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GABA_A receptor modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Apoptosis (2) Bacterial (1) Chloride Channel (2) COX (1) Cytochrome P450 (1) Endogenous Metabolite (5) GABA Receptor (62) Isotope-Labeled Compounds (2) Keap1-Nrf2 (1) Potassium Channel (2) Sirtuin (1)
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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N8852

6-Methoxyflavanone 6-MeOF	GABA Receptor	Neurological Disease
6-Methoxyflavanone (6-MeOF) is an orally active flavonoid compound. 6-Methoxyflavanone has anxiolytic properties. 6-Methoxyflavanone targets unique sites on GABA-A receptors, different from traditional benzodiazepines. 6-Methoxyflavanone can be used to study anxiety disorders. 6-Methoxyflavanone readily crosses the blood brain barrier (BBB) .

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-121393

Imidazenil	GABA Receptor	Neurological Disease
Imidazenil is a partial positive allosteric modulator of *GABA_A* receptors with anxiolytic, antipanic and anticonvulsant activities.

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-P5860

MmTx1 toxin Micrurotoxin 1	GABA Receptor	Neurological Disease
MmTx1 toxin (Micrurotoxin 1) is an allosteric *GABA_A* receptor modulator that increases GABA_A receptor susceptibility to agonist .

HY-146100

GABAA receptor agent 8	GABA Receptor	Neurological Disease
GABAA receptor agent 8 (compoud 5e) is a potent **GABAA receptor** positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy .

HY-146099

GABAA receptor agent 7	GABA Receptor	Neurological Disease
GABAA receptor agent 7 (compoud 5c) is a potent **GABAA receptor** positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy .

HY-109572

GABAA receptor modular-4	GABA Receptor	Neurological Disease
GABAA receptor module-4 (9eey) is a **GABAA receptor** modulator that can be used in the study of central nervous system diseases .

HY-147421

Xilmenolone	GABA Receptor	Neurological Disease
Xilmenolone is a **GABAA receptor** positive allosteric modulator .

HY-159826

Brexanolone caprilcerbate	GABA Receptor	Neurological Disease
Brexanolone caprilcerbate is a potent *GABAA* receptor positive allosteric modulator .

HY-103501

SB-205384	GABA Receptor	Neurological Disease
SB-205384 is a *GABAA* receptor modulator. The primary effect of SB-205384 on GABAA-activated currents is a prolonged response decay half-life upon removal of the agonist .

HY-105272

Loreclezole R 72063	GABA Receptor	Neurological Disease
Loreclezole, an antiepileptic compound, is a selective **GABA_A receptor** modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .

HY-105272A

Loreclezole hydrochloride R 72063 hydrochloride	GABA Receptor	Neurological Disease
Loreclezole hydrochloride, an antiepileptic compound, is a selective **GABA_A receptor** modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .

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-103535

GBLD345	GABA Receptor	Neurological Disease
GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent **GABAA receptor** positive allosteric modulator (PAM) .

HY-113346

Tetrahydrodeoxycorticosterone Tetrahydro-11-deoxycorticosterone	GABA Receptor Endogenous Metabolite	Neurological Disease
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of **GABA_A receptor**. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-103498

Org20599	GABA Receptor	Neurological Disease
Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of **GABA_A receptor with an EC₅₀** of 1.1 μM .

HY-P5857

MmTx2 toxin Micrurotoxin 2	GABA Receptor	Neurological Disease
MmTx2 toxin is a *GABA_A* receptor modulator that enhances *GABA_A* receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .

HY-161784

GABAA receptor modular-3	GABA Receptor	Neurological Disease
GABAA receptor modular-3 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA *receptor), with EC₅₀* of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modular-3 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modular-3 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression .

HY-19872

AZD-6280	GABA Receptor	Neurological Disease
AZD-6280 is a selective **GABAA(α2/3) receptor** modulator, used for treatment of generalized anxiety disorder.

HY-W001692

Ocinaplon DOV 273547	GABA Receptor	Neurological Disease
Ocinaplon (DOV 273547) is a partial *GABAA* receptor positive allosteric modulator with relatively high efficacy at the α1 subunit .

HY-112426

LAU159	GABA Receptor	Neurological Disease
LAU159 is a functionally selective positive modulator of α1β3 *GABA(A)* receptor with an EC₅₀ of 2.2 μM .

