Radiolabeled benzoylcholine derivatives as possible myocardial‐imaging agents

Robert F. Dannals; H. Donald Burns; Luigi G. Marzilli; Timothy C. Trageser; Henry N. Wagner

doi:10.1002/jps.2600700425

Radiolabeled benzoylcholine derivatives as possible myocardial‐imaging agents

Robert F. Dannals, H. Donald Burns, Luigi G. Marzilli, Timothy C. Trageser, Henry N. Wagner

School of Medicine

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

5 Scopus citations

Abstract

Two radioiodinated analogs of benzoylcholine were investigated as possible myocardial‐imaging agents. O‐([2‐¹²⁵I]iodobenzoyl)choline and N‐([2‐¹²⁵I]iodobenzoyl)cholamine were prepared by nucleophilic substitution of sodium [¹²⁵I] iodide for stable iodine in O‐(N,N‐dimethylaminoethyl)‐2‐iodobenzoate and N‐(N', N'‐dimethyiaminoethyl)‐2‐iodobenzamide, respectively, and by methylation with methyl iodide. The in vivo distribution of each compound in mice was determined as a function of time. Favorable heart‐to‐blood and heart‐to‐lung ratios were obtained with N‐([2‐¹²⁵I]iodobenzoyl)cholamine.

Original language	English (US)
Pages (from-to)	439-442
Number of pages	4
Journal	Journal of Pharmaceutical Sciences
Volume	70
Issue number	4
DOIs	https://doi.org/10.1002/jps.2600700425
State	Published - Apr 1981

Keywords

Benzoylcholine, radioiodinated analogs—synthesized and evaluated as possible myocardial‐imaging agents, biodistribution studies in mice
Biodistribution—radioiodinated benzoylcholine analogs synthesized and evaluated for use as myocardial‐imaging agents, mice
Radionuclide imaging, myocardial—radioiodinated benzoylcholine analogs synthesized and evaluated for use as myocardial‐imaging agents, mice
Radiopharmaceuticals, iodinated—benzoylcholine analogs, synthesis and evaluation for use as myocardial‐imaging agents, mice

ASJC Scopus subject areas

Pharmaceutical Science

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10.1002/jps.2600700425

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title = "Radiolabeled benzoylcholine derivatives as possible myocardial‐imaging agents",

abstract = "Two radioiodinated analogs of benzoylcholine were investigated as possible myocardial‐imaging agents. O‐([2‐125I]iodobenzoyl)choline and N‐([2‐125I]iodobenzoyl)cholamine were prepared by nucleophilic substitution of sodium [125I] iodide for stable iodine in O‐(N,N‐dimethylaminoethyl)‐2‐iodobenzoate and N‐(N', N'‐dimethyiaminoethyl)‐2‐iodobenzamide, respectively, and by methylation with methyl iodide. The in vivo distribution of each compound in mice was determined as a function of time. Favorable heart‐to‐blood and heart‐to‐lung ratios were obtained with N‐([2‐125I]iodobenzoyl)cholamine.",

keywords = "Benzoylcholine, radioiodinated analogs—synthesized and evaluated as possible myocardial‐imaging agents, biodistribution studies in mice, Biodistribution—radioiodinated benzoylcholine analogs synthesized and evaluated for use as myocardial‐imaging agents, mice, Radionuclide imaging, myocardial—radioiodinated benzoylcholine analogs synthesized and evaluated for use as myocardial‐imaging agents, mice, Radiopharmaceuticals, iodinated—benzoylcholine analogs, synthesis and evaluation for use as myocardial‐imaging agents, mice",

author = "Dannals, {Robert F.} and {Donald Burns}, H. and Marzilli, {Luigi G.} and Trageser, {Timothy C.} and Wagner, {Henry N.}",

year = "1981",

month = apr,

doi = "10.1002/jps.2600700425",

language = "English (US)",

volume = "70",

pages = "439--442",

journal = "Journal of Pharmaceutical Sciences",

issn = "0022-3549",

publisher = "John Wiley and Sons Inc.",

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}

TY - JOUR

T1 - Radiolabeled benzoylcholine derivatives as possible myocardial‐imaging agents

AU - Dannals, Robert F.

AU - Donald Burns, H.

AU - Marzilli, Luigi G.

AU - Trageser, Timothy C.

AU - Wagner, Henry N.

PY - 1981/4

Y1 - 1981/4

N2 - Two radioiodinated analogs of benzoylcholine were investigated as possible myocardial‐imaging agents. O‐([2‐125I]iodobenzoyl)choline and N‐([2‐125I]iodobenzoyl)cholamine were prepared by nucleophilic substitution of sodium [125I] iodide for stable iodine in O‐(N,N‐dimethylaminoethyl)‐2‐iodobenzoate and N‐(N', N'‐dimethyiaminoethyl)‐2‐iodobenzamide, respectively, and by methylation with methyl iodide. The in vivo distribution of each compound in mice was determined as a function of time. Favorable heart‐to‐blood and heart‐to‐lung ratios were obtained with N‐([2‐125I]iodobenzoyl)cholamine.

AB - Two radioiodinated analogs of benzoylcholine were investigated as possible myocardial‐imaging agents. O‐([2‐125I]iodobenzoyl)choline and N‐([2‐125I]iodobenzoyl)cholamine were prepared by nucleophilic substitution of sodium [125I] iodide for stable iodine in O‐(N,N‐dimethylaminoethyl)‐2‐iodobenzoate and N‐(N', N'‐dimethyiaminoethyl)‐2‐iodobenzamide, respectively, and by methylation with methyl iodide. The in vivo distribution of each compound in mice was determined as a function of time. Favorable heart‐to‐blood and heart‐to‐lung ratios were obtained with N‐([2‐125I]iodobenzoyl)cholamine.

KW - Benzoylcholine, radioiodinated analogs—synthesized and evaluated as possible myocardial‐imaging agents, biodistribution studies in mice

KW - Biodistribution—radioiodinated benzoylcholine analogs synthesized and evaluated for use as myocardial‐imaging agents, mice

KW - Radionuclide imaging, myocardial—radioiodinated benzoylcholine analogs synthesized and evaluated for use as myocardial‐imaging agents, mice

KW - Radiopharmaceuticals, iodinated—benzoylcholine analogs, synthesis and evaluation for use as myocardial‐imaging agents, mice

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SN - 0022-3549

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SP - 439

EP - 442

JO - Journal of Pharmaceutical Sciences

JF - Journal of Pharmaceutical Sciences

IS - 4

ER -

Radiolabeled benzoylcholine derivatives as possible myocardial‐imaging agents

Abstract

Keywords

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