123I-iodobenzoylglucosamines: Glucose analogues for heart imaging

123I-iodobenzoylglucosamines: Glucose analogues for heart imaging

The ortho‐, meta‐ and para‐[123I]‐2‐deoxy‐2‐N‐(iodobenzoyl)‐D‐glucosamine (BGA) derivatives were investigated to determine the effect of iodine position and lipophilicity on tissue distribution. There was no correlation between tissue uptake and lipophilicity. Maximum uptake was observed for o‐BGA d...

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Veröffentlicht in:Journal of labelled compounds & radiopharmaceuticals 1993-04, Vol.33 (4), p.327-344
Hauptverfasser: Lutz, T., Dougan, H., Rihela, T., Vo, C. V., Lyster, D. M.
Format: Artikel
Sprache:eng
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Biological and medical sciences
Contrast media. Radiopharmaceuticals
heart imaging and biodistribution studies
iodobenzoylglucosamine
Medical sciences
Pharmacology. Drug treatments
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container_end_page 344
container_issue 4
container_start_page 327
container_title Journal of labelled compounds & radiopharmaceuticals
container_volume 33
creator Lutz, T.
Dougan, H.
Rihela, T.
Vo, C. V.
Lyster, D. M.
description The ortho‐, meta‐ and para‐[123I]‐2‐deoxy‐2‐N‐(iodobenzoyl)‐D‐glucosamine (BGA) derivatives were investigated to determine the effect of iodine position and lipophilicity on tissue distribution. There was no correlation between tissue uptake and lipophilicity. Maximum uptake was observed for o‐BGA displaying a heart:blood ratio of 36.0 at 18 hours post injection. Yeast hexokinase phosphorylation studies in vitro and an in vivo insulin experiment were carried out on o‐BGA. No phosphorylation was detected, but the insulin study indicated that o‐BGA uses the glucose transporter. o‐BGA showed maximum tissue uptake in mice at an optimal specific activity of 0.004mg/μCi. Mouse biodistribution studies of o‐[123I]‐iodobenzamide(o‐123IBA) indicated that the glucose moiety of o‐BGA may be involved in the heart accumulation process in mice. Heart tissue extraction studies showed unmetabolized o‐[123I]BGA, recorded at 14 hours post injection, showed significant heart uptake.
doi_str_mv 10.1002/jlcr.2580330411
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source Wiley Online Library Journals Frontfile Complete
subjects Biological and medical sciences
Contrast media. Radiopharmaceuticals
heart imaging and biodistribution studies
iodobenzoylglucosamine
Medical sciences
Pharmacology. Drug treatments
title 123I-iodobenzoylglucosamines: Glucose analogues for heart imaging
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