H3R antagonist 8
H3R antagonist 8 is a selective nonimidazole histamine H3 receptor antagonist (IC50 = 0.35 μM). H3R antagonist 8 exhibits hERG channel blockade activity (IC50 = 0.67 μM). H3R antagonist 8 inhibits seizures by antagonizing H3 receptor. H3R antagonist 8 reduces tonic hind limb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED50 = 20.21 mg/kg) and and shortens pentylenetetrazol (PTZ)-induced total movement distance in AB strain zebrafish larvae. H3R antagonist 8 can be used for the study of epilepsy.
For research use only. We do not sell to patients.
- CAS No.: 3097193-89-7
- Formula: C23H27ClN2O2
- Molecular Weight:398.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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H3 receptor 0.35 μM (IC50) |
H3R antagonist 8 (Compound 6n) shows potent H3 receptor antagonistic activity with an IC50 value of 0.35 μM in the CRE-driven luciferase assay using HEK-293 cells expressing human H3R[1].
H3R antagonist 8 (0.1-100 μM) exhibits hERG channel blockade activity with an IC50 value of 0.67 μM using the patch-clamp technique in HEK-293 cells stably expressing hERG potassium channels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
H3R antagonist 8 (1 μM, pretreatment for 3 h) significantly reduces the total movement distance of AB strain zebrafish larvae induced by pentylenetetrazol (PTZ)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male KunMing mice (6-8 weeks old, 18-22 g) were used for the maximal electroshock seizure (MES)-induced seizure model[1]
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Dosage:30 mg/kg
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Administration:i.p., single dose
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Result:Abolished tonic hind limb extension (THLE) of mice at 4 h post-administration, with a median effective dose of 20.21 mg/kg.
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Animal Model:Pentylenetetrazol (PTZ)-induced AB strain zebrafish[1]
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Dosage:1 μM
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Administration:Pretreatment for 3 h
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Result:Reduced the total movement distance induced by PTZ.
Chemical Information
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CAS No. 3097193-89-7
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Molecular Weight 398.93
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Formula C23H27ClN2O2
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SMILES
CCN(CC)CCCOC1=CC=C(C2=C(C3=CC=CC=C3Cl)OC(C)=N2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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