HY-111298

TG 41	GABA Receptor	Neurological Disease
TG 41 is positive modulator of **GABAA receptor**. TG 41 enhances the binding both of GABA and of Flunitrazepam to rat cerebral cortical membranes .

HY-103497

U-89843A hydrochloride	GABA Receptor	Neurological Disease
U-89843A is an allosteric modulator of **GABAA receptor**. U-89843A enhances GABA-induced Cl ^- currents .

HY-120276

Golexanolone GR3027	GABA Receptor	Neurological Disease
Golexanolone is a **GABA_A receptor** modulating steroid antagonist. Golexanolone reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in hyperammonemic rats .

HY-132806

Alogabat RG-7816; RO-7017773	GABA Receptor	Neurological Disease
Alogabat (example 8) is a **GABA_A α5 receptor** positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1) .

HY-103524

Valerenic acid 1 Publications Verification (-)-Valerenic Acid	GABA Receptor 5-HT Receptor	Neurological Disease
Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of *GABA_A* receptors. Valerenic acid is also a partial agonist of the 5-HT_5a receptor. Valerenic acid mediates anxiolytic activity via GABA_A receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .

HY-16716

Basmisanil 1 Publications Verification RG1662; RO5186582	GABA Receptor	Neurological Disease
Basmisanil (RG1662) is a highly selective orally active *α subunit-containing GABAA* receptors (GABAAα5)** negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a K_i value of 5 nM and IC₅₀ value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .

HY-19371

Lorediplon	GABA Receptor	Neurological Disease
Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.

HY-14758

Adipiplon NG2-73	GABA Receptor	Neurological Disease
Adipiplon (NG2-73) is a selective **GABA_A receptor** positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.

HY-129408

SGE-516	GABA Receptor	Neurological Disease
SGE-516 is a neuroactive steroid that is a potent positive allosteric modulator of synaptic and extra-synaptic *GABAA* receptors. SGE-516 has anticonvulsant activity .

HY-153584

MRK-898	GABA Receptor	Neurological Disease
MRK-898 is an orally active **GABA(A) receptor** modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with K_i values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s) .

HY-N2096

Kavain	GABA Receptor	Neurological Disease
Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .

HY-103524R

Valerenic acid (Standard) (-)-Valerenic Acid (Standard)	5-HT Receptor GABA Receptor	Neurological Disease
Valerenic acid (Standard) is the analytical standard of Valerenic acid. This product is intended for research and analytical applications. Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of *GABA_A* receptors. Valerenic acid is also a partial agonist of the 5-HT_5a receptor. Valerenic acid mediates anxiolytic activity via GABA_A receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .

HY-131941

SJM-3	GABA Receptor	Neurological Disease
SJM-3 is a positive allosteric modulator of different isoforms of the *GABAA* receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface .

HY-113346S

Tetrahydrodeoxycorticosterone-d3 1 Publications Verification Tetrahydro-11-deoxycorticosterone-d₃	Isotope-Labeled Compounds GABA Receptor Endogenous Metabolite	Neurological Disease
Tetrahydrodeoxycorticosterone-d₃ is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].

HY-113320

Etiocholanolone 5β-Androsterone	GABA Receptor Endogenous Metabolite	Neurological Disease
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the *GABA_A*?receptor than its?enantiomer form .

HY-108204

AZD 3043 THRX 918661	Others	Others
AZD 3043 (THRX 918661) is a positive allosteric modulator of GABA(A) receptors with sedative and hypnotic activity. AZD 3043 can enhance GABA(A) receptor-mediated chloride currents in vitro and produce hypnotic and electroencephalographic inhibitory effects in vivo. Due to its esterase-dependent metabolic pathway, it has a short duration of action and can be quickly cleared even after long-term infusion, which may have clinical application potential.

HY-123489

3α,21-Dihydroxy-5α-pregnan-20-one THDOC	GABA Receptor	Neurological Disease
3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of *GABA_A* receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABA_A receptors in vitro.

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-N2096R

Kavain (Standard)	GABA Receptor	Neurological Disease
Kavain (Standard) is the analytical standard of Kavain. This product is intended for research and analytical applications. Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .

HY-16579

Etifoxine hydrochloride 1 Publications Verification HOE 36-801 hydrochloride	GABA Receptor	Neurological Disease
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing **GABA_A receptors**. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .

HY-16579A

Etifoxine 1 Publications Verification HOE 36-801	GABA Receptor	Neurological Disease
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing **GABA_A receptors**. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .

