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GABA(A)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (200) 5-HT Receptor (5) AAK1 (2) Akt (1) Apoptosis (4) Bacterial (3) Calcium Channel (2) Chloride Channel (2) COX (2) Cytochrome P450 (2) DNA/RNA Synthesis (1) Dopamine Receptor (2) Drug Metabolite (3) Dynamin (2) Endogenous Metabolite (23) ERK (1) Fungal (2) Histamine Receptor (1) iGluR (3) Interleukin Related (2) Isotope-Labeled Compounds (10) JNK (1) Keap1-Nrf2 (1) Lipoxygenase (1) nAChR (3) NKCC (4) Opioid Receptor (1) Parasite (1) Phosphodiesterase (PDE) (1) Potassium Channel (4) Reactive Oxygen Species (2) RSV (2) Sirtuin (1) Sodium Channel (4) TNF Receptor (2)
By Research Areas:	Cancer (21) Cardiovascular Disease (5) Infection (4) Inflammation/Immunology (15) Metabolic Disease (11) Neurological Disease (192)
Click Chemistry:	Alkynes (2)
Oligonucleotides:	Cholesterol (1)

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GABAA receptor agent 1	GABA Receptor	Neurological Disease
GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity .

GABAA receptor modular-4	GABA Receptor	Neurological Disease
GABAA receptor module-4 (9eey) is a GABAA receptor modulator that can be used in the study of central nervous system diseases .

GABAA receptor agonist 2	GABA Receptor	Neurological Disease
GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .

GABAA receptor agonist 1	GABA Receptor	Neurological Disease
GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .

GABAA receptor agent 8	GABA Receptor	Neurological Disease
GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy .

GABAA receptor agent 7	GABA Receptor	Neurological Disease
GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy .

GABAA receptor modular-3	GABA Receptor	Neurological Disease
GABAA receptor modular-3 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC₅₀ of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modular-3 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modular-3 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression .

GABAA receptor agent 4	GABA Receptor	Neurological Disease
GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an K_i of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential .

GABAA receptor agent 2 TFA	GABA Receptor	Neurological Disease
GABAA receptor agent 2 TFA is a potent and high-affinity GABA_A receptor antagonist with an IC₅₀ of 24 nM (human α1β2γ2 GABA_A-expressing tsA201 cells) and a K_i of 28 nM (*rat GABA_A* receptors*). GABAA* receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) .

GABAA receptor modulator-2	GABA Receptor	Neurological Disease
GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABA_AR negative allosteric modulator (NAM) with a K_i of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .

GABAA receptor agent 2	Others	Others
GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.

GABAA receptor agent 5	GABA Receptor	Neurological Disease
GABAA receptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an K_i of 0.020 µM. GABAA receptor agent 5 shows γ-GABAAR antagonist activity with low cellular membrane permeability .

GABAA receptor agent 6	GABA Receptor	Neurological Disease
GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an K_i of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability .

MRK-898	GABA Receptor	Neurological Disease
MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with K_i values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s) .

(-)-Bicuculline methobromide Maximum Cited Publications 21 Publications Verification l-Bicuculline methobromide	GABA Receptor	Neurological Disease
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent *GABA_A* receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca ²⁺-activated K ⁺ channels in various types of neurons .

(-)-Bicuculline methochloride l-Bicuculline methochloride	GABA Receptor	Neurological Disease
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent *GABA_A* receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca ²⁺-activated K ⁺ channels in various types of neurons .

Panadiplon FG 10571; PNU 78875	GABA Receptor	Neurological Disease
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a *5GABAA* partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .

RWJ-51204	GABA Receptor	Neurological Disease
RWJ-51204 is a partial agonist of GABA(A) receptor, with K_i of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.

MmTx1 toxin Micrurotoxin 1	GABA Receptor	Neurological Disease
MmTx1 toxin (Micrurotoxin 1) is an allosteric *GABA_A* receptor modulator that increases GABA_A receptor susceptibility to agonist .

Picrotoxinin 3 Publications Verification	Chloride Channel GABA Receptor	Neurological Disease
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA_A receptor antagonist, which negatively modulates the action of GABA on GABA_A receptors. Picrotoxinin inhibits α₁β₂γ_2L GABA_A receptor with an IC₅₀ of 1.15 μM .

