Synthesis of radiofluorinated analogs of m-tyrosine as potential l-dopa tracers via direct reaction with acetylhypofluorite
The direct electrophilic radiofluorination of m-tyrosine using [ 18F]acetylhypofluorite was investigated. Results showed that this reaction was both rapid and efficient with recovered decay corrected yield of 71% radiofluorinated m-tyrosines based on starting [ 18F]acetylhypofluorite. Specific activ...
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| Veröffentlicht in: | Applied radiation and isotopes 1990, Vol.41 (5), p.433-437 |
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| container_title | Applied radiation and isotopes |
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| creator | DeJesus, Onofre T. Sunderland, John J. Nickles, J.Robert Mukherjee, Jogeshwar Appelman, Evan H. |
| description | The direct electrophilic radiofluorination of
m-tyrosine using [
18F]acetylhypofluorite was investigated. Results showed that this reaction was both rapid and efficient with recovered decay corrected yield of 71% radiofluorinated
m-tyrosines based on starting [
18F]acetylhypofluorite. Specific activity of the product obtained in this study was 100–200 mCi/mmol although 1–5 Ci/mmol are easily achievable with our improved production of [
18F]AcOF. Three positional isomers were found and identified by
19F-NMR to be 2-, 4-, 6-fluoro-
m-tyrosine with a distribution of 36:11:52, respectively. This measured distribution allowed the assignment of the radio-HPLC peaks. Biological studies are currently underway in our laboratory using these fluoro-
m-tyrosines to determine which isomer would be most suited for the evaluation of the dopamine system by positron tomography. |
| doi_str_mv | 10.1016/0883-2889(90)90001-W |
| format | Article |
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m-tyrosine using [
18F]acetylhypofluorite was investigated. Results showed that this reaction was both rapid and efficient with recovered decay corrected yield of 71% radiofluorinated
m-tyrosines based on starting [
18F]acetylhypofluorite. Specific activity of the product obtained in this study was 100–200 mCi/mmol although 1–5 Ci/mmol are easily achievable with our improved production of [
18F]AcOF. Three positional isomers were found and identified by
19F-NMR to be 2-, 4-, 6-fluoro-
m-tyrosine with a distribution of 36:11:52, respectively. This measured distribution allowed the assignment of the radio-HPLC peaks. Biological studies are currently underway in our laboratory using these fluoro-
m-tyrosines to determine which isomer would be most suited for the evaluation of the dopamine system by positron tomography.</description><identifier>ISSN: 0883-2889</identifier><identifier>ISSN: 0969-8043</identifier><identifier>EISSN: 1872-9800</identifier><identifier>DOI: 10.1016/0883-2889(90)90001-W</identifier><identifier>PMID: 2166010</identifier><language>eng</language><publisher>Oxford: Elsevier B.V</publisher><subject>Biological and medical sciences ; Brain - diagnostic imaging ; Catecholaminergic system ; Fluorine Radioisotopes ; Humans ; Isotope Labeling - methods ; Levodopa - analysis ; Medical sciences ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pharmacology. Drug treatments ; Tomography, Emission-Computed ; Tyrosine - analogs & derivatives</subject><ispartof>Applied radiation and isotopes, 1990, Vol.41 (5), p.433-437</ispartof><rights>1990</rights><rights>1991 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c387t-acd4779af4d2f510f5c8fa88b24781d8e19ea5d1d0cecad2640c330d4a2e7db43</citedby><cites>FETCH-LOGICAL-c387t-acd4779af4d2f510f5c8fa88b24781d8e19ea5d1d0cecad2640c330d4a2e7db43</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,4024,27923,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=19899948$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2166010$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>DeJesus, Onofre T.</creatorcontrib><creatorcontrib>Sunderland, John J.</creatorcontrib><creatorcontrib>Nickles, J.Robert</creatorcontrib><creatorcontrib>Mukherjee, Jogeshwar</creatorcontrib><creatorcontrib>Appelman, Evan H.</creatorcontrib><title>Synthesis of radiofluorinated analogs of m-tyrosine as potential l-dopa tracers via direct reaction with acetylhypofluorite</title><title>Applied radiation and isotopes</title><addtitle>Int J Rad Appl Instrum A</addtitle><description>The direct electrophilic radiofluorination of
m-tyrosine using [
18F]acetylhypofluorite was investigated. Results showed that this reaction was both rapid and efficient with recovered decay corrected yield of 71% radiofluorinated
m-tyrosines based on starting [
18F]acetylhypofluorite. Specific activity of the product obtained in this study was 100–200 mCi/mmol although 1–5 Ci/mmol are easily achievable with our improved production of [
18F]AcOF. Three positional isomers were found and identified by
19F-NMR to be 2-, 4-, 6-fluoro-
m-tyrosine with a distribution of 36:11:52, respectively. This measured distribution allowed the assignment of the radio-HPLC peaks. Biological studies are currently underway in our laboratory using these fluoro-
