GABAA receptor chloride channel

Pathways Recommended:	Membrane Transporter/Ion Channel

By Targets:	Chloride Channel (4) Adrenergic Receptor (1) Calcium Channel (2) Dopamine Receptor (1) Drug Derivative (1) Endogenous Metabolite (1) GABA Receptor (16) iGluR (1) Insecticide (1) nAChR (1) Phosphodiesterase (PDE) (1) Potassium Channel (4) Reference Standards (4) Sodium Channel (5)
By Research Areas:	Cancer (1) Cardiovascular Disease (2) Infection (1) Metabolic Disease (2) Neurological Disease (18)
Oligonucleotides:	Cholesterol (1)

Targets Recommended: Chloride Channel Sodium Chloride Cotransporter (NCC)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N0219

Bicuculline 35+ Cited Publications (+)-Bicuculline	GABA Receptor	Neurological Disease
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter *GABA_A* receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca ²⁺ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .

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-172431

Opakalim BHV-7000	Potassium Channel	Neurological Disease
Opakalim (BHV-7000) is a selective Kv7.2/7.3 potassium channels activator with an EC₅₀ of 0.6 μM. Opakalim shows minimal GABAA receptor activation and exhibits potent anti-seizure efficacy in the maximal electroshock seizure (MES) model. Opakalim can be used for the study of seizures .

HY-108584

Flindokalner BMS-204352	Potassium Channel	Neurological Disease
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (K_i=3.7 μM), and acts as a negative modulator of *GABAA* receptors. Flindokalner shows anxiolytic efficacy in vivo .

HY-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate	nAChR GABA Receptor Potassium Channel Endogenous Metabolite	Cancer
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, **GABAA receptor*, and the inward-rectifier potassium ion channel*.

HY-B0799

Dihydroergotoxine mesylate Ergoloid mesylates	GABA Receptor Chloride Channel Adrenergic Receptor Dopamine Receptor Phosphodiesterase (PDE)	Cardiovascular Disease Neurological Disease
Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the **GABA_A receptor** associated Cl ^- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity .Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the **GABA_A receptor** associated Cl ^- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity .

HY-137790

Bicuculline methochloride Maximum Cited Publications 39 Publications Verification (-)-Bicuculline methochloride	GABA Receptor	Neurological Disease
Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective **GABAA receptor antagonist with an IC₅₀** value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca ²⁺ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders .

HY-B1671

(+)-Kavain	GABA Receptor Sodium Channel Calcium Channel	Neurological Disease Metabolic Disease
(+)-Kavain, a main kavalactone that can be extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na ⁺ and Ca ²⁺ channels . (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

HY-100783B

Bicuculline methobromide (+)-Bicuculline methobromide	GABA Receptor	Neurological Disease
Bicuculline methobromide is a selective **GABAA Receptor antagonist with an IC₅₀** value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca ²⁺ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders .

HY-N0219R

Bicuculline (Standard) (+)-Bicuculline (Standard)	Reference Standards GABA Receptor	Neurological Disease
Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .

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-114706

Suritozole MDL-26479	GABA Receptor	Neurological Disease
Suritozole (MGL-26479) is a cognitive enhancer that acts as a partial inverse agonist of benzodiazepine receptor sites on *GABAA* ion channel complexes. Suritozole can be used in the study of neurodegenerative diseases .

HY-170930

Anticonvulsant agent 9	GABA Receptor Sodium Channel	Neurological Disease
Anticonvulsant agent 9 (compound 4f) is an α1β2γ2 *GABAA* receptors activator. Anticonvulsant agent 9 activatesα1β2γ2 *GABAA* receptors with an EC₅₀ of 1.24 μM. Anticonvulsant agent 9 inhibits the inactivation of Nav1.2 channels. Anticonvulsant agent 9 exhibits significant anticonvulsant activities .

HY-108584R

Flindokalner (Standard) BMS-204352 (Standard)	Potassium Channel Reference Standards	Neurological Disease
Flindokalner (Standard) is the analytical standard of Flindokalner. This product is intended for research and analytical applications. Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo .

HY-163855

KGP-25	Sodium Channel GABA Receptor	Neurological Disease
KGP-25 is an inhibitor of voltage-gated sodium channel 1.8 (Nav1.8), which can be used for analgesia by targeting Nav1.8 in the peripheral nervous system (PNS). KGP-25 can also target γ-aminobutyric acid subtype A receptor (GABA_A) in the central nervous system (CNS) for general anesthesia .

