Formulation: A solid
Formal Name: 10,11-dihydro-N-methyl-5H-dibenz[b,f]azepine-2,4,6,8-d4-5-propanamine, monohydrochloride
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C18H18D4N2 • HCl
Formula Weight: 306,9
Shelf life (days): 1460
CAS Number: 61361-34-0
Notes: Desipramine-d4 is intended for use as an internal standard for the quantification of desipramine by GC- or LC-MS. Desipramine is a tricyclic antidepressant and an active metabolite of imipramine (Item No. 15890).{32156} It inhibits the serotonin (5-HT) and norepinephrine transporters (Kis = 163 and 3.5 nM for human SERT and NET, respectively) and is an antagonist of the 5-HT receptor subtype 5-HT2A and the α1-adrenergic receptor (α1-AR), as well as histamine H1 and muscarinic acetylcholine receptors (mAChRs; Kis = 115, 23, 31, and 37 nM, respectively). Desipramine is selective for the 5-HT2A receptor over the 5-HT1A receptor (Ki = 2,272 nM) and for α1-AR over α2-AR (Ki = 1,379 nM). It also selectively inhibits G protein-activated inward rectifier potassium channel (GIRK), also known as Kir3, currents in Xenopus oocytes expressing human GIRK1 and GIRK2 or human GIRK1 and GIRK4 (IC50s = 36.4 and 53.9 µM, respectively) over Kir1.1 or Kir2.1 currents in Xenopus oocytes expressing the human channels (IC50s = >100 µM for both).{67027} Desipramine (3.2 mg/kg) decreases immobility time in the forced swim test in mice.{67028} It also decreases flinching, as well as paw biting and licking, in the second phase of the formalin test in rats.{67029} Formulations containing desipramine have been used in the treatment of depression.
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