MRK-016	GABA Receptor	Cancer
MRK-016 is a selective, orally bioavailable inverse agonist of GABA_A α5 receptor, with an EC₅₀ of 3 nM for GABA_A α5, and K_is of 0.83, 0.85, 0.77?and 1.4?nM for human?GABA_A?α1β3γ2, GABA_A?α2β3γ2, GABA_A?α3β3γ2, and GABA_A?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.

Thiomuscimol	Others	Others
Thiomuscimol is a GABAA receptor agonist (IC₅₀=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.

SB-205384	GABA Receptor	Neurological Disease
SB-205384 is a *GABAA* receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist .

Basmisanil 1 Publications Verification RG1662; RO5186582	GABA Receptor	Neurological Disease
Basmisanil (RG1662) is a highly selective orally active *α subunit-containing GABAA* receptors (GABAAα5)** negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a K_i value of 5 nM and IC₅₀ value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .

Picrotoxinin (Standard)	Chloride Channel GABA Receptor	Neurological Disease
Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC₅₀ of 1.15 μM .

Isonipecotic acid	GABA Receptor	Neurological Disease
Isonipecotic acid is a GABAA receptor partial agonist .

PF-0713	GABA Receptor	Cancer
PF 0713 is a *GABAA* receptor agonist. .

NS11394 3 Publications Verification	GABA Receptor	Neurological Disease
NS11394 is an orally active and unique subtype-selective *GABA_A* positive allosteric receptor (PAM), with a K_i of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABA_A-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .

Xilmenolone	GABA Receptor	Neurological Disease
Xilmenolone is a GABAA receptor positive allosteric modulator .

HZ166	GABA Receptor	Neurological Disease
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and *α3-GABAA* receptors**. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

U93631	GABA Receptor	Neurological Disease
U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.

SL651498	GABA Receptor	Neurological Disease
SL651498 is a full agonist of α2 and *α3 GABAA* receptors, and a partial agonist of α1 and α5 GABAA receptors**. SL651498 shows anxiolytic and anticonvulsant activities .

(-)-Securinine 1 Publications Verification	GABA Receptor	Neurological Disease Cancer
(-)-Securinine is plant-derived alkaloid and also a GABA_A receptor antagonist.

6,2'-Dihydroxyflavone	GABA Receptor	Neurological Disease
6,2'-Dihydroxyflavone is a novel antagonist of GABA_A receptor.

Flumazenil 3 Publications Verification Ro 15-1788	GABA Receptor	Neurological Disease
Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

Dihydroergotoxine mesylate Ergoloid mesylates	GABA Receptor	Neurological Disease
Dihydroergotoxine mesylate is a series of alkaloid salt mixtures with high binding activity to GABAA receptors.

Flumazenil acid Ro 15-3890	GABA Receptor Drug Metabolite	Neurological Disease
Flumazenil acid is a metabolite of Flumazenil . Flumazenil is a GABAA receptor antagonist .

Brexanolone caprilcerbate	GABA Receptor	Neurological Disease
Brexanolone caprilcerbate is a potent *GABAA* receptor positive allosteric modulator .

MmTx2 toxin Micrurotoxin 2	GABA Receptor	Neurological Disease
MmTx2 toxin is a *GABA_A* receptor modulator that enhances *GABA_A* receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .

ONO-8590580	GABA Receptor	Neurological Disease
ONO-8590580 is a GABA_A α5 negative allosteric modulator.

6-Aminonicotinic acid	GABA Receptor	Others
6-Aminonicotinic acid is a GABA_A receptor agonist with K_i value of 4.4 nM .

6'''-Feruloylspinosin	GABA Receptor	Neurological Disease
6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons .

CP-409092	GABA Receptor	Neurological Disease
CP-409092 is a partial agonist of GABA_A receptor, with anti-anxiety activity .

U-101017 PNU 101017	GABA Receptor	Neurological Disease
U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.

Cirsimaritin	GABA Receptor	Neurological Disease
Cirsimaritin binds weakly to the benzodiazepine site on *GABA_A* receptors, with antidepressant, anxiolytic and antinociceptive activities.

CP-409092 hydrochloride	GABA Receptor	Neurological Disease
CP-409092 hydrochloride is a partial agonist of GABA_A receptor, with anti-anxiety activity .

