Drug intelligence / Profile preview

clomipramine + maprotiline

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Clomipramine + maprotiline is a combination of two antidepressant drugs, each with distinct but complementary mechanisms of action. Clomipramine is a tricyclic antidepressant (TCA) primarily used for obsessive-compulsive disorder and major depressive disorder, acting mainly as a serotonin reuptake inhibitor with additional effects on norepinephrine reuptake and various neurotransmitter receptors. Maprotiline is a tetracyclic antidepressant (TeCA) that inhibits the presynaptic uptake of norepinephrine and acts as an antagonist at central α2-adrenergic receptors, also displaying antihistaminic and antimuscarinic properties. The combination has been studied in severe depression, where it may provide broader symptom relief than either drug alone by targeting both serotonergic and noradrenergic pathways[1][4]. Both agents have demonstrated anti-inflammatory effects through inhibition of neutrophil migration and mast cell degranulation[6][7].

02

Targets

HRH1 (Histamine H1 Receptor)HTR2A (Serotonin receptor 5-HT2A)HTR7 (5-hydroxytryptamine receptor 7)ADRA2A (α2A)ADRA1A (α1A)NET (Norepinephrine Transporter)mAChR (Muscarinic acetylcholine receptors)HTR2C (5-hydroxytryptamine 2C receptor)SCN1A (Voltage-gated sodium channel protein type 1 subunit alpha)DAT (Dopamine plasma membrane transport protein)SERT (Sodium-dependent serotonin transporter)

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