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Results for "

GABAA PAM

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Cytochrome P450 (2) Endogenous Metabolite (5) GABA Receptor (18) Isotope-Labeled Compounds (3)
By Research Areas:	Inflammation/Immunology (2) Neurological Disease (18)

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-120874

Darigabat PF-06372865; CVL-865	GABA Receptor	Neurological Disease
Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective *GABA_A* positive allosteric modulator (PAM). Darigabat 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. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy .

HY-132806

Alogabat RG-7816; RO-7017773	GABA Receptor	Neurological Disease
Alogabat is a positive allosteric modulator (PAM) and agonist (K_i <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction .

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-11048

NS11394 3 Publications Verification	GABA Receptor	Neurological Disease
NS11394 is an orally active and unique subtype-selective *GABA_A* positive allosteric receptor (PAM), with a K_i of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABA_A-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .

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 .

HY-113320S

Etiocholanolone-d5 5β-Androsterone-d₅	Isotope-Labeled Compounds 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 . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .

HY-103535

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

HY-147421

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

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-175670

GABAA receptor modulator-10	GABA Receptor	Neurological Disease
GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances *α1β2γ2 GABAA* receptor** function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy .

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 . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .

HY-111052R

AZD7325 (Standard)	GABA Receptor Cytochrome P450	Neurological Disease Inflammation/Immunology
AZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=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-129431

U-89843A PNU-89843	GABA Receptor	Neurological Disease
U-89843A (PNU-89843) is a GABAA receptors positive allosteric modulator (PAM). U-89843A enhances GABA-induced Cl ^- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A shows antioxidant and sedative effects .

HY-103497

U-89843A hydrochloride PNU-89843 hydrochloride	GABA Receptor	Neurological Disease
U-89843A (PNU-89843) hydrochloride is a GABAA receptors positive allosteric modulator (PAM). U-89843A hydrochloride enhances GABA-induced Cl ^- currents in the α1β2γ2, α3β2γ2 and α6β2γ2 subtypes. U-89843A hydrochloride shows antioxidant and sedative effects .

HY-173251S

ENX-101	GABA Receptor	Neurological Disease
ENX-101 is an orally active (GABA_A) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC₅₀ = 0.76 nM), α2β3γ2L (EC₅₀ = 0.61 nM), α3 (EC₅₀ = 1.97 nM), α5 (EC₅₀ = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models .

HY-185007

LI-633	GABA Receptor	Neurological Disease
LI-633 is a selective and orally active GABAA receptor positive allosteric modulator (PAM) with a K_i of 21 nM. LI-633 produces robust potentiation of GABA-induced inward current, with EC₅₀ values ranging from 8 nM (α5β2γ2) to 128 nM (α3β2γ2). LI-633 potentiates muscimol-induced GABAergic currents in rat dorsal root ganglion (DRG) neurons with an EC₅₀ of 70.4 nM. LI-633 can be used for the study of visceral pain .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113320

Etiocholanolone 5β-Androsterone	Microorganisms Endogenous metabolite Steroids Source Classification	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-113346

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

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 .

HY-113320S

Etiocholanolone-d5
Etiocholanolone-d₅ is the deuterium labeled Etiocholanolone. 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 GABAA?receptor than its?enantiomer form .

HY-113320S1

Etiocholanolone-d2
Etiocholanolone-d₂ is the deuterium labeled Etiocholanolone. 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 GABAA?receptor than its?enantiomer form .

HY-173251S

ENX-101
ENX-101 is an orally active (GABA_A) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC₅₀ = 0.76 nM), α2β3γ2L (EC₅₀ = 0.61 nM), α3 (EC₅₀ = 1.97 nM), α5 (EC₅₀ = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models .

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GABAA PAM

Inhibitors & Agonists

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Isotope-Labeled Compounds

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