[2H3]-Maprotiline hydrochloride

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[2H3]-Maprotiline hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  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.

• Einzelnachweise

  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)

[2H3]-Maprotiline hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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