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GABAA

" in MedChemExpress (MCE) Product Catalog:

289

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28

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-175670

    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 .
    GABAA receptor modulator-10
  • HY-109572

    GABA Receptor Neurological Disease
    GABAA receptor modulator-1 (9eey) is a GABAA receptor modulator that can be used in the study of central nervous system diseases .
    GABAA receptor modulator-1
  • HY-135482

    GABA Receptor Neurological Disease
    GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) .
    GABAA receptor agent 2 TFA
  • HY-173616

    GABA Receptor Neurological Disease
    GABAA receptor modulator-8 (10c) is a blood-brain barrier penetrated, selective and positive modulator of GABAA receptor, with excellent antiepileptic activity .
    GABAA receptor modulator-8
  • HY-145258

    GABA Receptor Neurological Disease
    GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an Ki of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability .
    GABAA receptor agent 6
  • HY-170902

    GABA Receptor Neurological Disease
    GABAA receptor modulator-4 (Compound 4) is the negative allosteric modulator for GABAA receptor. GABAA receptor modulator-4 inhibits α1β3γ2 GABAA receptor-mediated peak and steady currents with IC50 of 10 μM and 10 μM .
    GABAA receptor modulator-4
  • HY-172588

    GABA Receptor Neurological Disease
    GABAA receptor modulator-7 (compound 1m), a spiro-Barbiturate, is a GABAA receptor modulator. GABAA receptor modulator-7 reverses the action of anesthetics without affecting GABA-induced desensitization and can be used for study of antiepileptics and anxiolytics .
    GABAA receptor modulator-7
  • HY-147736

    GABA Receptor Neurological Disease
    GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .
    GABAA receptor agonist 2
  • HY-147735

    GABA Receptor Neurological Disease
    GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .
    GABAA receptor agonist 1
  • HY-170498

    GABA Receptor Neurological Disease
    GABA-A Receptor Ligand-1 (Compound 4) is a ligand for GABA-A receptor with a pKi of 7.27. GABA-A Receptor Ligand-1 reduces mitochondrial dysfunction, promotes neurite outgrowth and neuronal regeneration. GABA-A Receptor Ligand-1 exhibits neuroprotective efficacy in rats ischemic stroke models .
    GABA-A Receptor Ligand-1
  • HY-146099

    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 .
    GABAA receptor agent 7
  • HY-146100

    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 .
    GABAA receptor agent 8
  • HY-133486

    GABA Receptor Neurological Disease
    GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity .
    GABAA receptor agent 1
  • HY-161784

    GABA Receptor Neurological Disease
    GABAA receptor modulator-5 (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 modulator-5 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modulator-5 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 .
    GABAA receptor modulator-5
  • HY-175251

    GABA Receptor Neurological Disease
    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) .
    GABAA receptor modulator-9
  • HY-145256

    GABA Receptor Neurological Disease
    GABAA receptor agent 4 (compound 1e) is a potent γ-GABAAR antagonist with an Ki of 0.18 µM. GABAA receptor agent 4 efficiently rescues inhibition of T cell proliferation. GABAA receptor agent 4 has the immunomodulatory potential .
    GABAA receptor agent 4
  • HY-147657

    GABA Receptor Neurological Disease
    GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .
    GABAA receptor modulator-2
  • 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-103513

    GABA Receptor Others
    GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
    GABAA receptor agent 2
  • HY-145257

    GABA Receptor Neurological Disease
    GABAA receptor agent 5 (compound 018) is a potent γ-GABAAR antagonist with an Ki of 0.020 µM. GABAA receptor agent 5 shows γ-GABAAR antagonist activity with low cellular membrane permeability .
    GABAA receptor agent 5
  • HY-170771

    GABA Receptor Neurological Disease
    α5-GABAA receptor modulator 1 (Compound A-4) is a silencing allosteric modulator (SAM) specifically targeting the a5 subunit of the GABAA receptor, suitable for research into central nervous system (CNS) disorders .
    α5-GABAA receptor modulator 1
  • HY-103501

    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 .
    SB-205384
  • HY-116813

    GABA Receptor Neurological Disease
    ZK 93423 is a potent benzodiazepine GABAA receptor agonist with a certain cooling effect on rodents .
    ZK 93423
  • HY-124534

