BP1.3656B
BP1.3656B is a selective, orally active, blood-brain barrier-permeable histamine H3 receptor (histamine H3 receptor) inverse agonist/antagonist, with a KB value of 0.08 nM for antagonizing agonist-induced activity and an IC50 value of 0.38 nM for directly inhibiting the basal activity of the receptor. BP1.3656B reduces alcohol consumption, alcohol-seeking behavior, alcohol self-administration, motivation to drink, alcohol relapse, alcohol-induced hyperlocomotion, and binge alcohol intake. BP1.3656B is applicable for the research of alcohol use disorder.
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- CAS No.: 914302-78-6
- Formule: C20H28Cl2N2O2
- Masse moléculaire:399.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
H3 receptor 0.38 nM (IC50) |
In Vivo
BP1.3656B (0.03-0.1 mg/kg; i.p.; single administration) dose-dependently increases extracellular acetylcholine levels in the hippocampus of male Wistar rats[1].
BP1.3656B (0.005-0.3 mg/kg; single administration) reduces alcohol-induced motor hyperactivity in female DBA/2J mice[1].
BP1.3656B (0.3 mg/kg; i.p.; once daily for 4 consecutive days) reduces alcohol-induced locomotor sensitization in female DBA/2J mice by 31%-44% over the 4-day treatment course[1].
BP1.3656B (0.3 mg/kg; i.p.; single administration) reduces alcohol intake by 25% in male mice in the dark drinking model, normalizes anxiety-like behaviors in mice during alcohol withdrawal, and decreases voluntary alcohol intake in non-addicted and alcohol-dependent male rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/2J (female)[1]
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Dosage:0.005 mg/kg; 0.03 mg/kg; 0.3 mg/kg
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Administration:i.p.; single dose
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Result:Reduced alcohol-induced locomotor activity by 37%.
Reduced alcohol-induced locomotor activity by 39%.
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Animal Model:DBA/2J (female)[1]
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Dosage:0.3 mg/kg
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Administration:i.p.; daily; 4 consecutive days
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Result:Reduced alcohol-induced locomotor sensitization by 31% on day 1, 44% on day 2, 25% on day 3, and 40% on day 4.
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Animal Model:C57BL/6J (male)[1]
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Dosage:0.3 mg/kg
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Administration:i.p.; singe dose
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Result:Reduced 2-hour binge alcohol intake by 25%.
Increased time spent in the open arms of the elevated plus maze
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Animal Model:Long Evans (male; non-dependent)[1]
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Dosage:0.3 mg/kg
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Administration:i.p.; single dose
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Result:Reduced active lever presses by 70%, alcohol consumption by 73%, and motivation (breakpoint) by 43% compared to placebo.
Reduced alcohol relapse by 44% on the first day post-extinction, with effects maintained across relapse sessions.
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Animal Model:Long Evans (male; alcohol-dependent)[1]
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Dosage:0.3 mg/kg
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Administration:i.p.; single dose
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Result:Reduced active lever presses by 46%, alcohol consumption by 55%, and motivation (breakpoint) by 44% compared to placebo.
Completely blocked alcohol relapse on the first day post-extinction, with effects maintained across relapse sessions.
Chemical Information
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CAS No. 914302-78-6
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Masse moléculaire 399.35
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Formule C20H28Cl2N2O2
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SMILES
C[C@H]1CCCN(C1)CCCOC2=CC=C(C=C2)C3=CC=[N+](C=C3)[O-].Cl.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BP1.3656B Related Classifications
HY-181960 Related Classifications
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