Histamine H1 receptors in human brain labelled with [3H]Doxepin

@article{Kanba1984HistamineHR,
  title={Histamine H1 receptors in human brain labelled with [3H]Doxepin},
  author={Shigenobu Kanba and Elliott Richelson},
  journal={Brain Research},
  year={1984},
  volume={304},
  pages={1-7}
}
Doxepin, a tricyclic antidepressant, is one of the most potent histamine H1 antagonists. Therefore, the binding of [3H]doxepin to human brain membranes was examined. Scatchard analysis revealed two distinct binding sites. The high-affinity binding site with a dissociation constant (KD +/- S.E.M.) of 3.1 +/- 0.3 X 10(-10) M was pharmacologically identified as histamine H1 receptors. Dissociation curves at low concentrations of [3H]doxepin were biphasic, suggesting several possibilities about the… 
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The histaminergic ligands for the histamine H(1), H(2) and H(3) receptors, which are currently used as tools in pharmacological studies, are described and the use of all these compounds as a tool in pharmacology is discussed.
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From the in vitro data, it is expected that adinazolam, bupropion, fluoxetine, sertraline, tomoxetines, and venlafaxine not to block any of these five receptors in vivo, which can provide guidelines for the clinician in the choice of antidepressant.
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