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Results for "

GABAaR

" in MedChemExpress (MCE) Product Catalog:

By Targets:	GABA Receptor (14) Isotope-Labeled Compounds (1)
By Research Areas:	Inflammation/Immunology (1) Neurological Disease (13)

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-120051

Afizagabar S44819; Egis-13529	GABA Receptor	Neurological Disease
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the *α5-GABAAR, with an IC₅₀* of 585 nM for α5β2γ2 and a K_i of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .

HY-107782

Picrotin	GABA Receptor	Neurological Disease
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

HY-115685

3-Methyl-GABA	GABA Receptor	Neurological Disease
3-Methyl-GABA is a potent *GABA* aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABA_A receptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity .

HY-145257

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 .

HY-145258

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 .

HY-147657

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 .

HY-145256

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 .

HY-170903

GABAA receptor modulator-3	GABA Receptor	Neurological Disease
GABAA receptor modulator-3 (compound 3b) is a positive allosteric modulator (PAM). GABAA receptor modulator-3 inhibits α1β3γ2 GABAAR at peak and steady state currents with IC₅₀s of 671 and 64 μM, respectively .

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-156061

NAP-1	GABA Receptor	Neurological Disease Inflammation/Immunology
NAP-1 is a compound with agent that can suppress or relieve pain. effects. NAP-1 enhances the inhibitory current by binding to a specific site of *GABAaR*, resulting in a narcotic effect. NAP-1 can be used in research to develop clinical agent that can suppress or relieve pain .

HY-10232

THIP 1 Publications Verification Gaboxadol	GABA Receptor	Neurological Disease
THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC₅₀ value of 13 µM for *δ-GABAAR. THIP induces strong tense GABAA*-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .

HY-107782R

Picrotin (Standard)	GABA Receptor	Neurological Disease
Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

HY-109009

Padsevonil 1 Publications Verification UCB-0942	GABA Receptor	Neurological Disease
Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of *GABA_AR*, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .

HY-10232S

THIP-d4 Gaboxadol-d₄	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC₅₀ value of 13 μM for *δ-GABAAR. THIP induces strong tense GABAA*-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-107782

Picrotin	Structural Classification other families Iridoids Terpenoids Source classification Plants	GABA Receptor
Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

HY-107782R

Picrotin (Standard)	Structural Classification other families Iridoids Terpenoids Source classification Plants	GABA Receptor
Picrotin (Standard) is the analytical standard of Picrotin. This product is intended for research and analytical applications. Picrotin is an active compound, also is one of the composition of picrotoxin (an antagonist of GABAA receptors (GABAARs) and glycine receptors (GlyRs)). Picrotin has sensitivity for GlyRs with IC₅₀ values range from 5.2 μM to 106 μM. Picrotin can be used for the research of neurotransmission .

Species:	Human (3)
Tag:	His (1) Strep (3)
Source:	HEK293 (3)

Cat. No.	Compare	Product Name	Species	Source

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

HY-P703132

	GABRR1 Protein, Human (HEK293, StrepⅡ) 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

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Cat. No.	Product Name	Chemical Structure

HY-10232S

THIP-d4
THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC₅₀ value of 13 μM for *δ-GABAAR. THIP induces strong tense GABAA*-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .

THIP-d4

THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC₅₀ value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .

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