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GABAA positive allosteric modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Apoptosis (1) Cytochrome P450 (1) Endogenous Metabolite (5) GABA Receptor (28) Isotope-Labeled Compounds (1) Keap1-Nrf2 (1) Sirtuin (1)
By Research Areas:	Cardiovascular Disease (1) Inflammation/Immunology (3) Neurological Disease (25)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-120837

PZ-II-029	GABA Receptor	Neurological Disease
PZ-II-029 is a *GABAA* positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects .

HY-147421

Xilmenolone

GABA Receptor Neurological Disease

Xilmenolone is a GABAA receptor positive allosteric modulator .
HY-103535

GBLD345

GABA Receptor Neurological Disease

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

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

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

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-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-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-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-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-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	GABA Receptor Endogenous Metabolite
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-107198

(2S)-6-Prenylnaringenin 1 Publications Verification	GABA Receptor	Neurological Disease
(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a *GABA_A* positive allosteric modulator at α+β- binding interface .

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-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-15831

L-838417-d9	Isotope-Labeled Compounds GABA Receptor	Neurological Disease
L-838417-d₉ is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

HY-113320S1

Etiocholanolone-d2 5β-Androsterone-d₂	GABA Receptor Endogenous Metabolite
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	GABA Receptor	Neurological Disease
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-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-123801

MIDD0301 GL-II-93	GABA Receptor	Others
MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABA_A receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases .

HY-103520

DS2	GABA Receptor	Neurological Disease
DS2 is a selective positive allosteric modulator of δ-GABA_A receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research .

HY-116152

Cipepofol Ciprofol; HSK3486	GABA Receptor Sirtuin Keap1-Nrf2 Apoptosis	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABA_A receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis .

HY-131997

2'MeO6MF	GABA Receptor	Neurological Disease Inflammation/Immunology
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABA_A receptors. 2'MeO6MF also can directly activate α2β2/3 and *α2β2/3γ2L GABA_A* receptors**. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response .

HY-111052

AZD7325	GABA Receptor Cytochrome P450	Neurological Disease Inflammation/Immunology
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (K_i=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.

HY-120874

PF-06372865	GABA Receptor	Neurological Disease
PF-06372865 is an orally active, α2/α3/α5 subtype-selective *GABA_A* positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABA_A receptors containing α1/α2/α3/α5 subunits (K_is of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .

Cat. No.	Product Name	Category	Target	Chemical Structure

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-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-107198

(2S)-6-Prenylnaringenin 1 Publications Verification	Structural Classification Flavonoids Humulus lupulus L. Flavonones Source classification Phenols Polyphenols Plants Moraceae	GABA Receptor
(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a *GABA_A* positive allosteric modulator at α+β- binding interface .

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-15831

L-838417-d9
L-838417-d₉ is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].

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].

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GABAA positive allosteric modulator

Inhibitors & Agonists

NaturalProducts

Isotope-Labeled Compounds

Natural
Products