| Effect of the prosthetic group on the pharmacologic properties of 18F-labeled rhodamine B, a potential myocardial perfusion agent for positron emission tomography (PET). | |
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MedLine Citation:
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PMID: 23210516 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We recently reported the development of the 2-[(18)F]fluoroethyl ester of rhodamine B as a potential positron emission tomography (PET) tracer for myocardial perfusion imaging. This compound, which was prepared using a [(18)F]fluoroethyl prosthetic group, has significant uptake in the myocardium in rats but also demonstrates relatively high liver uptake and is rapidly hydrolyzed in vivo in mice. We have now prepared (18)F-labeled rhodamine B using three additional prosthetic groups (propyl, diethylene glycol, and triethylene glycol) and found that the prosthetic group has a significant effect on the in vitro and in vivo properties of these compounds. Of the esters prepared to date, the diethylene glycol ester is superior in terms of in vitro stability and pharmacokinetics. These observations suggest that the prosthetic group plays a significant role in determining the pharmacological properties of (18)F-labeled compounds. They also support the value of continued investigation of (18)F-labeled rhodamines as PET radiopharmaceuticals for myocardial perfusion imaging. |
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Authors:
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Mark D Bartholomä; Vijay Gottumukkala; Shaohui Zhang; Amanda Baker; Patricia Dunning; Frederic H Fahey; S Ted Treves; Alan B Packard |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't Date: 2012-12-14 |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 55 ISSN: 1520-4804 ISO Abbreviation: J. Med. Chem. Publication Date: 2012 Dec |
Date Detail:
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Created Date: 2012-12-27 Completed Date: 2013-03-14 Revised Date: 2013-04-16 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: United States |
Other Details:
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Languages: eng Pagination: 11004-12 Citation Subset: IM |
Affiliation:
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Division of Nuclear Medicine and Molecular Imaging, Boston Children's Hospital, Boston, Massachusetts 02115, USA. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Esters Fluorine Radioisotopes Glycols / chemistry Heart / radionuclide imaging* Humans Mice Myocardial Perfusion Imaging* Myocardium / metabolism Positron-Emission Tomography Radiopharmaceuticals / chemical synthesis*, chemistry, pharmacokinetics Rats Rhodamines / chemical synthesis*, chemistry, pharmacokinetics Structure-Activity Relationship Tissue Distribution |
| Grant Support | |
ID/Acronym/Agency:
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1 R01 HL108107-01/HL/NHLBI NIH HHS; R01 HL108107/HL/NHLBI NIH HHS; RR 04648/RR/NCRR NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Esters; 0/Fluorine Radioisotopes; 0/Glycols; 0/Radiopharmaceuticals; 0/Rhodamines; K7G5SCF8IL/rhodamine B |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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