HY-114811

Leptophos oxon	Insecticide GABA Receptor Chloride Channel	Infection Neurological Disease
Leptophos oxon, a metabolite of leptophos, is a **GABA_A receptor chloride channel inhibitor with an IC₅₀** values of 89.6 μM. Leptophos oxon inhibits GABA-induced chloride influx, binds to GABA_A receptor-associated TBPS sites, and inhibits TBPS binding to voltage-dependent chloride channels. Leptophos oxon is a insecticide. Leptophos oxon can be used for the research of neurological disease .

HY-B1671R

(+)-Kavain (Standard)	Reference Standards GABA Receptor Sodium Channel Calcium Channel	Neurological Disease Metabolic Disease
(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

HY-182548

BTS 72664	GABA Receptor Sodium Channel iGluR	Cardiovascular Disease Neurological Disease
BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABA_A receptor (GABA_A *receptor*)-mediated chloride channel currents, while it exerts weak blocking effects on Na ⁺ channels (K_i = 350 μM) and NMDA receptors (NMDA receptor) (IC₅₀ = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine .

HY-N18341

Ginkgolide M	GABA Receptor Drug Derivative	Neurological Disease
Ginkgolide M (GM) is a ginkgolide that can be isolated from Ginkgo biloba. Ginkgolide M acts as an inhibitor of ligand-gated ion channels in the central nervous system and exerts inhibitory effects on the *GABAA* receptor. Ginkgolide M can be used for the research of neurodegenerative diseases such as Alzheimer's disease .

Cat. No.	Product Name

HY-L120

GABA Receptor Compound Library	209 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 209 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

GABA Receptor Compound Library

209 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 209 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

Cat. No.	Product Name	Type

HY-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate	Biochemical Assay Reagents
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, **GABAA receptor*, and the inward-rectifier potassium ion channel*.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0219

Bicuculline 35+ Cited Publications (+)-Bicuculline	Alkaloids Lamprocapnos spectabilis (L.) Fukuhara Plants Isoquinoline Alkaloids Papaveraceae Source Classification	GABA Receptor
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter *GABA_A* receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca ²⁺ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .

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-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate	Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification Cancer	nAChR GABA Receptor Potassium Channel Endogenous Metabolite
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, **GABAA receptor*, and the inward-rectifier potassium ion channel*.

HY-B1671

(+)-Kavain	Structural Classification Other Phenylpropanoids Piper methysticum G.Forst. Piperaceae Phenylpropanoids Plants Source Classification	GABA Receptor Sodium Channel Calcium Channel
(+)-Kavain, a main kavalactone that can be extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na ⁺ and Ca ²⁺ channels . (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

HY-N0219R

Bicuculline (Standard) (+)-Bicuculline (Standard)	Alkaloids Structural Classification Lamprocapnos spectabilis (L.) Fukuhara Plants Isoquinoline Alkaloids Papaveraceae Source Classification	Reference Standards GABA Receptor
Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .

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-B1671R

(+)-Kavain (Standard)	Structural Classification Other Phenylpropanoids Piper methysticum G.Forst. Piperaceae Phenylpropanoids Plants Source Classification	Reference Standards GABA Receptor Sodium Channel Calcium Channel
(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

HY-N18341

Ginkgolide M	Structural Classification Ginkgoaceae Terpenoids Sesquiterpenes Plants Ginkgo biloba Source Classification	GABA Receptor Drug Derivative
Ginkgolide M (GM) is a ginkgolide that can be isolated from Ginkgo biloba. Ginkgolide M acts as an inhibitor of ligand-gated ion channels in the central nervous system and exerts inhibitory effects on the *GABAA* receptor. Ginkgolide M can be used for the research of neurodegenerative diseases such as Alzheimer's disease .

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

Cat. No.	Compare	Product Name	Species	Source	Image

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

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
	GABRR1 Protein, Human (HEK293, StrepⅡ) is the recombinant human-derived GABRR1 protein, expressed by HEK293, with N-StrepⅡ tag.

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

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HY-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate		Cholesterol
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, **GABAA receptor*, and the inward-rectifier potassium ion channel*.

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GABAA receptor chloride channel

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

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Recombinant Proteins

Oligonucleotides

Natural
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