(N-Methyl-[11C])pyrilamine,a radiotracer for histamine H-1 receptors: Radiochemical synthesis and biodistribution study in mice |
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| Institution: | 1. Pharmaceutical Analysis Research Center, Tabriz University of Medical Sciences, Tabriz, Iran;2. Student Research Committee, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran;3. Infectious and Tropical Diseases Research Center, Tabriz University of Medical Sciences, Tabriz, Iran;4. Faculty of Pharmacy, Near East University, PO BOX: 99138 Nicosia, North Cyprus, Mersin 10, Turkey |
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| Abstract: | The histamine H-1 receptor antagonist, pyrilamine (N-((4-methoxyphenyl)methyl)-N′,N′-dimethyl-N-2-pyridinyl-1,2-ethanediamine) 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/μmol (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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