    GABA Receptor Neurological Disease
    (1S,3R)-3-Aminocyclopentane carboxylic acid has GABAA receptor activity .
    (1S,3R)-3-Aminocyclopentane carboxylic acid
  • HY-147421

    GABA Receptor Neurological Disease
    Xilmenolone is a GABAA receptor positive allosteric modulator .
    Xilmenolone
  • HY-168986

    GABA Receptor Neurological Disease
    Moxetomidate is a GABAA receptor agonist with hypnotic effect .
    Moxetomidate
  • 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 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 .
    Picrotoxinin
  • HY-116622

    L-822179

    GABA Receptor Neurological Disease
    α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential .
    α5IA
  • HY-B1494R

    Reference Standards 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 .
    Picrotoxinin (Standard)
  • HY-N10884

    Others Others
    Withasomniferolide A is a withanolide, isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .
    Withasomniferolide A
  • 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-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-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-103524R

    (-)-Valerenic Acid (Standard)

    5-HT Receptor GABA Receptor Reference Standards 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-103535

    GABA Receptor Neurological Disease
    GBLD345, a nonbenzodiazepine anxiolytic agent, is a non- selective, potent GABAA receptor positive allosteric modulator (PAM) .
    GBLD345
  • HY-116457

    Sombrevin; Fabantol

    GABA Receptor Cardiovascular Disease Neurological Disease
    Propanidid (Sombrevin; Fabantol) is a γ-aminobutyric acid type A (GABAA) receptor agonist and a short-acting non-barbiturate general agent that can suppress or relieve pain. Propanidid can decrease the arterial pressure .
    Propanidid
  • HY-124030

    Drug Metabolite Neurological Disease
    3-Hydroxyphenazepam is an active metabolite of Cinazepam. Cinazepam is a GABAA receptor agonist. 3-Hydroxyphenazepam can inhibit synaptosomal transporter-mediated [ 3H]GABA uptake .
    3-Hydroxyphenazepam
  • HY-115854

    GABA Receptor Neurological Disease
    Ro 15-1310 is an imidazobenzodiazepine that exhibits high affinity and selectivity for alpha 5-containing GABAA receptors. Ro 15-1310 is promising for research of convulsions .
    Ro 15-1310
  • HY-124463

    5α,3β-THDOC

    GABA Receptor iGluR Neurological Disease
    Epiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer .
    Epiallopregnanolone
  • 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 Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
    Basmisanil
  • HY-N10887

    GABA Receptor Neurological Disease
    Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera .
    Withasomniferolide B
  • HY-138014

    GABA Receptor Neurological Disease
    Cinazepam is a partial GABAA receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders .
    Cinazepam
  • HY-168758

    GABA Receptor Neurological Disease
    Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons .
    Delta3,5-cholestadien-7-one
  • HY-A0134
    Isoflurane
    5+ Cited Publications

    GABA Receptor Neurological Disease
    Isoflurane is a volatile general anaesthetic used for induction and maintenance of general anesthesia. Isoflurane binds to and enhances GABAA receptor. Isoflurane inhibits electron transfer in respiratory complex I .
    Isoflurane
  • 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-N8852

    6-MeOF

    GABA Receptor Taste Receptor Neurological Disease Metabolic Disease
    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 .
    6-Methoxyflavanone
  • HY-100991

    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 (Ki=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 .
    FG 7142
  • HY-U00199A

    (S)-N-Desmethyl zopiclone; SEP-174559

    GABA Receptor nAChR iGluR Neurological Disease
    (S)-Norzopiclone ((S)-N-Desmethyl zopiclone; SEP-174559) is a metabolite of Zopiclone with anxiolytic and anticonvulsant effects. (S)-Norzopiclone has benzodiazepine-like actions at γ2-bearing subtypes of the GABAA receptor and inhibits nACh and NMDA receptors .
    (S)-Norzopiclone
  • HY-B1606

    Chlorthymol; 6-Chlorothymol

    GABA Receptor Bacterial Neurological Disease Inflammation/Immunology
    Chlorothymol (Chlorthymol) is a potent GABAA 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 .
    Chlorothymol
  • HY-100991R

    ZK 39106 (Standard); LSU-65 (Standard)

    Reference Standards GABA Receptor Neurological Disease
    FG 7142 (Standard) is the analytical standard of FG 7142. This product is intended for research and analytical applications. FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=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 .
    FG 7142 (Standard)

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