2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  3. GABA Receptor 5-HT Receptor Reactive Oxygen Species (ROS) TNF Receptor Interleukin Related COX NF-κB IKK NO Synthase
  4. GABAAR/5-HT2AR modulator-1

GABAAR/5-HT2AR modulator-1 is an orally active and brain-penetrant GABAAR agonist and 5-HT2AR antagonist with Kd values of 0.89 and 0.78 μM. GABAAR/5-HT2AR modulator-1 blocks 5-HT-stimulated IP1 accumulation, inducing a chloride current, reduces LPS (HY-D1056)-induced increases of ROS, NO, TNF-α, IL-6, IL-1β, iNOS, and COX-2 levels. Antidepressant agent 11 dihydrochloride inhibits NF-κB pathway activation by reducing IκBα and p65 phosphorylation and blocking p65 nuclear translocation. GABAAR/5-HT2AR modulator-1 alleviates depression-like behaviors in LPS-challenged and chronic restraint stress-challenged mice, and protects hippocampal neurons against inflammation-mediated damage.

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GABAAR/5-HT2AR modulator-1

GABAAR/5-HT2AR modulator-1 Chemical Structure

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GABAAR/5-HT2AR modulator-1 Related Antibodies

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COX COX-1 COX-2 COX-3

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nNOS iNOS eNOS

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Description

GABAAR/5-HT2AR modulator-1 is an orally active and brain-penetrant GABAAR agonist and 5-HT2AR antagonist with Kd values of 0.89 and 0.78 μM. GABAAR/5-HT2AR modulator-1 blocks 5-HT-stimulated IP1 accumulation, inducing a chloride current, reduces LPS (HY-D1056)-induced increases of ROS, NO, TNF-α, IL-6, IL-1β, iNOS, and COX-2 levels. Antidepressant agent 11 dihydrochloride inhibits NF-κB pathway activation by reducing IκBα and p65 phosphorylation and blocking p65 nuclear translocation. GABAAR/5-HT2AR modulator-1 alleviates depression-like behaviors in LPS-challenged and chronic restraint stress-challenged mice, and protects hippocampal neurons against inflammation-mediated damage[1].

IC50 & Target[1]

5-HT2A Receptor

0.78 μM (Kd)

GABAA

0.89 μM (Kd)

IL-1β

 

IL-6

 

COX-2

 

In Vitro

GABAAR/5-HT2AR modulator-1 (Compound 4f) binds to 5-HT2AR with a Kd of 0.78 μM and binds to GABAAR with a Kd of 0.89 μM[1].
GABAAR/5-HT2AR modulator-1 binds to 5-HT1AR, 5-HT6R, 5-HT7R, and D2R with Kd values of 5.94 μM, 3.62 μM, 2.96 μM, and 8.12 μM, respectively[1].
GABAAR/5-HT2AR modulator-1 inhibits hERG potassium channels with an IC50 >30 μM, indicating low cardiotoxic risk[1].
GABAAR/5-HT2AR modulator-1 has low cytotoxicity in HEK293T, BV2, and HT22 cells, with IC50 values >100 μM[1].
GABAAR/5-HT2AR modulator-1 acts as a 5-HT2AR antagonist in transfected HEK293T cells, blocking 5-HT-stimulated IP1 accumulation with an IC50 of 0.83 μM[1].
GABAAR/5-HT2AR modulator-1 (1 μM) functions as a GABAAR agonist in HEK293T cells stably expressing human α1β3γ2 GABAAR, inducing a chloride current amplitude of -726 pA[1].
GABAAR/5-HT2AR modulator-1 (5-20 μM) concentration-dependently reduces LPS (HY-D1056)-induced ROS and NO production in BV2 microglial cells[1].
GABAAR/5-HT2AR modulator-1 (5-20 μM) concentration-dependently reduces LPS-induced mRNA expression of TNF-α, IL-6, IL-1β, iNOS, and COX-2 in BV2 microglial cells[1].
GABAAR/5-HT2AR modulator-1 (5-20 μM) concentration-dependently reduces LPS-induced secretion of TNF-α, IL-6, and IL-1β in BV2 microglial cells[1].
GABAAR/5-HT2AR modulator-1 (5-20 μM) concentration-dependently reduces LPS-induced COX-2 and iNOS protein expression in BV2 microglial cells[1].
GABAAR/5-HT2AR modulator-1 (5-20 μM) concentration-dependently inhibits LPS-induced NF-κB pathway activation in BV2 microglial cells by reducing IκBα and p65 phosphorylation and blocking p65 nuclear translocation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GABAAR/5-HT2AR modulator-1 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax AUC0-t AUC0-∞ T1/2 Bioavailability Tmax (Plasma) Cmax (Brain) Tmax (Brain)
Mice[1] 1 mg/kg i.v. 42.2 ng/mL 0.083 h 24.7 ng·h/mL 25.4 ng·h/mL 1.15 h / / / /
Mice[1] 10 mg/kg p.o. 35.4 ng/mL 0.417 h 47.9 ng·h/mL 50 ng·h/mL 1.86 h 19.4 % / / /
Mice[1] 10 mg/kg p.o. / / / / / / 0.5 h 5.63 ng/mL 2 h
In Vivo

GABAAR/5-HT2AR modulator-1 (Compound 4f) (25-50 mg/kg; p.o.) dose-dependently alleviates inflammation-driven depression-like behaviors, reduces neuroinflammatory markers, and protects hippocampal tissue in LPS (HY-D1056)-challenged male ICR mice[1].
GABAAR/5-HT2AR modulator-1 (25-50 mg/kg; p.o.) dose-dependently alleviates stress-related depression-like behaviors in chronic restraint stress-exposed male ICR mice[1].
GABAAR/5-HT2AR modulator-1 (25-50 mg/kg; p.o.) exhibits significant antidepressant-like activity at oral doses of 25 mg/kg and 50 mg/kg in naive male ICR mice and shows no overt toxicological effects on major vital organs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Depressent ICR mice (male, LPS-induced inflammation-driven depression)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: p.o.
Result: Restored ambulatory activity and increased central zone entries in the open field test compared to LPS-treated mice.
Significantly reduced immobility time in the tail suspension test and forced swimming test, with the 50 mg/kg dose showing the most pronounced effect.
Dose-dependently reduced hippocampal mRNA levels of TNF-α, IL-6, IL-1β, iNOS, and COX-2.
Reduced serum levels of TNF-α, IL-6, and IL-1β.
Reduced hippocampal protein levels of iNOS and COX-2.
Dose-dependently restored hippocampal structural integrity via Nissl staining, with the 50 mg/kg dose exhibiting near-normal morphology.
Dose-dependently suppressed LPS-induced microglial activation via immunofluorescence staining, with the 50 mg/kg dose displaying near-complete normalization of microglial phenotype.
Molecular Weight

408.36

Formula

C18H31Cl2N3O3
SMILES

COC1=CC=CC=C1N2CCN(CCCOC(CCCN)=O)CC2.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GABAAR/5-HT2AR modulator-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GABAAR/5-HT2AR modulator-1GABA Receptor5-HT ReceptorReactive Oxygen Species (ROS)TNF ReceptorInterleukin RelatedCOXNF-κBIKKNO SynthaseGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorTumor Necrosis Factor ReceptorTNFRILCyclooxygenaseNuclear factor-κBNuclear factor-kappaBIκB kinaseI kappa B kinase Nitric oxide synthasesNOShippocampal neuronsHT22 cellsGABAARNF-κB pathwayneuroinflammationICR mice5-HT2ARHEK293T cellsmicroglial GABAARsBV2 microglial cellsInhibitorinhibitorinhibit

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