(N-methyl-[11C])pyrilamine, a radiotracer for histamine H-1 receptors: radiochemical synthesis and biodistribution study in mice.
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.
Yanai
K
K
Division of Nuclear Medicine and Radiation Health Sciences, Johns Hopkins Medical Institutions, Baltimore, MD 21205-2179.
Dannals
R F
RF
Wilson
A A
AA
Ravert
H T
HT
Scheffel
U
U
Tanada
S
S
Wagner
H N
HN
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
D000631:Aminopyridines; D002250:Carbon Radioisotopes; D011969:Receptors, Histamine H1; D011738:Pyrilamine