Labeling of histamine H1-receptors in vivo: A compartment model analysis and positron emission tomographic imaging

K. Yanai, T. Watanabe, M. Itoh, J. Hatazawa, R. Iwata, T. Ido

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)

Abstract

Binding of [3H]-pyrilamine to guinea-pig brain in vivo was studied and analyzed kinetically on the basis of a four-compartment model to establish the method of analysis for the in vivo binding. The pharmacological properties of the [3H]-pyrilamine binding in vivo were similar to those of the in vitro binding to brain homogenate. The distribution of histamine H1-receptors in dog brain, which was obtained by positron emission tomography (PET) with [11C]pyrilamine or doxepin as a tracer, was in good correlation to that obtained by the in vitro binding method. We finally applied this in vivo binding method to a living healthy human to reveal the distribution of H1-receptor in the brain.

Original languageEnglish
Pages (from-to)381-386
Number of pages6
JournalAgents and Actions
Volume33
Issue numberSUPPL.
DOIs
Publication statusPublished - 1991

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology (medical)

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