| Synthesis of high specific activity [75Br]- and [77Br]bromperidol and tissue distribution studies in the rat. | |
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MedLine Citation:
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PMID: 4032434 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A rapid synthesis of [75Br]- and [77Br]bromperidol with specific activity exceeding 10000 Ci/mmol is described in which a trimethylstannylated analogue of bromperidol is used as a substrate for regiospecific no-carrier-added radiobromination. 4-[4-[4-(Trimethylstannyl)phenyl]-4-hydroxypiperidino]-4'- fluorobutyrophenone was synthesized by the reaction of (trimethylstannyl)sodium with haloperidol and purified by preparative HPLC. Subsequent radiobromination with no-carrier-added 75Br- or 77Br- and in situ oxidation using H2O2/CH3COOH gave a corrected radiochemical yield of 35% with a 30-min preparation time. Tissue distribution studies in the rat show a rapid and prolonged uptake into the brain, liver, and kidneys and consistently low blood concentrations that differ quantitatively from previous studies using relatively low specific activity bromperidol. Potential clinical applications for this high specific activity radiobrominated neuroleptic are discussed. |
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Authors:
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S M Moerlein; G L Stöcklin |
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Publication Detail:
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Type: Journal Article; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 28 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 1985 Sep |
Date Detail:
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Created Date: 1985-10-17 Completed Date: 1985-10-17 Revised Date: 2008-11-21 |
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: 1319-24 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 / metabolism Bromine* Chemical Phenomena Chemistry Female Haloperidol / analogs & derivatives*, chemical synthesis, metabolism Isotope Labeling / methods* Kidney / metabolism Kinetics Liver / metabolism Lung / metabolism Radioisotopes* Rats Rats, Inbred Strains Tissue Distribution Trimethyltin Compounds |
| Grant Support | |
ID/Acronym/Agency:
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1-F-32-NS-07047-2/NS/NINDS NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Radioisotopes; 0/Trimethyltin Compounds; 10457-90-6/bromperidol; 1631-73-8/trimethyltin; 52-86-8/Haloperidol; 7726-95-6/Bromine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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