Drug intelligence / Profile preview

maprotiline

Development stage
Phase 1
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Maprotiline is a tetracyclic antidepressant primarily used to treat depressive disorders, including major depressive disorder, dysthymic disorder (depressive neurosis), and bipolar disorder (manic depressive illness), as well as anxiety associated with depression. It acts mainly by inhibiting the reuptake of norepinephrine at nerve endings in the brain, thereby increasing its availability and enhancing adrenergic neurotransmission. Maprotiline has strong antihistaminic properties, moderate antagonism at 5-HT2 and α1-adrenergic receptors, weak antagonism at D2 and muscarinic acetylcholine receptors, and is a potent antagonist of the 5-HT7 receptor. Its pharmacological profile explains its antidepressant, sedative, anxiolytic, and sympathomimetic activities. Maprotiline differs from tricyclic antidepressants in that it has minimal effect on serotonin reuptake but may increase serotonergic transmission at higher doses[1][2][5][6][8].

Brand names
Ludiomil
Other names
maprotiline hydrochloride
02

Targets

HTR2A (Serotonin receptor 5-HT2A)mAChR (Muscarinic acetylcholine receptors)HRH1 (Histamine H1 Receptor)NET (Norepinephrine Transporter)ADRA1A (α1A)HTR7 (5-hydroxytryptamine receptor 7)DRD2 (Dopamine D2 Receptor)

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