Search Result
Results for "
GABAA positive allosteric modulator
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-111052
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GABA Receptor
Cytochrome P450
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Neurological Disease
Inflammation/Immunology
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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.
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- HY-113320
-
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5β-Androsterone
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GABA Receptor
Endogenous Metabolite
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Neurological Disease
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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 .
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- HY-116152
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Ciprofol; HSK3486
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GABA Receptor
Sirtuin
Keap1-Nrf2
Apoptosis
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABAA 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 .
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- HY-107198
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GABA Receptor
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Neurological Disease
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(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface .
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- HY-103524
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(-)-Valerenic Acid
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GABA Receptor
5-HT Receptor
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Neurological Disease
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Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
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- HY-16579
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HOE 36-801 hydrochloride
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GABA Receptor
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Neurological Disease
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Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
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- HY-101165
-
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iGluR
GABA Receptor
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Neurological Disease
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Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
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- HY-16579A
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HOE 36-801
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GABA Receptor
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Neurological Disease
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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 .
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- HY-W677042
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5α-Androst-16-en-3α-ol
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GABA Receptor
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Neurological Disease
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α-Androstenol (5α-Androst-16-en-3α-ol) is a steroid pheromone that has been found in boar testes and male axillary sweat. α-Androstenol is also a positive allosteric modulator of GABAA receptors, which enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50 of 0.4 μM). α-Androstenol produces anxiolytic-like, antidepressant-like, and anticonvulsant effects in mice. α-Androstenol can be used for the research of seizures .
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- HY-120874
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PF-06372865; CVL-865
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GABA Receptor
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Neurological Disease
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Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). Darigabat is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis 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 .
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- HY-132806
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RG-7816; RO-7017773
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GABA Receptor
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Neurological Disease
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Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <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 .
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- HY-113346
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Tetrahydro-11-deoxycorticosterone
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GABA Receptor
Endogenous Metabolite
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Neurological Disease
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Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
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- HY-105272
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R 72063
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GABA Receptor
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Neurological Disease
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Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
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- HY-120837
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GABA Receptor
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Neurological Disease
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PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects .
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- HY-113346S
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- HY-N8852
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6-MeOF
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GABA Receptor
Taste Receptor
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Neurological Disease
Metabolic Disease
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6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABAA receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABAA receptors, and is relatively inactive on the α1β2 GABAA receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain .
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- HY-103520
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GABA Receptor
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Neurological Disease
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DS2 is a selective positive allosteric modulator of δ-GABAA 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 .
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- HY-W001692
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DOV 273547
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GABA Receptor
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Neurological Disease
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Ocinaplon (DOV 273547) is an orally active positive allosteric modulator of GABAA receptor, with an EC50 ranging from 3.07 μM (α1β2γ2 subtype) to 10.03 μM (α1β2γ3 subtype). Ocinaplon enhances GABA-stimulated chloride currents across multiple GABAA receptor subtypes, with varying potency between different subtypes. Ocinaplon exerts anxiolytic and anticonvulsant effects, and causes motor impairment at high doses. Ocinaplon can be used for research on generalized anxiety disorder .
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- HY-129408
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GABA Receptor
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Neurological Disease
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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 .
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- HY-159826
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- HY-121393
-
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GABA Receptor
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Neurological Disease
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Imidazenil is a partial positive allosteric modulator of GABAA receptors with anxiolytic, antipanic and anticonvulsant activities.
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- HY-113320S
-
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5β-Androsterone-d5
|
Isotope-Labeled Compounds
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
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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 .
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- HY-103524R
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(-)-Valerenic Acid (Standard)
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5-HT Receptor
GABA Receptor
Reference Standards
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Neurological Disease
|
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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 GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
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- HY-105115
-
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ZK 112119
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GABA Receptor
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Neurological Disease
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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 GABAA 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 .
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- HY-129431
-
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PNU-89843
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GABA Receptor
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Neurological Disease
|
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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 .
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- HY-103497
-
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PNU-89843 hydrochloride
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GABA Receptor
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Neurological Disease
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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 .
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- HY-147421
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- HY-170903
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GABA Receptor
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Neurological Disease
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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 .
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- HY-103535
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- HY-117979
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Alfadolone
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GABA Receptor
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Neurological Disease
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Alphadolone is a GABAA receptor positive allosteric modulator. Alphadolone has antinociceptive effects. Alphadolone causes general anaesthesia .
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- HY-103498
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GABA Receptor
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Neurological Disease
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Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM .
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- HY-175670
-
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GABA Receptor
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Neurological Disease
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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 .
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- HY-105272A
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R 72063 hydrochloride
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GABA Receptor
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Neurological Disease
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Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
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- HY-14758
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NG2-73
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GABA Receptor
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Neurological Disease
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Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.
