2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. 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.

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H3R antagonist 8

H3R antagonist 8 Chemical Structure

CAS No. : 3097193-89-7

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H3R antagonist 8 Related Antibodies

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Description

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[1].

IC50 & Target[1]

H3 receptor

0.35 μM (IC50)

In Vitro

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 Related Antibodies
In Vivo

H3R antagonist 8 (Compound 6n) (30 mg/kg, i.p., single dose) completely abolishes tonic hind limb extension (THLE) of male KunMing mice in the maximal electroshock seizure (MES)-induced seizure model[1].
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.

Animal Model: Male KunMing mice (6-8 weeks old, 18-22 g) were used for the maximal electroshock seizure (MES)-induced seizure model[1]
Dosage: 30 mg/kg
Administration: i.p., single dose
Result: Abolished tonic hind limb extension (THLE) of mice at 4 h post-administration, with a median effective dose of 20.21 mg/kg.
Animal Model: Pentylenetetrazol (PTZ)-induced AB strain zebrafish[1]
Dosage: 1 μM
Administration: Pretreatment for 3 h
Result: Reduced the total movement distance induced by PTZ.
Molecular Weight

398.93

Formula

C23H27ClN2O2
CAS No.
SMILES

CCN(CC)CCCOC1=CC=C(C2=C(C3=CC=CC=C3Cl)OC(C)=N2)C=C1
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H3R antagonist 8 Related Classifications

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  • 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:

H3R antagonist 83097193-89-7Histamine ReceptorEpilepsyzebrafishH3 receptorhERG channelInhibitorinhibitorinhibit

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