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GABAA positive allosteric modulator

" in MedChemExpress (MCE) Product Catalog:

38

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3

Natural
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5

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-120837

    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 .
    PZ-II-029
  • HY-121393

    GABA Receptor Neurological Disease
    Imidazenil is a partial positive allosteric modulator of GABAA receptors with anxiolytic, antipanic and anticonvulsant activities.
    Imidazenil
  • HY-113346

    Tetrahydro-11-deoxycorticosterone

    GABA Receptor Endogenous Metabolite Neurological Disease
    Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
    Tetrahydrodeoxycorticosterone
  • HY-W001692

    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 .
    Ocinaplon
  • HY-147421

    GABA Receptor Neurological Disease
    Xilmenolone is a GABAA receptor positive allosteric modulator .
    Xilmenolone
  • HY-159826

    GABA Receptor Neurological Disease
    Brexanolone caprilcerbate is a potent GABAA receptor positive allosteric modulator .
    Brexanolone caprilcerbate
  • HY-103535

    GABA Receptor Neurological Disease
    GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM) .
    GBLD345
  • HY-170903

    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 .
    GABAA receptor modulator-3
  • HY-117979

    Alfadolone

    GABA Receptor Neurological Disease
    Alphadolone is a GABAA receptor positive allosteric modulator. Alphadolone has antinociceptive effects. Alphadolone causes general anaesthesia .
    Alphadolone
  • HY-103498

    GABA Receptor Neurological Disease
    Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM .
    Org20599
  • HY-132806

    RG-7816; RO-7017773

    GABA Receptor Neurological Disease
    Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1) .
    Alogabat
  • HY-105272A

    R 72063 hydrochloride

    GABA Receptor Neurological Disease
    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 .
    Loreclezole hydrochloride
  • HY-105272

    R 72063

    GABA Receptor Neurological Disease
    Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
    Loreclezole
  • HY-129408

    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 .
    SGE-516
  • HY-14758

    NG2-73

    GABA Receptor Neurological Disease
    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.
    Adipiplon
  • HY-131941

    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 .
    SJM-3
  • 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].
    Tetrahydrodeoxycorticosterone-d3
  • HY-113320

    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 GABAA?receptor than its?enantiomer form .
    Etiocholanolone
  • 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 GABAA positive allosteric modulator at α+β- binding interface .
    (2S)-6-Prenylnaringenin
  • 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 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 .
    Valerenic acid
  • HY-113320S

    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].
    Etiocholanolone-d5
  • HY-16579
    Etifoxine hydrochloride
    2 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 GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
    Etifoxine hydrochloride
  • HY-16579A
    Etifoxine
    2 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 GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
    Etifoxine
  • HY-15831

    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].
    L-838417-d9
  • HY-113320S1

    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].
    Etiocholanolone-d2
  • HY-108204

    THRX 918661

    GABA Receptor 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.
    AZD 3043
  • HY-103524R

    (-)-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 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 .
    Valerenic acid (Standard)
  • HY-169432

    GABA Receptor Neurological Disease
    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) .
    TET-13
  • HY-16579AS2

    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].
    Etifoxine-d5
  • HY-16579AR

    GABA Receptor Neurological Disease
    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 .
    Etifoxine (Standard)
  • HY-105115

    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 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 .
    Abecarnil
  • HY-103520

    GABA Receptor Neurological Disease
    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 .
    DS2
  • HY-115857

    GABA Receptor Neurological Disease
    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 .
    SH-053-S-CH3-2'F
  • HY-116152

    Ciprofol; HSK3486

    GABA Receptor Sirtuin Keap1-Nrf2 Apoptosis Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    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 .
    Cipepofol
  • HY-131997

    GABA Receptor Neurological Disease Inflammation/Immunology
    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 .
    2'MeO6MF
  • HY-111052

    GABA Receptor Cytochrome P450 Neurological Disease Inflammation/Immunology
    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.
    AZD7325
  • HY-120874

    GABA Receptor Neurological Disease
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 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. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
    PF-06372865
  • HY-117106

    GABA Receptor Others
    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 .
    PNU-107484A

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