Lofepramine

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].

Product Specifications

CAS Number

[23047-25-8]

Product Name Alternative

Lopramine

UNSPSC

12352005

Hazard Statement

H302, H335, H413

Target

5-HT Receptor; Adrenergic Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/lofepramine.html

Purity

99.0

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C26H27ClN2O

Molecular Weight

418.96

Precautions

H302, H335, H413

References & Citations

[1]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.|[2]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.|[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. |[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) :101-5.