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GABA and GABA receptor antagonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (45) Chloride Channel (2) CXCR (1) Cytochrome P450 (1) Dopamine Receptor (1) Environmental Pollutants (1) Glycine Receptor (GlyR) (1) HIV (1) iGluR (7) Isotope-Labeled Compounds (3) nAChR (1) Necroptosis (3) NTPDase (1) P2X Receptor (1) Parasite (1) Potassium Channel (7) Reactive Oxygen Species (ROS) (1) Reference Standards (6) RIP kinase (3) Sodium Channel (3) TRP Channel (3)
By Research Areas:	Infection (2) Inflammation/Immunology (11) Neurological Disease (38)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: GABA Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-103533

Gabazine Maximum Cited Publications 9 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-B1494

Picrotoxinin 4 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-B0339

Primidone 2 Publications Verification	TRP Channel RIP kinase Sodium Channel GABA Receptor Necroptosis	Neurological Disease Inflammation/Immunology
Primidone is the orally active inhibitor for TRPM3 (IC₅₀ = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for **GABA receptor**. Primidone can be used as the analgesic and anticonvulsant agent .

HY-B1240

Droperidol 5 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-17001A

Flupirtine 1 Publications Verification D 9998	Potassium Channel iGluR GABA Receptor	Neurological Disease Inflammation/Immunology
Flupirtine (D 9998) is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a **GABA receptor** activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .

HY-17001

Flupirtine Maleate 1 Publications Verification D 9998 Maleate	Potassium Channel iGluR GABA Receptor	Neurological Disease Inflammation/Immunology
Flupirtine (D 9998) Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a **GABA receptor** activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .

HY-108689

Broflanilide 3 Publications Verification	Environmental Pollutants 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-116564

Lotilaner 1 Publications Verification	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-D0976

NF279 1 Publications Verification	P2X Receptor HIV NTPDase CXCR	Infection
NF279 is a selective P2X1 receptor antagonist and NTPDase inhibitor, with a P2X1 IC₅₀ value of 19 nM. NF279 suppresses GABA-evoked currents, reduces ATP-excited respiratory activity, alters hypoglossal nerve burst parameters, and blocks CXCR4, CCR5, CXCR3, and CXCR7-mediated calcium responses. NF279 arrests HIV-1 fusion downstream of CD4 binding, inhibits R5- and X4-tropic HIV-1 strains. NF279 can be used for the research of HIV-1 infection .

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 is a selective, orally active, blood-brain barrier permeable GABA-B receptor (GABA-B *Receptor) antagonist* with an IC₅₀ of 1.1 μM in rats. SCH 50911 blocks baclofen-induced antitussive effects, regulates neuronal firing and GABA release. SCH 50911 promotes spontaneous seizures during withdrawal in ethanol-dependent rats, alters reward-related neurotransmission, and reduces or suppresses lever responding and self-administration behaviors of alcohol and sucrose in rats. SCH 50911 is applicable to research related to ethanol withdrawal syndrome, absence epilepsy and alcohol use disorder .

HY-B0339R

Primidone (Standard) 2 Publications Verification	Reference Standards TRP Channel RIP kinase Sodium Channel GABA Receptor Necroptosis	Neurological Disease Inflammation/Immunology
Primidone (Standard) is the analytical standard of Primidone. This product is intended for research and analytical applications. Primidone is the orally active inhibitor for TRPM3 (IC₅₀ = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for **GABA receptor**. Primidone can be used as the analgesic and anticonvulsant agent .

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-W050122

S-(+)-GABOB	GABA Receptor	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-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-110230

Flupirtine-d4 hydrochloride D 9998-d4 hydrochloride	Isotope-Labeled Compounds Potassium Channel iGluR GABA Receptor	Neurological Disease Inflammation/Immunology
Flupirtine-d₄ (D 9998-d₄) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a **GABA receptor** activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .

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-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-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-108689R

Broflanilide (Standard)	Reference Standards 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-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-175190

GABA receptor antagonist 2	GABA Receptor	Others
GABA receptor antagonist 2 (Compound IId) is a **GABA receptor** antagonist with a LC₅₀ of 0.0735 μg/mL for Plutella xylostella (P. xylostella). GABA receptor antagonist 2 has significant insecticidal activities against P. xylostella and its resistant strain, and Spodoptera frugiperda, and Chilo suppressalis. GABA receptor antagonist 2 binds the GABA receptor at the site of Drosophila Rdl ^G335. GABA receptor antagonist 2 can be used to manage resistant pest populations .

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-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-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-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 .

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-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-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-103533R

Gabazine (Standard) SR95531 (Standard)	Reference Standards GABA Receptor	Neurological Disease
Gabazine (Standard) is the analytical standard of Gabazine. This product is intended for research and analytical applications. Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.

HY-174147

GABAB receptor antagonist 4	GABA Receptor	Neurological Disease
GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist. GABAB receptor antagonist 4 can inhibit GABA-induced G protein activation. GABAB receptor antagonist 4 competitively binds to the orthosteric site of GABAB receptor. GABAB receptor antagonist 4 can be used to study GABAB receptor-related neurological diseases .