HY-113320S

Etiocholanolone-d5	GABA Receptor Endogenous Metabolite	Neurological Disease
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].

HY-100991

FG 7142 ZK 39106; LSU-65	GABA Receptor	Neurological Disease
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing **GABAA receptor (K_i*=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates* GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC₅₀= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex .

HY-113320S1

Etiocholanolone-d2 5β-Androsterone-d₂	Isotope-Labeled Compounds GABA Receptor Endogenous Metabolite	Neurological Disease
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].

HY-169432

TET-13	GABA Receptor	Neurological Disease
TET-13 is a positive allosteric modulator of **GABA_A receptor with an EC₅₀ of 5.65 μM, lower than that of Etomidate (EC₅₀: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED₅₀**: 0.48 mg/kg and 0.69 mg/kg, respectively) .

HY-105115

Abecarnil ZK 112119	GABA Receptor	Neurological Disease
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of **GABA_A receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC₅₀** of 0.82 nM. Abecarnil can be used for epilepsy research .

HY-N6084

Humulone α-Lupulic acid	COX GABA Receptor Apoptosis	Cardiovascular Disease
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of **GABA_A receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis**-inducing properties .

HY-B1606

Chlorothymol Chlorthymol; 6-Chlorothymol	GABA Receptor Bacterial	Neurological Disease Inflammation/Immunology
Chlorothymol (Chlorthymol) is a potent *GABA_A* receptor subunit LGC-37 positive modulator. Chlorothymol is an effective anticonvulsant. Chlorothymol is protective in several mouse seizure assays, including the 6-Hz 44-mA model of pharmacoresistant seizures. Chlorothymol possess GABAergic, membrane-modifying, antioxidant and topical antiseptic properties .

Cat. No.	Product Name	Target	Research Area

HY-P5860

MmTx1 toxin Micrurotoxin 1	GABA Receptor	Neurological Disease
MmTx1 toxin (Micrurotoxin 1) is an allosteric *GABA_A* receptor modulator that increases GABA_A receptor susceptibility to agonist .

HY-P5857

MmTx2 toxin Micrurotoxin 2	GABA Receptor	Neurological Disease
MmTx2 toxin is a *GABA_A* receptor modulator that enhances *GABA_A* receptor sensitivity to agonists. MmTx2 toxin can be obtained from venom of coral snake. MmTx2 toxin can be used in the study of neurological diseases such as epilepsy, schizophrenia and chronic pain .

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-113346

Tetrahydrodeoxycorticosterone Tetrahydro-11-deoxycorticosterone	Structural Classification Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Steroids	GABA Receptor Endogenous Metabolite
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of **GABA_A receptor**. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .

HY-N2096

Kavain	Structural Classification Natural Products Source classification Piper methysticum G.Forst. Piperaceae Plants	GABA Receptor
Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .

HY-113320

Etiocholanolone 5β-Androsterone	Structural Classification Microorganisms Source classification Endogenous metabolite Steroids	GABA Receptor Endogenous Metabolite
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the *GABA_A*?receptor than its?enantiomer form .

HY-N6084

Humulone α-Lupulic acid	Cardiovascular Disease Classification of Application Fields Ketones, Aldehydes, Acids Humulus lupulus L. Source classification Plants Moraceae Disease Research Fields	COX GABA Receptor Apoptosis
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of **GABA_A receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis**-inducing properties .

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 .

HY-N2096R

Kavain (Standard)	Structural Classification Natural Products Source classification Piper methysticum G.Forst. Piperaceae Plants	GABA Receptor
Kavain (Standard) is the analytical standard of Kavain. This product is intended for research and analytical applications. Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor .

Cat. No.	Product Name	Chemical Structure

HY-113346S

Tetrahydrodeoxycorticosterone-d3 1 Publications Verification
Tetrahydrodeoxycorticosterone-d₃ is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].

HY-113320S

Etiocholanolone-d5
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].

HY-113320S1

Etiocholanolone-d2
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].

HY-16579AS2

Etifoxine-d5
Etifoxine-d₅ is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].

HY-123489S

3α,21-Dihydroxy-5α-pregnan-20-one-d3
3α,21-Dihydroxy-5α-pregnan-20-one-d₃ is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.

Cat. No.	Product Name		Classification

HY-120276

Golexanolone GR3027		Alkynes
Golexanolone is a **GABA_A receptor** modulating steroid antagonist. Golexanolone reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in hyperammonemic rats .

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GABA_A receptor modulator

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