Document Detail


Effect of the prosthetic group on the pharmacologic properties of 18F-labeled rhodamine B, a potential myocardial perfusion agent for positron emission tomography (PET).
MedLine Citation:
PMID:  23210516     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
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:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2012-12-14
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  55     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2012 Dec 
Date Detail:
Created Date:  2012-12-27     Completed Date:  2013-03-14     Revised Date:  2014-01-09    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  11004-12     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
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:
1 R01 HL108107-01/HL/NHLBI NIH HHS; R01 HL108107/HL/NHLBI NIH HHS; RR 04648/RR/NCRR NIH HHS
Chemical
Reg. No./Substance:
0/Esters; 0/Fluorine Radioisotopes; 0/Glycols; 0/Radiopharmaceuticals; 0/Rhodamines; K7G5SCF8IL/rhodamine B
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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