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GABA-A receptor benzodiazepine site

" in MedChemExpress (MCE) Product Catalog:

17

Inhibitors & Agonists

1

Peptides

1

Inhibitory Antibodies

3

Natural
Products

1

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N7110
    6-Hydroxyflavone
    2 Publications Verification

    		 Akt ERK JNK GABA Receptor Neurological Disease Metabolic Disease Inflammation/Immunology
    6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .
    6-Hydroxyflavone
  • HY-124467
    Difludiazepam

    Ro 07-4065

    		 GABA Receptor Neurological Disease
    Difludiazepam (Ro 07-4065), a benzodiazepine derivative, is a GABAA receptor ligand with an IC50 of 4.1 nM. Difludiazepam binds to an allosteric site on the GABAA receptor to potentiate the receptor's response to GABA, reducing neuron excitability. Difludiazepam contains halogenated groups at the ortho position of its phenyl ring .
    Difludiazepam
  • HY-P2602
    α-Casozepine

    		GABA Receptor Neurological Disease
    α-Casozepine is an orally effective anxiolytic that binds to the benzodiazepine site of the GABAA receptor in bovine samples with an IC50 of 88 μM. α-Casozepine exerts anxiolytic and anti-stress effects on cats exposed to unfamiliar environments and dogs undergoing road transport . α-Casozepine exhibits significant anxiolytic activity in rats. α-Casozepine can be used in studies related to fear, anxiety and stress .
    α-Casozepine
  • HY-105056
    Bretazenil

    Ro 16-6028

    		 GABA Receptor Neurological Disease
    Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
    Bretazenil
  • HY-14840
    Phenylpiracetam

    Carphedon

    		 nAChR Dopamine Transporter GABA Receptor iGluR Neurological Disease
    Phenylpiracetam (Carphedon) is a positive allosteric modulator of nicotinic acetylcholine receptors (nAChR) with an IC50 of 5.86 μM. Phenylpiracetam is applicable to studies on scopolamine (Scopolamine) (HY-N0296)-induced amnesia, depression and immune stress .
    Phenylpiracetam
  • HY-N6648
    Cirsimaritin

    		GABA Receptor Neurological Disease
    Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin
  • HY-123249
    HZ166

    		GABA Receptor Neurological Disease
    HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HZ166
  • HY-103512
    TP003

    		GABA Receptor Neurological Disease
    TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors .
    TP003
  • HY-19308
    RWJ-51204

    		GABA Receptor Neurological Disease
    RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.
    RWJ-51204
  • HY-114706
    Suritozole

    MDL-26479

    		 GABA Receptor Neurological Disease
    Suritozole (MGL-26479) is a cognitive enhancer that acts as a partial inverse agonist of benzodiazepine receptor sites on GABAA ion channel complexes. Suritozole can be used in the study of neurodegenerative diseases .
    Suritozole
  • 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 .
    SJM-3
  • HY-117560
    PWZ-029

    		GABA Receptor Neurological Disease
    PWZ-029 is a selective inverse agonist for 5 GABAA receptors. PWZ-029 is a benzodiazepine site ligand. PWZ-029 shows a weak but significant partial agonistic effect at 1- and 3-containing receptors. PWZ-029 significantly increases retention session latency in mouse fibroblast cells. PWZ-029 can improve object recognition in normal and scopolamine-treated rat model .
    PWZ-029
  • HY-115857
    SH-053-S-CH3-2'F

    		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-169651
    GABA-IN-4

    		GABA Receptor Neurological Disease
    GABA-IN-4 (Compound 17) is a N-(indol-3-ylglyoxylyl)benzylamine derivative. GABA-IN-4 exhibits high affinity for the benzodiazepine receptor (BzR) (binding site in GABAA receptor complex) with Ki value of 67 nM. Benzodiazepines are widely used as antianxiety, sedative-hypnotic and anticonvulsant agents .
    GABA-IN-4
  • HY-N6648R
    Cirsimaritin (Standard)

    		GABA Receptor Reference Standards Neurological Disease
    Cirsimaritin (Standard) is the analytical standard of Cirsimaritin (HY-N6648). This product is intended for research and analytical applications. Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin (Standard)
  • HY-105056R
    Bretazenil (Standard)

    Ro 16-6028 (Standard)

    		 Reference Standards GABA Receptor Neurological Disease
    Bretazenil (Standard) is the analytical standard of Bretazenil (HY-105056). This product is intended for research and analytical applications. Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
    Bretazenil (Standard)
  • HY-P992360
    GT-002

    		GABA Receptor Neurological Disease Cancer
    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 .
    GT-002

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