Abstract
The specific binding of [(11)C]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 [(11)C]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.
Publication types
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Comparative Study
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Evaluation Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Brain / diagnostic imaging*
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Brain / drug effects
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Brain / metabolism*
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Carbon Radioisotopes / pharmacokinetics
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Doxepin / pharmacokinetics*
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Guinea Pigs
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Histamine Agonists / pharmacology
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Humans
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Macaca mulatta
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Male
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Metabolic Clearance Rate
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Mice
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Protein Binding
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Rabbits
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Radiopharmaceuticals / pharmacokinetics
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Rats
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Rats, Wistar
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Receptors, Histamine H1 / metabolism*
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Species Specificity
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Tissue Distribution
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Tomography, Emission-Computed / methods
Substances
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Carbon Radioisotopes
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Histamine Agonists
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Radiopharmaceuticals
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Receptors, Histamine H1
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Doxepin