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[sup 123]I-iodobenzoylglucosamines: glucose analogues for heart imaging

Abstract

The ortho-, meta- and para-[[sup 123]I]-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/[mu]Ci. Mouse biodistribution studies of o-[[sup 123]I]-iodobenzamide(o-[sup 123]IBA) 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-[[sup 123]I]BGA was the predominant species. A rabbit image of o-[[sup 123]I]BGA, recorded at 14 hours post injection, showed significant heart uptake. (author).
Authors:
Lutz, T; [1]  Dougan, H; [2]  Rihela, T; Vo, C V; [3]  Lyster, D M [4] 
  1. British Columbia Univ., Vancouver, BC (Canada). Dept. of Pharmaceutical Sciences
  2. TRIUMF, Vancouver, BC (Canada)
  3. Vancouver General Hospital (Canada). Div. of Nuclear Medicine
  4. British Columbia Univ., Vancouver, BC (Canada). Dept. of Pharmaceutical Sciences Vancouver General Hospital (Canada). Div. of Nuclear Medicine
Publication Date:
Jan 01, 1993
Product Type:
Journal Article
Reference Number:
AIX-24-071528; EDB-93-142982
Resource Relation:
Journal Name: Journal of Labelled Compounds and Radiopharmaceuticals; (United Kingdom); Journal Volume: 33:4
Subject:
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY; HEART; RADIOPHARMACEUTICALS; HEXOSAMINES; IODINE 123; STRUCTURE-ACTIVITY RELATIONSHIPS; CHEMICAL PREPARATION; LABELLING; MICE; RABBITS; SCINTISCANNING; TISSUE DISTRIBUTION; AMINES; ANIMALS; BETA DECAY RADIOISOTOPES; BODY; CARBOHYDRATES; CARDIOVASCULAR SYSTEM; COUNTING TECHNIQUES; DIAGNOSTIC TECHNIQUES; DISTRIBUTION; DRUGS; ELECTRON CAPTURE RADIOISOTOPES; HEXOSES; HOURS LIVING RADIOISOTOPES; INTERMEDIATE MASS NUCLEI; IODINE ISOTOPES; ISOTOPES; LABELLED COMPOUNDS; MAMMALS; MONOSACCHARIDES; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANS; RADIOISOTOPE SCANNING; RADIOISOTOPES; RODENTS; SACCHARIDES; SYNTHESIS; VERTEBRATES; 400703* - Radiochemistry & Nuclear Chemistry- Radioisotope Production
OSTI ID:
6077174
Country of Origin:
United Kingdom
Language:
English
Other Identifying Numbers:
Journal ID: ISSN 0362-4803; CODEN: JLCRD4
Submitting Site:
GBN
Size:
Pages: 327-343
Announcement Date:

Citation Formats

Lutz, T, Dougan, H, Rihela, T, Vo, C V, and Lyster, D M. [sup 123]I-iodobenzoylglucosamines: glucose analogues for heart imaging. United Kingdom: N. p., 1993. Web. doi:10.1002/jlcr.2580330411.
Lutz, T, Dougan, H, Rihela, T, Vo, C V, & Lyster, D M. [sup 123]I-iodobenzoylglucosamines: glucose analogues for heart imaging. United Kingdom. doi:10.1002/jlcr.2580330411.
Lutz, T, Dougan, H, Rihela, T, Vo, C V, and Lyster, D M. 1993. "[sup 123]I-iodobenzoylglucosamines: glucose analogues for heart imaging." United Kingdom. doi:10.1002/jlcr.2580330411. https://www.osti.gov/servlets/purl/10.1002/jlcr.2580330411.
@misc{etde_6077174,
title = {[sup 123]I-iodobenzoylglucosamines: glucose analogues for heart imaging}
author = {Lutz, T, Dougan, H, Rihela, T, Vo, C V, and Lyster, D M}
abstractNote = {The ortho-, meta- and para-[[sup 123]I]-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/[mu]Ci. Mouse biodistribution studies of o-[[sup 123]I]-iodobenzamide(o-[sup 123]IBA) 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-[[sup 123]I]BGA was the predominant species. A rabbit image of o-[[sup 123]I]BGA, recorded at 14 hours post injection, showed significant heart uptake. (author).}
doi = {10.1002/jlcr.2580330411}
journal = {Journal of Labelled Compounds and Radiopharmaceuticals; (United Kingdom)}
volume = {33:4}
journal type = {AC}
place = {United Kingdom}
year = {1993}
month = {Jan}
}