduce the GABA-induced chloride current of GABAA receptors(α1β2γ2S subtype) expressed.
E7965New (2S)-6-Prenylnaringenin (2S)-6-Prenylnaringenin demonstrates the highest efficacy among tested compounds in the forebrain. This compound functions as a positive allosteric modulator of GABAA receptors at the α+β- binding interface.
S1989 GABAA receptor agent 1 GABAA receptor agent 1 is a high affinity ligand for Gamma-aminobutyric acid A (GABAA) receptor that exerts potent anticonvulsant activity.
S4197 Bemegride Bemegride(Bemegrid,3-Ethyl-3-methylglutarimide) is a central nervous system stimulant and antidote for barbiturate poisoning.
S5049 Thiocolchicoside Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.
S0164 AZD7325 AZD7325 is a potent and orally active partial selective Positive allosteric modulator (PAM) of GABAAα2 and Aα3 receptor with Ki=0.3 and 1.3 nM, respectively, and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes.
S9409 Kavain Kavain ((+)-Kavain), the main kavalactone found mostly in the roots of the kava plant, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. This compound positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
S6094 Imidazole-4(5)-acetic Acid Hydrochloride Imidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors.
E2232 Guvacine hydrochloride Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and displays modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
S4772 alpha-Asarone Alpha (α)-asarone (trans-Asarone) is one of the main pharmacologically active compounds present in Acorus calamus Linn (Acoraceae), Acorus tatarinowii Schott (Acoraceae), and Acorus gramineus Solander. It has anticonvulsant, neuroprotective, anxiolytic and nootropic effects.
S5319 Imepitoin Imepitoin(ELB-138,AWD 131-138) is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy. This compound is an antiepileptic and antianxietic drug, it can stimulate different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.
S6100 Picrotoxin Picrotoxin (Picrotin, Cocculin, Cocculus, NSC 403139), a plant alkaloid, is a non-competitive antagonist of neuronal GABA and glycine receptors.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
S3748 Acamprosate Calcium Acamprosate (N-Acetylhomotaurine, Calcium acetylhomotaurinate,N-acetylhomotaurinate) is a synthetic compound with a chemical structure similar to the amino acid neurotransmitter gamma-aminobutyric acid (GABA) and the amino acid neuromodulator taurine.
S6470 Fluralaner Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally. This compound inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls)
E6042 Riluzole hydrochloride Riluzole hydrochloride (PK 26124 hydrochloride) is an antiepileptic drug, a state-dependent inhibitor of Na+ channels and a selective inhibitor of glutamate release. It also inhibits GABA uptake with an IC50 of 43 µM.
S3977 (-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor. This compound has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
S4494 Methionine Methionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity.
S9176 Pimpinellin Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
E3508 Magnolia Obovata Extract Magnolia Obovata Extract is extracted from magnolia obovata, which has an anxiolytic effect through enhancement of the GABA receptor and anti-neuroinflammatory mechanisms.
S5612 Isonipecotic acid Isonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid) is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist.
S6755 NS 11394 NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes.
E0960 RO5186582 RO5186582 (Basmisanil, RG1662) is a highly selective GABAAα5 negative allosteric modulator.
S1168 Valproic Acid sodium Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
J Exp Clin Cancer Res, 2024, 43(1):152
J Immunother Cancer, 2024, 12(11)e009805
Front Pharmacol, 2024, 15:1534772
Verified customer review of Valproic Acid sodium
S7071 (+)-Bicuculline (+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
Commun Biol, 2024, 7(1):1408
Front Pharmacol, 2024, 15:1525753
bioRxiv, 2024, 2024.12.27.630524
Verified customer review of (+)-Bicuculline
S5194 Furosemide sodium Furosemide (Frusemide) sodium is a potent and orally active inhibitor of Na-K-Cl cotransporter (NKCC). Furosemide sodium is a subtype-selective antagonist of gamma-aminobutyric acid type A (GABAA) receptor.
Nat Commun, 2024, 15(1):7342
Ren Fail, 2022, 44(1):1345-1355
S3786 Glabridin Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
Biochem Pharmacol, 2025, 241:117171
Life Sci, 2021, S0024-3205(20)31752-5
S3018 Niflumic acid Niflumic acid (Nifluril) is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
Oncol Lett, 2020, 20(4):39
S9065 Songorine Songorine, a ubiquitous alkaloid in the genus Aconitum, is a novel antagonist of the GABAA receptor in rat brain and has antiarrhythmic, antinociceptive, anti-inflammatory, regenerative and CNS-modulating properties.