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}
}
Studies on Muscarinic Binding Sites in Human Brain Identified with [3H]Pirenzepine
TLDR
Pirenzepine, a potent antimuscarinic agent with apparent selectivity for a subtype of muscarinic receptors, was used in tritiated form to characterize its binding to human brain tissue to indicate a significant correlation for the maximum number of binding sites for the two radioligands in 13 brain regions.
Re-examination of [3H]mepyramine binding assay for histamine H1 receptor using quinine.
Selective ligands as tools to study histamine receptors.
Binding of [3H]Neurotensin in Human Brain: Properties and Distribution
TLDR
The binding of [3H]neurotensin to membranes from human brain at 0°C was specific, saturable, and reversible, and the carboxy‐terminal portion of neurotensin played an important part in the binding of this neuropeptide in human brain, a result described for other species.
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
Binding of antidepressants to human brain receptors: focus on newer generation compounds
TLDR
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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References

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THE BINDING OF [3H]MEPYRAMINE TO HISTAMINE H1 RECEPTORS IN GUINEA‐PIG BRAIN
TLDR
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
TLDR
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.
Tricyclic antidepressants block histamine H1 receptors of mouse neuroblastoma cells
TLDR
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.
TLDR
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.
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