Doxepin is a tricyclic antidepressant that targets various receptors in the brain, including serotonin receptors (5-HT2A, 5-HT2C, 5-HT3), histamine receptors (H1), and adrenergic receptors (α1, α2). The dissociation constant (KI) and half-maximal inhibitory concentration (IC50) of doxepin to its targets are as follows:

  • 5-HT2A receptor: KI = 1.5 nM; IC50 = 4.2 nM
  • 5-HT2C receptor: KI = 1.1 nM; IC50 = 10 nM
  • 5-HT3 receptor: KI = 11 nM; IC50 = 30 nM
  • H1 receptor: KI = 4 nM; IC50 = 3.6 nM
  • α1 receptor: KI = 7.6 nM; IC50 = 9.4 nM
  • α2 receptor: KI = 35 nM; IC50 = 18 nM

Note that these values may vary depending on the assay, cell line, and experimental conditions used

what is the KI and IC50 of doxepin to its targets

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