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Cat. No. Name Size Price Add Cart
KI0809Doxepin1 g$88

Chemical Characteristic

Product NameDoxepin
SynonymsXepin, Zonalon, Sinequan
CAS No.1668-19-5
Molecular Weight 279.38
FormulaC19H21NO
Chemical Structure

Biological activities

Doxepin is a moderately potent competitive inhibitor of serotonin uptake in human blood platelets in vitro, with an inhibitory constant Ki of about 200 nM. The inhibitory effect of doxepin is 6 times stronger in an artificial, protein-free medium than in diluted plasma, corresponding to about 85% protein binding. Doxepin is a psychotropic agent with tricyclic antidepressant and anxiolytic properties. Doxepin is a tricyclic antidepressant formulated as a mixture of E-(trans) and Z-(cis) stereoisomers. Doxepin is a particularly effective H1-antihistamine in vitro. [1] The equilibrium dissociation constants (KDS) for doxepin at the human histamine H1 receptor and alpha-1 receptor is 0.24 and 24 nM, respectively.[2] Doxepin is well absorbed after oral administration and measurable amounts of doxepin and demethyl doxepin quickly appear in the blood. [3] In addition, doxepin also inhibits CYP2D6 activity in vivo.[4]

Protocols

In vivo: Doxepin hydrochloride is dissolved in water.[3]

References

[1] Lingjaerde O, et al. Effect of doxepin on uptake and efflux of serotonin human blood patelets in vitro. Psychopharmacologia. 1976, 47(2): 183-186.
[2] Richelson E, et al. Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro. J Pharmacol Exp Ther. 1984, 230(1): 94-102. 閵嗏偓閵嗏偓
[3] Hobbs DC, et al. Distribution and metabolism of doxepin. Biochem Pharmacol. 1969, 18(8): 1941-1954. 閵嗏偓閵嗏偓
[4] Szewczuk-Bogus?awska M, et al. Doxepin inhibits CYP2D6 activity in vivo. Pol J Pharmacol. 2004, 56(4): 491-494. 閵嗏偓閵嗏偓

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