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Cat. No.: HY-129862A

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Eclanamine

Eclanamine is an orally effective non-tricyclic antidepressant and an adrenergic receptor modulator. Eclanamine blocks biogenic amine uptake and enhances α2-receptor sensitivity, and long-term administration induces downregulation and desensitization of cortical β-receptors. Eclanamine is used in the study of depression.

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CAS No.: 67450-44-6
Formule: C₁₆H₂₂Cl₂N₂O
Masse moléculaire:329.26

Stockage:

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

Eclanamine Chemical Structure

CAS No.: 67450-44-6

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
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Activité biologique

Description

IC₅₀ & Target

^[1]

α2-adrenergic receptor

β adrenergic receptor

Voir tous les produits spécifiques à Isoform Adrenergic Receptor :

In Vitro

Eclanamine weakly inhibits the binding of (³H)-dihydroalpranolol (DHA) in rat brain cortex tissue homogenates (inhibition rate below 50%)^[3].
Eclanamine induces gene mutations in CHO/HPRT and AS52 cells^[2].

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

In Vivo

Eclanamine (45 mg single dose; p.o.; single administration; urine is monitored and collected for 96 h after administration) produces N-desmethyleclanamine (DME) and N,N-didesmethyleclanamine (DDME) metabolites and is excreted in urine^[1].
Eclanamine (1-30 mg/kg/day; i.v.; continuous infusion; treatment duration of 8 to 168 h) dose-dependently downregulates cerebral cortical β-adrenergic receptor (beta-AR) density in female Sprague-Dawley rats^[3].

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

Animal Model:

Sprague-Dawley rats (female, 280-320 g)^[3]
Dosage:

1, 3, 10, and 30 mg/kg/day
Administration:

i.v.; continuous infusion; 24 h
Result:

Dose-dependently reduced the density of beta-adrenergic receptors (Bmax) in the cerebral cortex with a significant dose-response relationship.
The minimum effective dose that significantly down-regulated beta-AR at 24 hours was 3.0 mg/kg/day.

Animal Model:

Sprague-Dawley rats (female)^[3]
Dosage:

10 mg/kg/day
Administration:

i.v.; continuous infusion; 8, 16, 24, 48, 72, and 168 hours
Result:

Resulted in a significant reduction in the number of beta-AR at 16 and 24 hours.
The peak effect was observed at 72 hours, at which time it produced a similar degree of down-regulation to imipramine.

Chemical Information

CAS No. 67450-44-6
Masse moléculaire 329.26
Formule C₁₆H₂₂Cl₂N₂O
SMILES

CCC(N(C1=CC(Cl)=C(C=C1)Cl)[C@H]2[C@@H](CCC2)N(C)C)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Lakings DB, et al. High-performance liquid chromatographic method for the determination of eclanamine and its N-desmethyl and N,N-didesmethyl metabolites in urine. J Chromatogr. 1988 Jun 24;428(1):131-9.

[2]. Aaron CS, et al. Risk and benefit evaluation in development of pharmaceutical products. Environ Health Perspect.

[3]. Sethy VH, et al. Dose-dependent down-regulation of beta-adrenergic receptors after chronic intravenous infusion of antidepressants. Progress in neuro-psychopharmacology & biological psychiatry. 1988;12(5):673-82.

[4]. Szmuszkovicz J, et al. A new nontricyclic antidepressant agent. Synthesis and activity of N-[trans-2-(dimethylamino)cyclopentyl]-N-(3,4-dichlorophenyl)propanamide and related compounds. J Med Chem. 1981 Oct;24(10):1230-6. [Content Brief]

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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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100 mg

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