C20H23D3N2•C4H4O4
货号:ajcx24260
CAS:N/A
分子式:C20H23D3N2•C4H4O4
分子量：413.5
溶解度:DMSO: soluble,Methanol: soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Trimipramine-d₃(maleate) is intended for use as an internal standard for the quantification of trimipramine (maleate) by GC- or LC-MS. Trimipramine is a tricyclic antidepressant.^1,2,3It selectively binds the serotonin (5-HT) transporter (SERT) over the norepinephrine transporter (NET) and dopamine transporter (DAT; K_ds = 149, 2,450, and 3,780 nM, respectively) and acts as a histamine H₁receptor antagonist (K_i= 0.02 µM) that is selective for histamine H₁over H₂, H₃, and H₄receptors (K_is = 0.04, >100, and 43.6 µM, respectively).^1,2Trimipramine binds to muscarinic acetylcholine and α₁- and α₂-adrenergic receptors (K_ds = 58, 24, and 580 nM, respectively), as well as dopamine D₁and D₂receptors and 5-HT receptor subtypes 5-HT_1Cand 5-HT₂(K_is = 346.7, 57.5, 537, and 19.5 nM, respectively).^1,3It reduces immobility time in the forced swim test in rats when administered at a dose of 10 mg/kg.⁴Formulations containing trimipramine have previously been used in the treatment of depression.

1.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) 2.Appl, H., Holzammer, T., Dove, S., et al.Interactions of recombinant human histamine H1, H2, H3, and H4 receptors with 34 antidepressants and antipsychoticsNaunyn-Schmiedebergs Arch. Pharmacol.385(2)145-170(2012) 3.Gross, G., Xin, X., and Gastpar, M.Trimipramine: Pharmacological reevaluation and comparison with clozapineNeuropharmacology30(11)1159-1166(1991) 4.Delini-Stula, A., Radeke, E., and van Riezen, H.Enhanced functional responsiveness of the dopaminergic system-the mechanism of anti-immobility effects of antidepressants in the behavioural despair test in the ratNeuropharmacology27(9)943-947(1988)