GABA receptor inhibitor

By Targets:	GABA Receptor (11) Apoptosis (1) Chloride Channel (1) Cytochrome P450 (2) Drug Metabolite (1) nAChR (1) Parasite (1)
By Research Areas:	Infection (1) Inflammation/Immunology (1) Metabolic Disease (3) Neurological Disease (5)

Targets Recommended: GABA Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-16974

Afoxolaner	GABA Receptor Chloride Channel Parasite	Infection
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-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 .

HY-100800

TACA trans-4-Aminocrotonic acid
TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABA_A and GABA_C receptors (K_D= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons .

HY-103526

DPNI-GABA	GABA Receptor	Neurological Disease
DPNI-GABA is a nitroindoline cage compound that inhibits *GABA(A)* receptors and reduces GABA-evoked peak responses with an IC₅₀ value of 0.5 mM .

HY-155381

APS3

GABA Receptor nAChR Others

APS3 is a GABA and nACh receptors inhibitor, with a LC₅₀ of 7.2423 μg/mL against Plutella xylostella .

APS3	GABA Receptor nAChR	Others
APS3 is a *GABA* and nACh receptors inhibitor, with a LC₅₀ of 7.2423 μg/mL against Plutella xylostella .

HY-156339

GABA receptor Antagonist 1	GABA Receptor	Others
GABA receptor Antagonist 1 (compound 7w) inhibits Px RDL1 GABAR with an IC₅₀ value of 7.08 nmol/L. GABA receptor Antagonist 1 shows insecticide activity against P. xylostella, S. frugiperda, S. exigua, and S. litura, with LC₅₀ of 0.09, 0.84, 0.87, and 0.68 mg/L respectively. GABA receptor Antagonist 1 shows a medium toxicity to honeybee (48 h, ID₅₀ = 2.22 μg/adult), and low toxicity to zebrafish (LC₅₀: 42.4 mg/L) .

HY-B1494

Picrotoxinin 3 Publications Verification
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 .

HY-124030

3-Hydroxyphenazepam	Drug Metabolite	Neurological Disease
3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAA receptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ ³H]GABA uptake .

HY-108689

Broflanilide 1 Publications Verification	GABA Receptor	Neurological Disease
Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) **GABA Receptor*, and inhibits* S. litura RDL GABAR, with an IC₅₀ value of 1.3 nM .

HY-B0822

Fipronil
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits **GABA receptor with IC₅₀s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis** in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .

HY-101060

FGIN 1-43
FGIN 1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety .

HY-B0822R

Fipronil (Standard)	GABA Receptor Cytochrome P450 Apoptosis	Neurological Disease
Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits **GABA receptor with IC₅₀s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis** in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .

HY-10061

Lesogaberan AZD-3355	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan for rat GABA_B and GABA_A receptors, as measured by displacement of [ ³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

HY-10061B

Lesogaberan hydrochloride AZD-3355 hydrochloride	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptor. The affinity (K_is) of Lesogaberan hydrochloride for rat GABA_B and GABA_A receptors, as measured by displacement of [ ³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

HY-10061A

Lesogaberan napadisylate AZD-3355 napadisylate	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. The affinity (K_is) of Lesogaberan napadisylate for rat GABA_B and GABA_A receptors, as measured by displacement of [ ³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

HY-125296

Fipronil sulfone	GABA Receptor	Neurological Disease
Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC₅₀ of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).

HY-B0822S1

Fipronil-13C6	GABA Receptor Cytochrome P450	Inflammation/Immunology
Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

Cat. No.	Product Name

HY-L120

GABA Receptor Compound Library	139 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 139 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

GABA Receptor Compound Library

139 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 139 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

Cat. No.	Compare	Product Name	Species	Source

HY-P72166

	DBI Protein, Human (103a.a, His) ACBD1; ACBP; ACBP_HUMAN; Acyl CoA binding domain containing 1; Acyl CoA binding protein; Acyl Coenzyme A binding domain containing 1; Acyl coenzyme A binding protein; Acyl-CoA-binding protein; CCK RP; CCKRP; Cholecystokinin releasing peptide trypsin sensitive; DBI; Diazepam-binding inhibitor; Endozepine; EP; GABA receptor modulator; MGC70414	Human	E. coli
	DBI, a versatile protein, binds medium- and long-chain acyl-CoA esters, indicating a potential intracellular carrier role. It also displaces diazepam from the benzodiazepine recognition site on the GABA type A receptor. This dual functionality suggests DBI may act as a neuropeptide, modulating GABA receptor activity. Remarkably, DBI functions as a monomer in these interactions. DBI Protein, Human (103a.a, His) is the recombinant human-derived DBI protein, expressed by E. coli , with N-6*His labeled tag. The total length of DBI Protein, Human (103a.a, His) is 103 a.a., with molecular weight of ~14 kDa.


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Cat. No.	Product Name	Chemical Structure

HY-B0822S1

Fipronil-13C6
Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

Fipronil-13C6

Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

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Inhibitors & Agonists

Screening Libraries

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