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Evaluation of in vivo selective binding of [11C]doxepin to histamine H1receptors in five animal species

Authors
Publisher
Elsevier Inc.
Publication Date
Volume
31
Issue
4
Identifiers
DOI: 10.1016/j.nucmedbio.2003.11.005
Keywords
  • [11C]Doxepin
  • Histamine H1Receptor
  • Positron Emission Tomography
Disciplines
  • Medicine

Abstract

Abstract The specific binding of [ 11C]doxepin, which has been used as a radioligand for mapping histamine H 1 receptors in human brain by positron emission tomography, was evaluated in five animal species. In mice the [ 11C]doxepin uptake was reduced by treatment with cold doxepin and two H 1 receptor antagonists, but not with H 2/H 3 antagonists. The specific binding evaluated with treatment with (+)-chlorpheniramine (H 1 antagonist) was in the range of 10–30% in mouse, rat, rabbit, and monkey, but was not detected in guinea pig.

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