Lofepramine hydrochloride
Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) (HY-13715) and 5-hydroxytryptamine (5-HT) with IC50s of 2.7 μM and 11 μM, respectively. Lofepramine exerts its antidepressant activity by promoting noradrenergic neurotransmission. Lofepramine also enhances serotonergic neurotransmission by inhibiting neuronal uptake of 5-HT and tryptophan pyrrolase. Lofepramine exhibits significant anxiolytic properties. .
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- CAS No.: 26786-32-3
- Formula: C26H28Cl2N2O
- Molecular Weight:455.42
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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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Help & FAQs
Biological Activity
Lofepramine (0.01-100 μM, 10 min) inhibits both 3H-5-HT and 3H-NA uptake into synaptosomal fractions in rats brain cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Lofepramine (50 mg /kg, i.p., was injected 30 min before intraventricular administration of 3H-5-HT (0.75 μCi) or 3H-NA (1.2 μCi)) is effective in inhibiting Noradrenaline (HY-13715) uptake into both fractions (the P2- and S-fractions) [1].
Lofepramine (20 mg /kg, i.p., daily, 2 weeks) and it’s desmethylated metabolites, DMI (Desipramine) (HY-B1272A), DML(Desmethyl lofepramine) and DDMI (Desmethyl desipramin), exhibits antidepressant activity in the OB (olfactory bulbectomy) model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar strain rats, 150-200 g[1].
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Dosage:28, 45 mg/kg
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Administration:i.p., 1 h before experiment , SKF 525A, 30 mg/kg, i.p., was injected 30 min before experiment.
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Result:Did not influence the in vitro uptake of either 5-HT or noradrenaline in normal rats, but significantly decreased the uptake of both in rats at 28 mg/kg pretreated with SKF 525A.
Decreased significantly both 5-HT and noradrenaline uptake in intact rats at 45 mg/kg.
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Animal Model:Male Wistar strain rats, 150-200 g[1].
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Dosage:30, 50 mg/kg
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Administration:i.p., was injected 30 min before intraventricular administration of 3H-5-HT (0.75 μCi) or 3H-NA (1.2 μCi).
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Result:Was also effective in inhibiting noradrenaline uptake into both fractions (the P2- and S-fractions) at 50 mg/kg.
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Animal Model:Male Sprague-Dawley, 250–280 g. Bilateral olfactory bulbectomy (OB) was performed under anaesthesia (2.5% w/v; 10 mL/kg, i.p.)[4].
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Dosage:20 mg/kg
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Administration:i.p., daily, 2 weeks
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Result:Had no effects on immobility time.
Attenuated the increase in activity in the OB control group.
Chemical Information
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CAS No. 26786-32-3
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Molecular Weight 455.42
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Formula C26H28Cl2N2O
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SMILES
CN(CC(C1=CC=C(Cl)C=C1)=O)CCCN2C3=CC=CC=C3CCC4=CC=CC=C42.Cl
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Synonyms
Lopramine hydrochloride
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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
[1]. Segawa T, et al. Effect of lofepramine and other antidepressants on the uptake of 5-hydroxytryptamine and noradrenaline into rat brain monoaminergic neurons. J Pharm Pharmacol. 1977 Mar;29(3):139-42. [Content Brief]
[2]. Lancaster SG, et al. Lofepramine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness. Drugs. 1989 Feb;37(2):123-40. [Content Brief]
[3]. McIntyre RS, et al. The neurogenic compound, NSI-189 phosphate: a novel multi-domain treatment capable of pro-cognitive and antidepressant effects. Expert Opin Investig Drugs. 2017 Jun;26(6):767-770. [Content Brief]
[4]. Kelly JP, et al. An investigation of the antidepressant properties of lofepramine and its desmethylated metabolites in the forced swim and olfactory bulbectomized rat models of depression. Eur Neuropsychopharmacol. 1999 Jan;9(1-2):101 [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lofepramine hydrochloride Related Classifications
HY-12390A Related Classifications
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