Description
Maprotiline is a tetracyclic antidepressant that also exhibits sedative, anxiolytic, sympathomimetic, and anticancer activities. Maprotiline acts as an antagonist at norepinephrine transporters (NET), H1 histamine receptors, 5-HT2 receptors, α1-adrenergic receptors, muscarinic acetylcholine receptors (mAChRs), and L-type Ca2+ channels. Maprotiline induces caspase-mediated apoptosis in neuroblastoma cells, inhibiting cell viability in a JNK- and ERK-dependent manner. This compound also acts as a functional inhibitor of acid sphingomyelinase (FIASMA).
References
Jan CR, Su JA, Teng CC, et al. Mechanism of maprotiline-induced apoptosis: role of [Ca2+](i), ERK, JNK and caspase-3 signaling pathways. Toxicology. 2013 Feb 8;304:1-12. PMID: 23219590.
Zahradník I, Minarovic I, Zahradníková A. Inhibition of the cardiac L-type calcium channel current by antidepressant drugs. J Pharmacol Exp Ther. 2008 Mar;324(3):977-84. PMID: 18048694.
Mayers AG, Baldwin DS. Antidepressants and their effect on sleep. Hum Psychopharmacol. 2005 Dec;20(8):533-59. PMID: 16229049.
Muscat R, Papp M, Willner P. Reversal of stress-induced anhedonia by the atypical antidepressants, fluoxetine and maprotiline. Psychopharmacology (Berl). 1992;109(4):433-8. PMID: 1365858.
