Formulation: A solid
Formal Name: 3-dibenz[b,e]oxepin-11(6H)-ylidene-N-methyl-N-(methyl-d3)-1-propanamine, monohydrochloride
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C19H18D3NO • HCl
Formula Weight: 318,9
Shelf life (days): 1460
CAS Number: 347840-07-7
Notes: Doxepin-d3 is intended for use as an internal standard for the quantification of doxepin (Item No. 15888) by GC- or LC-MS. Doxepin is a tricyclic antidepressant that binds to the serotonin (5-HT) transporter (SERT) and norepinephrine transporter (NET; Kds = 68 and 29.5 nM, respectively).{22877} It is a histamine H1 receptor antagonist (Ki = 1.23 nM).{40358} Doxepin selectively binds to SERT and NET over the dopamine transporter (DAT; Kd = 12,100 nM) and inhibits histamine H1 over H2, H3, and H4 receptors (Kis = 170, 39,810, and 15,135 nM, respectively).{22877,40358} It also binds to the 5-HT2 receptor, as well as to muscarinic acetylcholine and α1-adrenergic receptors (α1-ARs; Kds = 27, 23, and 23.5 nM, respectively).{25803} Doxepin (10 mg/kg, i.p.) decreases allodynia and hyperalgesia in a mouse model of chronic constriction injury-induced neuropathic pain.{48874} It increases the distance traveled in the center of the open field test and reduces immobility time in the forced swim test in a mouse model of depression induced by chronic stress when administered orally at a dose of 15 mg/kg.{48875} Formulations containing doxepin have been used in the treatment of depression and insomnia.