Preparation of the hypoxia imaging PET tracer [ 18F]FAZA: reaction parameters and automation
18F-labeling of the nitroimidazole nucleoside analogue 1-(5-fluoro-5-deoxy- α- D-arabinofuranosyl)-2-nitroimidazole (FAZA) was developed to use this tracer in PET for detection of hypoxia. Parameters for labeling and hydrolysis were optimized with regard to amount of precursor, temperature and time....
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| Veröffentlicht in: | Applied radiation and isotopes 2005-06, Vol.62 (6), p.897-901 |
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| container_title | Applied radiation and isotopes |
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| creator | