| No-carrier-added 3-(2'-[18F]fluoroethyl)spiperone, a new dopamine receptor-binding tracer for positron emission tomography. | |
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MedLine Citation:
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PMID: 3494003 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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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:
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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:
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Created Date: 1987-04-30 Completed Date: 1987-04-30 Revised Date: 2008-02-21 |
Medline Journal Info:
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Nlm Unique ID: 8611098 Medline TA: Int J Rad Appl Instrum B Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 617-24 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Brain / radionuclide imaging Kinetics Macaca nemestrina Receptors, Dopamine / metabolism* Spiperone / analogs & derivatives*, chemical synthesis, diagnostic use, metabolism Tomography, Emission-Computed* / methods |
| Grant Support | |
ID/Acronym/Agency:
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P01-NS-15654/NS/NINDS NIH HHS; R01-MH-37916/MH/NIMH NIH HHS; R01-NS-20867/NS/NINDS NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Receptors, Dopamine; 106114-42-5/3-N-(2-fluoroethyl)spiperone; 749-02-0/Spiperone |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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