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GABA receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (28) Chloride Channel (2) Cytochrome P450 (1) Dopamine Receptor (1) Leukotriene Receptor (1) nAChR (1) Parasite (1) Platelet-activating Factor Receptor (PAFR) (1)
By Research Areas:	Infection (1) Inflammation/Immunology (3) Neurological Disease (23)

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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 Maximum Cited Publications 6 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-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-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-117256

Gabazine free base SR95531 free base	GABA Receptor	Inflammation/Immunology
Gabazine is a selective and competitive antagonist of GABA_A receptor, with an IC₅₀ of 0.2 μM for GABA receptor .

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-115856

Sch 50910	GABA Receptor	Neurological Disease
Sch 50910 is a GABA(B) receptor antagonist with some activity in inhibiting GABA(B) autoreceptors. Sch 50910 had no effect on electrically stimulated release at a concentration of 100 μM. The activity of Sch 50910 suggests that it may not have a significant role in studies of GABA(B) receptor function .

HY-103495

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-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	GABA Receptor	Neurological Disease
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-101207

NCS-382	GABA Receptor	Neurological Disease
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-103513

GABAA receptor agent 2	GABA Receptor	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.

HY-123222

CGP 56999	GABA Receptor	Neurological Disease
CGP 56999 is a potent antagonist **GABA(B) receptor, with the IC₅₀** of 0.002 μM. CGP 56999 increased the levels of BDNF mRNA in the brain in vivo and in vitro .

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-B1240

Droperidol 3 Publications Verification Dehydrobenzperidol	Dopamine Receptor GABA Receptor nAChR	Neurological Disease
Droperidol (Dehydrobenzperidol) is a butyrophenone pamine-2 receptor antagonist that inhibits the activation of *GABA(A)* and neuronal nicotinic receptors (nAChR), with IC₅₀ values of 12.6 nM and 5.8 μM. Droperidol has anesthetic and sedative properties .

HY-B1494

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 .

HY-W025443

6-(4-Methoxyphenyl)pyridazin-3-amine	GABA Receptor	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-B1494R

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 .

HY-108689R

Broflanilide (Standard)	GABA Receptor	Neurological Disease
Broflanilide (Standard) is the analytical standard of Broflanilide. This product is intended for research and analytical applications. 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-W050122

S-(+)-GABOB	Others	Neurological Disease
S-(+)-GABOB is an endogenous ligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor .

HY-114076

CGP55845	GABA Receptor	Neurological Disease
CGP55845 is a potent and selective GABAB receptor antagonist with activity that blocks agonist binding. The IC50 value of CGP55845 is 5 nM, indicating that it exhibits significant activity in inhibiting GABA and glutamate release. The apparent Kd of CGP55845 when forming a complex with the GABAB receptor is 30 nM, indicating its high affinity for this receptor. CGP55845 is as potent as 100 μM CGP 35348 in relieving the inhibitory effect of (R)-(-)-baclofen .

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-163101

CP-96021	Platelet-activating Factor Receptor (PAFR) Leukotriene Receptor	Inflammation/Immunology
CP-96021 is a potent and orally available leukotriene D₄ (LTD₄ K_i=34 μM) / platelet activating factor (PAF K_i=37 μM) receptor antagonist. CP-96021 has antagonist capable of simultaneously targeting two different inflammatory mediators, LTD₄ and PAF. CP-96021 shows high specificity for α1, α2, β, dopamine-2, adenosine 1, 5-HT1, H1, muscarine, μ opioid, and *GABA* receptors, all expressing IC₅₀ values greater than 10 μM. CP-96021 can be used to study the pathogenesis of many inflammatory diseases such as asthma .

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.

HY-129907

2-AEMP 2-Aminoethyl methylphosphonate	GABA Receptor	Neurological Disease
2-AEMP (2-Aminoethyl methylphosphonate) is an anti-GABA(A)-ρ1 receptor compound with antagonist activity. 2-AEMP exhibits competitive inhibition compared to TPMPA with an IC(50) value of 18 μM, compared to 7 μM for TPMPA. The release rate of inhibition at termination of 2-AEMP is significantly higher than that of TPMPA. The preincubation time required for the onset of inhibition of 2-AEMP is much shorter than that of TPMPA. Some analogs of 2-AEMP, especially those with benzyl or n-butyl substituents, show lower potency in terms of biological activity .

Cat. No.	Product Name

HY-L070

Neuroprotective Compound Library	1,225 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 1,225 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.

Neuroprotective Compound Library

1,225 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 1,225 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-B1494

Picrotoxinin 3 Publications Verification	Structural Classification Natural Products other families Source classification Plants	Chloride Channel GABA Receptor
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-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 .

HY-B1494R

Picrotoxinin (Standard)	Structural Classification Natural Products other families Source classification Plants	Chloride Channel GABA Receptor
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 .

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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GABA receptor antagonist

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