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Lofepramine

CAT: 0804-HY-12390-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12390-01Size:5 mg
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Description
Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) 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.[2][3][4].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched