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Results for "

GABA receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (17) Cytochrome P450 (1) Parasite (1)
By Research Areas:	Infection (1) Inflammation/Immunology (1) Neurological Disease (14)

Inhibitors & Agonists

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Isotope-Labeled Compounds

Targets Recommended: GABA Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W008645

NCS-382 sodium	GABA Receptor	Neurological Disease
NCS-382 (sodium) is a potent *GABA* receptor antagonist. NCS-382 (sodium) has anti-sedative and anti-hypnotic activities and can be used in research related to neurological diseases .

HY-139145

Etbicyphat Trimethylopropane phosphate	GABA Receptor	Neurological Disease
Etbicyphat (Trimethylopropane phosphate) is a potent **GABA(A) receptors** competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors .

HY-103533

Gabazine 5 Publications Verification SR95531	GABA Receptor	Neurological Disease
Gabazine is a selective and competitive antagonist of GABA_A receptor, with an IC₅₀ of ~0.2 μM for GABA receptor.

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-N3478

Isohyenanchin Hydroxycoriatin	GABA Receptor	Neurological Disease
Isohyenanchin (Hydroxycoriatin) is an RDLac homo-oligomers antagonist. Isohyenanchin also is a weak antagonist of ionotropic GABA receptors .

HY-103495

17-PA

GABA Receptor Neurological Disease

17-PA is a selective antagonist of neurosteroid potentiation and direct gating of GABA ^A receptors .

17-PA	GABA Receptor	Neurological Disease
17-PA is a selective antagonist of neurosteroid potentiation and direct gating of GABA ^A receptors .

HY-139145S

Etbicyphat-13C3 Trimethylopropane phosphate-¹³C₃	GABA Receptor	Neurological Disease
Etbicyphat- ¹³C₃ is the ¹³C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].

HY-116564

Lotilaner	Parasite GABA Receptor	Infection
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC₅₀ of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor .

HY-129636

(E)-GABAB receptor antagonist 1	GABA Receptor	Neurological Disease
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC₅₀ of 37.9 μM .

HY-12783

SCH 50911 hydrochloride	GABA Receptor	Neurological Disease
SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B *GABA(B)* receptor antagonist, binds to GABA(B) receptor with IC₅₀ of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated ³H overflow with an IC₅₀ of 3 μM.

HY-100798

Phaclofen
Phaclofen is a selective GABA_B receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact .

HY-12783A

SCH 50911	GABA Receptor	Neurological Disease
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B *GABA(B)* receptor antagonist, binds to GABA(B) receptor with IC₅₀ of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated ³H overflow with an IC₅₀ of 3 μM .

HY-129636A

GABAB receptor antagonist 1	GABA Receptor	Neurological Disease
GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC₅₀ of 37.9 μM .

HY-101207

NCS-382
NCS-382 is a potent *GABA* receptor antagonist and also a GHBR receptor antagonist. NCS-382 has anticonvulsant and antisedative activity. NCS-382 is used in the related research of hereditary nervous system diseases .

HY-103518

CGP36216	GABA Receptor	Neurological Disease
CGP36216 is a selective antagonist at **GABA presynaptic receptor*. CGP36216 binds to GABAB receptor* with a K_i value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .

HY-103518A

CGP36216 hydrochloride	GABA Receptor	Neurological Disease
CGP36216 hydrochloride is a selective antagonist at **GABA presynaptic receptor*. CGP36216 binds to GABAB receptor* with a K_i value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .

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-W025443

6-(4-Methoxyphenyl)pyridazin-3-amine	Others	Others
6-(4-Methoxyphenyl)pyridazin-3-amine is an aminopyridazine derivative, and can be used for the synthesis of SR 95103. SR 95103 is a selective and competitive **GABA-A receptor** antagonist .

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-135482

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) .

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.

Neuroprotective Compound Library	1068 compounds
Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases. MCE offers a unique collection of 1068 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N3478

Isohyenanchin Hydroxycoriatin	Structural Classification Terpenoids Sesquiterpenes Source classification Campanulaceae Campanula medium L. Plants	GABA Receptor
Isohyenanchin (Hydroxycoriatin) is an RDLac homo-oligomers antagonist. Isohyenanchin also is a weak antagonist of ionotropic GABA receptors .

Cat. No.	Product Name	Chemical Structure

HY-139145S

Etbicyphat-13C3
Etbicyphat- ¹³C₃ is the ¹³C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].

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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