Biological Activity
Maprotiline-d3 is intended for use as an internal standard for the quantification of maprotiline by GC- or LC-MS. Maprotiline is a tricyclic antidepressant.1,2 It binds to the norepinephrine transporter (NET; Kd = 11 nM) and is selective for NET over the serotonin and dopamine transporters (Kds = 5,800 and 1,000 nM, respectively).2 Maprotiline also binds to the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 51 nM), as well as histamine H1, muscarinic acetylcholine, α1-adrenergic, and dopamine D2 receptors (Kds = 2, 570, 90, and 350 nM, respectively).3 In vivo, maprotiline inhibits norepinephrine reuptake in rat brain and peripheral tissues.4 It reduces isolation-induced aggressive behavior and inhibits electrical foot-shock stimulation-induced belligerence in mice when administered at doses ranging from 3 to 10 mg/kg. Maprotiline also reduces aggressive behavior in rhesus monkeys housed in groups. Formulations containing maprotiline have been used in the treatment of depression and anxiety.
References
1.Spencer, P.S.Review of the pharmacology of existing antidepressantsBr. J. Clin. Pharmacol.4(Suppl 2)57S-68S(1977)
2.Tatsumi, M., Groshan, K., Blakely, R.D., et al.Pharmacological profile of antidepressants and related compounds at human monoamine transportersEur. J. Pharmacol.340(2-3)249-258(1997)
3.Richelson, E., and Nelson, A.Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitroJ. Pharmacol. Exp. Ther.230(1)94-102(1984)
4.Pinder, R.M., Brogden, R.N., Speight, T.M., et al.Maprotiline: A review of its pharmacological properties and therapeutic efficacy in mental depressive statesDrugs13(5)321-352(1977)
