Document Detail

No-carrier-added 3-(2'-[18F]fluoroethyl)spiperone, a new dopamine receptor-binding tracer for positron emission tomography.
MedLine Citation:
PMID:  3494003     Owner:  NLM     Status:  MEDLINE    
No-carrier-added (NCA)3-(2'-[18F]fluoroethyl)spiperone (5), a new dopamine receptor-binding radiopharmaceutical for positron emission tomography, was synthesized by two different methods. Alkylation of the amide nitrogen in spiperone by NCA [18F]fluorobromoethane in the presence of a strong base gave 5 (Method A). Experimental methods were also developed for the syntheses of functional 3-N-alkylderivatives of spiperone such as 3-(2'-bromoethyl)- or 3-(2'-methylsulfonyloxyethyl)spiperone (4a and 4b, respectively). These derivatives (4) reacted with NCA Ag18F, Cs18F or K18F/Kryptofix 222 in acetonitrile or DMSO to give 5 (Method B). Method B, using K18F/Kryptofix 222 in acetonitrile provided 5 in multimillicure amounts (30-40% isolated radiochemical yield) with a specific activity of 2-10/mumol (EOS) in less than 60 min. This one-step, one-pot synthesis is simple, and the high radiochemical yield of 5, as well as the 110 min half-life of 18F, permit multiple tomographic studies a day with one preparation. Tomographic results in monkey brain with 5 are consistent with the labeling of dopamine-D2 receptor systems.
N Satyamurthy; G T Bida; J R Barrio; A Luxen; J C Mazziotta; S C Huang; M E Phelps
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology     Volume:  13     ISSN:  0883-2897     ISO Abbreviation:  Int J Rad Appl Instrum B     Publication Date:  1986  
Date Detail:
Created Date:  1987-04-30     Completed Date:  1987-04-30     Revised Date:  2008-02-21    
Medline Journal Info:
Nlm Unique ID:  8611098     Medline TA:  Int J Rad Appl Instrum B     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  617-24     Citation Subset:  IM    
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MeSH Terms
Brain / radionuclide imaging
Macaca nemestrina
Receptors, Dopamine / metabolism*
Spiperone / analogs & derivatives*,  chemical synthesis,  diagnostic use,  metabolism
Tomography, Emission-Computed* / methods
Grant Support
Reg. No./Substance:
0/Receptors, Dopamine; 106114-42-5/3-N-(2-fluoroethyl)spiperone; 749-02-0/Spiperone

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