| 包装: | 1mg |
| 规格: | 98% |
| 市场价: | 1930元 |
| 分子量: | 319.9 |
Background:
Doxepin-13C-d3is intended for use as an internal standard for the quantification of doxepin 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).1It is a histamine H1receptor antagonist (Ki= 1.23 nM).2Doxepin selectively binds to SERT and NET over the dopamine transporter (DAT; Kd= 12,100 nM) and inhibits histamine H1over H2, H3, and H4receptors (Kis = 170, 39,810, and 15,135 nM, respectively).1,2It also binds to the 5-HT2receptor, as well as to muscarinic acetylcholine and α1-adrenergic receptors (α1-ARs; Kds = 27, 23, and 23.5 nM, respectively).3Doxepin (10 mg/kg, i.p.) decreases allodynia and hyperalgesia in a mouse model of chronic constriction injury-induced neuropathic pain.4It 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.5Formulations containing doxepin have been used in the treatment of depression and insomnia.
1.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) 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.Cusack, B., Nelson, A., and Richelson, E.Binding of antidepressants to human brain receptors: Focus on newer generation compoundsPsychopharmacology (Berl.)114(4)559-565(1994) 4.Mika, J., Jurga, A.M., Starnowska, J., et al.Effects of chronic doxepin and amitriptyline administration in naÏve mice and in neuropathic pain mice modelNeuroscience29438-50(2015) 5.Kim, Y.R., Park, B.-K., Kim, Y.H., et al.Antidepressant effect of Fraxinus rhynchophylla Hance extract in a mouse model of chronic stress-induced depressionBioMed. Res. Int.8249563(2018)
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