Cat. No.	Product Name

HY-L120

GABA Receptor Compound Library

145 compounds

GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). GABA receptors are significant drug targets in the treatment of neuropsychiatric disorders such as epilepsy, insomnia, and anxiety, as well as in anesthesia in surgical operations.

MCE offers a unique collection of 145 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

Cat. No.	Product Name	Type

HY-D1704

Bodipy TMR-X muscimol	Fluorescent Dyes/Probes
Bodipy TMR-X muscimol is a Bodipy labeled Muscimol (HY-N2313) (Ex=543 nm, Em=572 nm). Muscimol is a GABAA agonist. Bodipy TMR-X muscimol can be used for imaging the spread of reversible brain inactivations .

Cat. No.	Product Name	Type

HY-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate	Drug Delivery
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.

Cat. No.	Product Name	Target	Research Area

HY-P5964A

K1 peptide TFA	Peptides	Neurological Disease
K1 peptide TFA is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP) .

HY-P1083

Dynamin inhibitory peptide 1 Publications Verification	Dynamin	Neurological Disease
Dynamin inhibitory peptide competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide blocks the dopamine D3 effect on GABAA receptors .

HY-P5860

MmTx1 toxin Micrurotoxin 1	GABA Receptor	Neurological Disease
MmTx1 toxin (Micrurotoxin 1) is an allosteric *GABA_A* receptor modulator that increases GABA_A receptor susceptibility to agonist .

HY-P5857

MmTx2 toxin Micrurotoxin 2	GABA Receptor	Neurological Disease
MmTx2 toxin is a *GABA_A* receptor modulator that enhances *GABA_A* receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .

HY-P5964

K1 peptide	Peptides	Neurological Disease
K1 peptide is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP) .

HY-P1083A

Dynamin inhibitory peptide TFA	Dynamin	Neurological Disease
Dynamin inhibitory peptide TFA competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide TFA blocks the dopamine D₃ effect on GABA_A receptors .

Species:	Human (8)
Tag:	His (5) Strep (3) GST (1) MBP (1) Fc (1)
Source:	HEK293 (3) E. coli (5)

Cat. No.	Compare	Product Name	Species	Source

HY-P72639

	GABARAP Protein, Human (His, Fc) GABA(A) Receptor-Associated Protein; GABARAP Protein; HCG1987397 Isoform CRA_b; GABARAP	Human	E. coli
	GABARAP (gamma-aminobutyric acid receptor-associated protein) is a protein that performs multiple functions within cells. As a ubiquitin-like modifier, it participates in the intracellular transport of GABA(A) receptors and interacts with the cytoskeleton. GABARAP Protein, Human (His, Fc) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-His, C-hFc labeled tag. The total length of GABARAP Protein, Human (His, Fc) is 117 a.a., with molecular weight of ~50 kDa.

HY-P70913

	GABARAPL1/GEC-1 Protein, Human (His) Gamma-Aminobutyric Acid Receptor-Associated Protein-Like 1; Early Estrogen-Regulated Protein; GABA(A) Receptor-Associated Protein-Like 1; Glandular Epithelial Cell Protein 1; GEC-1; GABARAPL1; GEC1	Human	E. coli
	GABARAPL1/GEC-1 is a multifunctional ubiquitin-like modifier that contributes to cell surface expression of kappa-type opioid receptors and contributes to autophagy, shaping autophagosome vacuoles.Unlike LC3, which is involved in phagophore elongation, the GABARAP/GATE-16 subfamily plays a crucial role in late autophagosome maturation.GABARAPL1/GEC-1 Protein, Human (His) is the recombinant human-derived GABARAPL1/GEC-1 protein, expressed by E.coli , with N-6*His labeled tag.

HY-P71447

	GABRB2 Protein, Human (His) GABA(A) receptor subunit beta-2	Human	E. coli
	GABRB2 protein is an important component of heteropentameric GABA receptors that form ligand-gated chloride channels. It plays a crucial role in establishing functional inhibitory GABAergic synapses, contributing to synaptic depression. GABRB2 Protein, Human (His) is the recombinant human-derived GABRB2 protein, expressed by E. coli , with N-His labeled tag.