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- HY-175251
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GABA Receptor
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Neurological Disease
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GABAA receptor modulator-9 is and positive allosteric modulator of a1β2y2 subtype GABAA that can cross the blood-brain barrier. GABAA receptor modulator-9 exhibits comparable activity on α1β2γ2 (EC50: 0.9 μM in oocytes, 0.2 μM in CHO cells) and on α1β2, α3β2γ2 and α1β3γ2 (EC50s of 1.3, 3.4 and 1.1 μM). GABAA receptor modulator-9 significantly suppresses seizure progression and reduces delayed mortality. GABAA receptor modulator-9 can be used for the study of status epilepticus (SE) .
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- HY-131941
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GABA Receptor
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Neurological Disease
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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 .
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- HY-105272R
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R 72063 (Standard)
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Reference Standards
GABA Receptor
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Neurological Disease
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Loreclezole (Standard) is the analytical standard of Loreclezole. This product is intended for research and analytical applications. Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
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- HY-113320S1
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5β-Androsterone-d2
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Isotope-Labeled Compounds
GABA Receptor
Endogenous Metabolite
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Neurological Disease
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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 .
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- HY-108204
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THRX 918661
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GABA Receptor
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Others
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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.
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- HY-169432
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GABA Receptor
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Neurological Disease
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TET-13 is a positive allosteric modulator of GABAA 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) .
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- HY-16579AS2
-
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GABA Receptor
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Neurological Disease
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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 .
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- HY-16579AR
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HOE 36-801 (Standard)
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Reference Standards
GABA Receptor
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Neurological Disease
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Etifoxine (Standard) is the analytical standard of Etifoxine. This product is intended for research and analytical applications. 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 .
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- HY-101165R
-
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Reference Standards
iGluR
GABA Receptor
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Neurological Disease
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Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
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- HY-173251S
-
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GABA Receptor
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Neurological Disease
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ENX-101 is an orally active (GABAA) 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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- HY-115857
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GABA Receptor
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Neurological Disease
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SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs .
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- HY-131997
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GABA Receptor
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Neurological Disease
Inflammation/Immunology
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2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response .
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- HY-111052R
-
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GABA Receptor
Cytochrome P450
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Neurological Disease
Inflammation/Immunology
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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.
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- HY-117106
-
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GABA Receptor
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Others
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PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
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- HY-W742312
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Ucedorm
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GABA Receptor
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Metabolic Disease
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Brallobarbitone is a positive allosteric modulator of GABAA receptor. Brallobarbitone can be used in the research of β-cell dysfunction .
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- HY-W644305
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3β-Androstenol
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GABA Receptor
Endogenous Metabolite
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Neurological Disease
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Androst-16-en-3-ol is a pheromone derived from boars that triggers mating responses in estrous sows. It also exists in human urine, plasma, saliva and sweat. As an endogenous neurosteroid, Androst-16-en-3-ol acts as a positive allosteric modulator of GABAA receptors (GABAA receptor) and exerts anxiolytic, antidepressant and anticonvulsant activities in mice.
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- HY-182511
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GABA Receptor
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Neurological Disease
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IUN-00433 (Compound 36) is a selective positive allosteric modulator of α4β1δ-type GABAA receptors, with an EC50 of 0.060 μM. IUN-00433 is applicable to research related to neurological disorders .
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- HY-16579R
-
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HOE 36-801 hydrochloride (Standard)
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GABA Receptor
Reference Standards
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Neurological Disease
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Etifoxine (hydrochloride) (Standard) is the analytical standard of Etifoxine (hydrochloride). This product is intended for research and analytical applications. Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
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- HY-P992360
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GABA Receptor
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Neurological Disease
Cancer
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GT-002 is a partial positive allosteric modulator targeting the α3 subtype of GABAA receptors, as well as a specific binder of tumor-associated TF-glycosylated LYPD3. GT-002 mildly enhances GABA-induced chloride currents by binding to the benzodiazepine site of GABAA receptors, thereby alleviating prefrontal hypofunction and improving cognitive, memory and social interaction abilities. GT-002 can be used in research related to schizophrenia spectrum disorders, various squamous cell carcinomas, colorectal cancer, non-small cell lung cancer, and aromatic L-amino acid decarboxylase deficiency .
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- HY-185007
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GABA Receptor
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Neurological Disease
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LI-633 is a selective and orally active GABAA receptor positive allosteric modulator (PAM) with a Ki 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 .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P992360
-
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GABA Receptor
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Neurological Disease
Cancer
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GT-002 is a partial positive allosteric modulator targeting the α3 subtype of GABAA receptors, as well as a specific binder of tumor-associated TF-glycosylated LYPD3. GT-002 mildly enhances GABA-induced chloride currents by binding to the benzodiazepine site of GABAA receptors, thereby alleviating prefrontal hypofunction and improving cognitive, memory and social interaction abilities. GT-002 can be used in research related to schizophrenia spectrum disorders, various squamous cell carcinomas, colorectal cancer, non-small cell lung cancer, and aromatic L-amino acid decarboxylase deficiency .
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Product Name |
Category |
Target |
Chemical Structure |
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Chemical Structure |
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