The histamine H-1 receptor antagonist, pyrilamine (N-((4-methoxyphenyl)methyl)-N',N'-dimethyl-N-2-pyridinyl-1,2-ethaned i ami ne) was labeled with carbon-11 by N-alkylation of desmethylpyrilamine with [11C]iodomethane, and purified by preparative high performance liquid chromatography. The chemically and radiochemically pure labeled pyrilamine was obtained with specific activity of approximately 2500 mCi/mumol (EOS). In vivo distribution studies in mice suggest that the distribution of this compound parallels the known histamine H-1 receptor density in the brain.
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