m-tyrosines to determine which isomer would be most suited for the evaluation of the dopamine system by positron tomography.</description><subject>Biological and medical sciences</subject><subject>Brain - diagnostic imaging</subject><subject>Catecholaminergic system</subject><subject>Fluorine Radioisotopes</subject><subject>Humans</subject><subject>Isotope Labeling - methods</subject><subject>Levodopa - analysis</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pharmacology. Drug treatments</subject><subject>Tomography, Emission-Computed</subject><subject>Tyrosine - analogs & derivatives</subject><issn>0883-2889</issn><issn>0969-8043</issn><issn>1872-9800</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1990</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMGKFDEQhoMo6-zqGyjkouihtZLumU4ugiyuCgseVPYYapKKE-lJ2iSz0vjy9uw0681TDv9Xf6U-xp4JeCNAbN6CUm0jldKvNLzWACCamwdsJVQvG60AHrLVPfKYnZfyE0BK3cszdibFZgMCVuzP1ynWHZVQePI8owvJD4eUQ8RKjmPEIf24y_ZNnXIqIRLHwsdUKdaAAx8al0bkNaOlXPhtQO5CJlt5JrQ1pMh_h7rjc1ynYTeNy4JKT9gjj0Ohp8t7wb5fffh2-am5_vLx8-X768a2qq8NWtf1vUbfOenXAvzaKo9KbWXXK-EUCU24dsKBJYtObjqwbQuuQ0m923btBXt56h1z-nWgUs0-FEvDgJHSoZheaylBtjPYnUA7H1oyeTPmsMc8GQHm6NwchZqjUKPB3Dk3N_PY86X_sN2Tux9aJM_5iyXHYnHwGaMN5V-3VlrrTs3cuxNHs4zbQNkUGyhaOvk0LoX_f-Qv5-ahkQ</recordid><startdate>1990</startdate><enddate>1990</enddate><creator>DeJesus, Onofre T.</creator><creator>Sunderland, John J.</creator><creator>Nickles, J.Robert</creator><creator>Mukherjee, Jogeshwar</creator><creator>Appelman, Evan H.</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>1990</creationdate><title>Synthesis of radiofluorinated analogs of m-tyrosine as potential l-dopa tracers via direct reaction with acetylhypofluorite</title><author>DeJesus, Onofre T. ; Sunderland, John J. ; Nickles, J.Robert ; Mukherjee, Jogeshwar ; Appelman, Evan H.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c387t-acd4779af4d2f510f5c8fa88b24781d8e19ea5d1d0cecad2640c330d4a2e7db43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1990</creationdate><topic>Biological and medical sciences</topic><topic>Brain - diagnostic imaging</topic><topic>Catecholaminergic system</topic><topic>Fluorine Radioisotopes</topic><topic>Humans</topic><topic>Isotope Labeling - methods</topic><topic>Levodopa - analysis</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pharmacology. Drug treatments</topic><topic>Tomography, Emission-Computed</topic><topic>Tyrosine - analogs & derivatives</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>DeJesus, Onofre T.</creatorcontrib><creatorcontrib>Sunderland, John J.</creatorcontrib><creatorcontrib>Nickles, J.Robert</creatorcontrib><creatorcontrib>Mukherjee, Jogeshwar</creatorcontrib><creatorcontrib>Appelman, Evan H.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Applied radiation and isotopes</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>DeJesus, Onofre T.</au><au>Sunderland, John J.</au><au>Nickles, J.Robert</au><au>Mukherjee, Jogeshwar</au><au>Appelman, Evan H.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of radiofluorinated analogs of m-tyrosine as potential l-dopa tracers via direct reaction with acetylhypofluorite</atitle><jtitle>Applied radiation and isotopes</jtitle><addtitle>Int J Rad Appl Instrum A</addtitle><date>1990</date><risdate>1990</risdate><volume>41</volume><issue>5</issue><spage>433</spage><epage>437</epage><pages>433-437</pages><issn>0883-2889</issn><issn>0969-8043</issn><eissn>1872-9800</eissn><abstract>The direct electrophilic radiofluorination of
m-tyrosine using [
18F]acetylhypofluorite was investigated. Results showed that this reaction was both rapid and efficient with recovered decay corrected yield of 71% radiofluorinated
m-tyrosines based on starting [
18F]acetylhypofluorite. Specific activity of the product obtained in this study was 100–200 mCi/mmol although 1–5 Ci/mmol are easily achievable with our improved production of [
18F]AcOF. Three positional isomers were found and identified by
19F-NMR to be 2-, 4-, 6-fluoro-
m-tyrosine with a distribution of 36:11:52, respectively. This measured distribution allowed the assignment of the radio-HPLC peaks. Biological studies are currently underway in our laboratory using these fluoro-
m-tyrosines to determine which isomer would be most suited for the evaluation of the dopamine system by positron tomography.</abstract><cop>Oxford</cop><pub>Elsevier B.V</pub><pmid>2166010</pmid><doi>10.1016/0883-2889(90)90001-W</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0883-2889 |
| ispartof | Applied radiation and isotopes, 1990, Vol.41 (5), p.433-437 |
| issn | 0883-2889 0969-8043 1872-9800 |
| language | eng |
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| source | MEDLINE; Alma/SFX Local Collection |
| subjects | Biological and medical sciences Brain - diagnostic imaging Catecholaminergic system Fluorine Radioisotopes Humans Isotope Labeling - methods Levodopa - analysis Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Tomography, Emission-Computed Tyrosine - analogs & derivatives |
| title | Synthesis of radiofluorinated analogs of m-tyrosine as potential l-dopa tracers via direct reaction with acetylhypofluorite |
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