(N-Methyl-[11C])pyrilamine, a radiotracer for histamine H-1 receptors: Radiochemical synthesis and biodistribution study in mice

Kazuhiko Yanai; Robert F. Dannals; Alan A. Wilson; Hayden T. Ravert; Ursula Scheffel; Shuji Tanada; Henry N. Wagner

doi:10.1016/0883-2897(88)90050-5

(N-Methyl-[¹¹C])pyrilamine, a radiotracer for histamine H-1 receptors: Radiochemical synthesis and biodistribution study in mice

Kazuhiko Yanai, Robert F. Dannals, Alan A. Wilson, Hayden T. Ravert, Ursula Scheffel, Shuji Tanada, Henry N. Wagner

School of Medicine

Research output: Contribution to journal › Article › peer-review

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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.

Original language	English (US)
Pages (from-to)	605-610
Number of pages	6
Journal	International Journal of Radiation Applications and Instrumentation.
Volume	15
Issue number	6
DOIs	https://doi.org/10.1016/0883-2897(88)90050-5
State	Published - 1988

ASJC Scopus subject areas

General Medicine

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10.1016/0883-2897(88)90050-5

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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-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.",

author = "Kazuhiko Yanai and Dannals, {Robert F.} and Wilson, {Alan A.} and Ravert, {Hayden T.} and Ursula Scheffel and Shuji Tanada and Wagner, {Henry N.}",

year = "1988",

doi = "10.1016/0883-2897(88)90050-5",

language = "English (US)",

volume = "15",

pages = "605--610",

journal = "International Journal of Radiation Applications and Instrumentation.",

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T1 - (N-Methyl-[11C])pyrilamine, a radiotracer for histamine H-1 receptors

T2 - Radiochemical synthesis and biodistribution study in mice

AU - Yanai, Kazuhiko

AU - Dannals, Robert F.

AU - Wilson, Alan A.

AU - Ravert, Hayden T.

AU - Scheffel, Ursula

AU - Tanada, Shuji

AU - Wagner, Henry N.

PY - 1988

Y1 - 1988

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AB - 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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(N-Methyl-[¹¹C])pyrilamine, a radiotracer for histamine H-1 receptors: Radiochemical synthesis and biodistribution study in mice

Abstract

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