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Cat. No.: HY-12391

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Dibenzepine

Dibenzepine is a blood-brain barrier permeable ligand of the histamine H1 receptor (Histamine H1 Receptor), with a K_i value of 0.02 μM. Dibenzepine exhibits varying degrees of affinity for multiple serotonin receptors and dopamine receptors. Dibenzepine can be used in research related to depression, schizophrenia, dementia, and non-specific agitation.

For research use only. We do not sell to patients.

CAS No.: 4498-32-2
Formula: C₁₈H₂₁N₃O
Molecular Weight:295.39

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Dibenzepine Chemical Structure

CAS No.: 4498-32-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

H₁ Receptor

0.02 μM (Ki)

All Histamine Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Ventricular myocyte	IC₅₀	364 μM Compound: Dibenzepin	Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes	[PMID: 22761000]

In Vitro

Dibenzepine (compound 5) exhibits high-affinity binding to the histamine H₁ receptor (K_i = 0.02 μM), shows moderate affinity for 5-HT₁A, 5-HT₂A, 5-HT₆, and 5-HT₇ receptors, weak affinity for SERT, and extremely low affinity for the D₂ receptor^[1].
Dibenzepine (1 μM-0.01 M; 1 h) inhibits hypotonic hemolysis of human erythrocytes and induces hemolysis at a concentration of 5 mM^[8].

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

In Vivo

Dibenzepine (3.5 mg/kg; administered daily for 28 consecutive days) increases the β-endorphin content in the brain of healthy albino Wistar rats to 906.63 pg/g^[10].

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

Animal Model:

Albino Wistar (250 g)^[10]
Dosage:

3.5 mg/kg
Administration:

once daily for 28 days
Result:

Produced a brain β-endorphin content of 906.63 pg/g, which was higher than the control group's value but not statistically significant.

Chemical Information

CAS No. 4498-32-2
Molecular Weight 295.39
Formula C₁₈H₂₁N₃O
SMILES

O=C1C=2C=CC=CC2N(C=3C=CC=CC3N1CCN(C)C)C
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

Handling Instructions (2659 KB)

References

[1]. Bieszczad B, et al. Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs. Bioorganic & medicinal chemistry letters. 2020 Nov 01;30(21):127493.

[2]. Bieszczad B, et al. Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs. Bioorganic & medicinal chemistry letters. 2020 Nov 01;30(21):127493.

[3]. De Leenheer A, et al. Improved method for determining dibenzepine and its N-demethylated metabolites in human urine. J Pharm Sci. 1973 Jan;62(1):31-6.

[4]. Brochon R, et al. The detection and determination of dibenzepine and its metabolites in autopsy material. Arch Toxikol. 1969;24(4):249-59.

[5]. Christensen H, et al. Dibenzepine and its metabolites in blood, muscle, liver, vitreous body and urine from fatal poisoning. Acta Pharmacol Toxicol (Copenh). 1975 Nov;37(5):393-401.

[6]. Bonnichsen R, et al. Determination of dibenzepine in autopsy material. Z Rechtsmed. 1971;68(5):253-60.

[7]. Schlicht HJ, et al. Gas chromatographic determination of dibenzepine and its basic metabolites in biological material. J Chromatogr. 1978 Dec 11;166(2):599-603.

[8]. Langslet A, et al. Effects of dibenzepine and imipramine on the isolated rat heart. Eur J Pharmacol. 1971 May;14(4):333-9. [Content Brief]

[9]. van der Meer JW, et al. Abstract!. The Netherlands journal of medicine. 2002 Dec;60(11):418. [Content Brief]

[10]. Jadrić R, et al. Comparison of trazodone, diazepame and dibenzepine influences on rat brain beta-endorphins content. Bosnian journal of basic medical sciences. 2007 Aug;7(3):222-5.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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