Lofepramine hydrochloride  (Synonyms: Lopramine 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. ^[1][2][3][4].

Lofepramine (0.01-100 μM, 10 min) inhibits both ³H-5-HT and ³H-NA uptake into synaptosomal fractions in rats brain cells^[1].

Lofepramine (28-45 mg /kg, i.p., 1 h before experiment) only decreases the uptake of both in rats at 28 mg/kg pretreated with SKF 525A and decreases both 5-HT and Noradrenaline (HY-13715) in intact rats at 45 mg/kg^[1].
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.

455.42

C₂₆H₂₈Cl₂N₂O

26786-32-3

CN(CC(C1=CC=C(Cl)C=C1)=O)CCCN2C3=CC=CC=C3CCC4=CC=CC=C42.Cl

Room temperature in continental US; may vary elsewhere.

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

• [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]