HY-P76942

	GABARAP Protein, Human (His-MBP) GABA(A) Receptor-Associated Protein; HCG1987397 Isoform CRA_b	Human	E. coli
	GABARAP Protein is essential for regulating ubiquitination and degradation of TIAM1, a guanyl-nucleotide exchange factor (GEF) involved in RAC1 activation and downstream signaling. The D6/7 E3 ubiquitin ligase complex, where GABARAP is a key component, contributes to diverse biological processes, including cytoskeletal organization, cell migration, proliferation, and apoptosis. GABARAP Protein, Human (His-MBP) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-His, N-MBP labeled tag. The total length of GABARAP Protein, Human (His-MBP) is 117 a.a., with molecular weight of 49-58 kDa.

HY-P70861

	GABARAP Protein, Human (GST) GABA(A) Receptor-Associated Protein; GABARAP Protein; HCG1987397 Isoform CRA_b; GABARAP	Human	E. coli
	GABARAP (gamma-aminobutyric acid receptor-associated protein) is a protein that performs multiple functions within cells. As a ubiquitin-like modifier, it participates in the intracellular transport of GABA(A) receptors and interacts with the cytoskeleton. GABARAP Protein, Human (GST) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-GST labeled tag. The total length of GABARAP Protein, Human (GST) is 117 a.a., with molecular weight of ~37.0 kDa.

HY-P703132

	GABRR1 Protein, Human (HEK293, Strep) Gamma-aminobutyric acid receptor subunit rho-1; GABA(A) receptor subunit rho-1; GABAAR subunit rho-1; GABA(C) receptor; GABRR1; Homo sapiens; Human; Chloride channel; Ion channel	Human	HEK293

HY-P703130

	GABRA1-GABRB2-GABRG2 Protein, Human (HEK293, Strep) Gamma-aminobutyric acid receptor subunit alpha-1; GABA(A) receptor subunit alpha-1; GABAAR subunit alpha-1; GABRA1; Homo sapiens; Human; Chloride channel; Ion channel; Ligand-gated ion channel; Receptor	Human	HEK293

HY-P703131

	GABRA5-GABRB3 Protein, Human (HEK293, His, Strep) Gamma-aminobutyric acid receptor subunit alpha-5; GABA(A) receptor subunit alpha-5; GABAAR subunit alpha-5; GABRA5; Homo sapiens; Human; GABAAR subunit alpha-5; Chloride channel; Ion channel; Ligand-gated ion channel; Receptor;	Human	HEK293

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Cat. No.	Compare	Product Name	Application	Reactivity

HY-P82013

	GABA A Receptor beta 2 Antibody (YA1758) GABA; GABA(A) receptor beta 2; GABA(A) receptor subunit beta-2; GABRB2	WB	Human, Mouse, Rat
	GABA A Receptor beta 2 Antibody (YA1758) is a biotin-conjugated non-conjugated IgG antibody, targeting GABA A Receptor beta 2, with a predicted molecular weight of 59 kDa (observed band size: 59 kDa). GABA A Receptor beta 2 Antibody (YA1758) can be used for WB experiment in human, mouse, rat background.

HY-P82516

	GABA A Receptor beta 1 Antibody (YA2261) GABA-A receptor; beta-1 polypeptide; Gabrb-1; GABRB1; GARB1	WB	Human, Mouse, Rat
	GABA A Receptor beta 1 Antibody (YA2261) is a biotin-conjugated non-conjugated IgG antibody, targeting GABA A Receptor beta 1, with a predicted molecular weight of 54 kDa (observed band size: 48 kDa). GABA A Receptor beta 1 Antibody (YA2261) can be used for WB experiment in human, mouse, rat background.

HY-P81570

	GABA A Receptor alpha 1 Antibody (YA1315) Gabra1, Gabra-1	WB, IHC-P	Mouse, Rat
	GABA A Receptor alpha 1 Antibody (YA1315) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1315), targeting GABA A Receptor alpha 1, with a predicted molecular weight of 52 kDa (observed band size: 52 kDa). GABA A Receptor alpha 1 Antibody (YA1315) can be used for WB, IHC-P experiment in mouse, rat background.

HY-P82504

	GABA A Receptor alpha 5 Antibody (YA2249) GAA 5; GAA5; GABRA 5; Gabra5	WB, ICC/IF	Human, Mouse, Rat
	GABA A Receptor alpha 5 Antibody (YA2249) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2249), targeting GABA A Receptor alpha 5, with a predicted molecular weight of 52 kDa (observed band size: 70 kDa). GABA A Receptor alpha 5 Antibody (YA2249) can be used for WB, ICC/IF experiment in human, mouse, rat background.