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}
}
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80 Citations
Background Citations
9
Methods Citations
1
Results Citations
1

80 Citations

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Affinity of neuroleptics for D1 receptor of human brain striatum.

We determined the inhibition-dissociation constant (Ki) of a number of neuroleptics for D1 receptors of normal human brain tissue using [3H]SCH23390…

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References

SHOWING 1-10 OF 18 REFERENCES

[3H]doxepin interactions with histamine H1-receptors and other sites in guinea pig and rat brain homogenates.

High-affinity binding of [3H]doxepin to histamine H1-receptors in rat brain: possible identification of a subclass of histamine H1-receptors.

High affinity binding of tricyclic antidepressants to histamine H1-receptors: fact and artifact.

THE BINDING OF [3H]MEPYRAMINE TO HISTAMINE H1 RECEPTORS IN GUINEA‐PIG BRAIN

The distribution of histamine H1 receptors, defined by the promethazine‐sensitive binding of [3H]mepyramine, in 11 different brain regions was uneven with the largest amounts in cerebellum, superior and inferior colliculus and hypothalamus and the smallest in caudate nucleus, brain stem and spinal cord.

HETEROGENEITY OF HISTAMINE Hi‐RECEPTORS: SPECIES VARIATIONS IN [3H]MEPYRAMINE BINDING OF BRAIN MEMBRANES

The tricyclic antidepressant doxepin and the neuroleptic clozapine are the most potent of all drugs examined in competing for [3H]mepyramine binding, exceeding in potency any H1 antihistamines examined.

Interaction between mianserin, an antidepressant drug, and central H1- and H2-histamine-receptors: In vitro and in vivo studies and radioreceptor assay

Tricyclic antidepressants block histamine H1 receptors of mouse neuroblastoma cells

It is shown that these drugs are potent competitive inhibitors of histamine H1 receptors and that some of these compounds are amongst the most potent H1 antagonists known.

Tricyclic antidepressants and histamine H1 receptors.

Doxepin hydro chloride and amitriptyline hydrochloride may be the most potent antihistamines known, and the antihistaminic potencies of these and the other tricyclic antidepressant drugs may relate directly to their ability to cause sedation and drowsiness in patients.

Tricyclic antidepressants: potent blockade of histamine H1 receptors of guinea pig ileum.

Antidepressants are weak competitive antagonists of histamine H2 receptors in dissociated brain tissue.