title: (N-methyl-[11C])pyrilamine, a radiotracer for histamine H-1 receptors: radiochemical synthesis and biodistribution study in mice.
abstract: 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.
authors.affiliation: Division of Nuclear Medicine and Radiation Health Sciences, Johns Hopkins Medical Institutions, Baltimore, MD 21205-2179.
authors.forename: K
authors.initials: K
authors.lastname: Yanai
authors.forename: R F
authors.initials: RF
authors.lastname: Dannals
authors.forename: A A
authors.initials: AA
authors.lastname: Wilson
authors.forename: H T
authors.initials: HT
authors.lastname: Ravert
authors.forename: U
authors.initials: U
authors.lastname: Scheffel
authors.forename: S
authors.initials: S
authors.lastname: Tanada
authors.forename: H N
authors.initials: HN
authors.lastname: Wagner
mesh_terms: D000631:Aminopyridines; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D001923:Brain Chemistry; D002250:Carbon Radioisotopes; D007553:Isotope Labeling; D008297:Male; D051379:Mice; D011738:Pyrilamine / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D011969:Receptors, Histamine H1 / Q000032:analysis*; D014018:Tissue Distribution
chemical_list: D000631:Aminopyridines; D002250:Carbon Radioisotopes; D011969:Receptors, Histamine H1; D011738:Pyrilamine