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-12783

SCH 50911 hydrochloride	GABA Receptor	Neurological Disease
SCH 50911 dihydrochloride is a selective, orally active, blood-brain barrier permeable GABA-B receptor (GABA-B *Receptor) antagonist* with an IC₅₀ of 1.1 μM in rats. SCH 50911 dihydrochloride blocks baclofen-induced antitussive effects, regulates neuronal firing and GABA release. SCH 50911 dihydrochloride promotes spontaneous seizures during withdrawal in ethanol-dependent rats, alters reward-related neurotransmission, and reduces or suppresses lever responding and self-administration behaviors of alcohol and sucrose in rats. SCH 50911 dihydrochloride is applicable to research related to ethanol withdrawal syndrome, absence epilepsy and alcohol use disorder .

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-B0339S

Primidone-d5	Isotope-Labeled Compounds RIP kinase TRP Channel Sodium Channel GABA Receptor Necroptosis	Neurological Disease Inflammation/Immunology
Primidone-d₅ is the deuterium labeled Primidone. Primidone is the orally active inhibitor for TRPM3 (IC₅₀ = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for **GABA receptor**. Primidone can be used as the analgesic and anticonvulsant agent .

HY-B1494R

Picrotoxinin (Standard)	Reference Standards 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-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-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 .

HY-W709349

Flupirtine hydrochloride D 9998 hydrochloride	Potassium Channel iGluR GABA Receptor	Neurological Disease Inflammation/Immunology
Flupirtine (D 9998) hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a **GABA receptor** activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .

HY-17001R

Flupirtine Maleate (Standard) D 9998 Maleate (Standard)	Reference Standards Potassium Channel iGluR GABA Receptor	Neurological Disease Inflammation/Immunology
Flupirtine Maleate (Standard) is the analytical standard of Flupirtine Maleate (HY-17001). This product is intended for research and analytical applications. Flupirtine Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a **GABA receptor** activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .

HY-17001AR

Flupirtine (Standard) D 9998 (Standard)	Reference Standards Potassium Channel iGluR GABA Receptor	Neurological Disease Inflammation/Immunology
Flupirtine (Standard) (D 9998 (Standard)) is the analytical standard of Flupirtine (HY-17001A). This product is intended for research and analytical applications. Flupirtine is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a **GABA receptor** activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .

HY-179519

Umbelopsisin A	GABA Receptor Reactive Oxygen Species (ROS)	Neurological Disease
Umbelopsisin A is a GABA_A and GABA_B non-selective agonist. Umbelopsisin A activates the GABAergic pathway, including notch signaling and fatty acid metabolism. Umbelopsisin A shows dual neuroprotection against glutamate excitotoxicity in vitro (reducing ROS and cell death) and in vivo. Umbelopsisin A can be used for the study of glaucoma and broader neurodegenerative disease applications .

HY-129090

CGS-9895	GABA Receptor	Neurological Disease
CGS-9895 is a *GABA* antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors .

HY-183910

Pitrazepin	GABA Receptor Glycine Receptor (GlyR)	Neurological Disease
Pitrazepin is a GABA_A receptor antagonist and glycine receptor antagonist. Pitrazepin blocks synaptic GABA action, induces neuronal bursting and reduces inhibitory postsynaptic potentials. Pitrazepin can be used in research on depression and psychosis .

HY-W709349S

Flupirtine-d6 hydrochloride D 9998-d6 hydrochloride	Isotope-Labeled Compounds Potassium Channel iGluR GABA Receptor	Neurological Disease
Flupirtine-d₆ (D 9998-d₆) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a **GABA receptor** activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .

Cat. No.	Product Name

HY-L070

Neuroprotective Compound Library

1,748 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 1,748 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 4 Publications Verification	Structural Classification other families Terpenoids Sesquiterpenes Plants Source Classification	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	Terpenoids Sesquiterpenes Campanulaceae Campanula medium L. Plants Source Classification	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 Plants Source Classification	Reference Standards 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 .

HY-179519

Umbelopsisin A	Structural Classification Alkaloids Microorganisms Indole Alkaloids Source Classification	GABA Receptor Reactive Oxygen Species (ROS)
Umbelopsisin A is a GABA_A and GABA_B non-selective agonist. Umbelopsisin A activates the GABAergic pathway, including notch signaling and fatty acid metabolism. Umbelopsisin A shows dual neuroprotection against glutamate excitotoxicity in vitro (reducing ROS and cell death) and in vivo. Umbelopsisin A can be used for the study of glaucoma and broader neurodegenerative disease applications .

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.

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 .

HY-B0339S

Primidone-d5
Primidone-d₅ is the deuterium labeled Primidone. Primidone is the orally active inhibitor for TRPM3 (IC₅₀ = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for **GABA receptor**. Primidone can be used as the analgesic and anticonvulsant agent .

HY-W709349S

Flupirtine-d6 hydrochloride

Flupirtine-d₆ (D 9998-d₆) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .

Cat. No.	Product Name		Classification

HY-174147

GABAB receptor antagonist 4		Azide
GABAB receptor antagonist 4 (Compound 28) is a GABAB receptor antagonist. GABAB receptor antagonist 4 can inhibit GABA-induced G protein activation. GABAB receptor antagonist 4 competitively binds to the orthosteric site of GABAB receptor. GABAB receptor antagonist 4 can be used to study GABAB receptor-related neurological diseases .

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GABA and GABA receptor antagonists

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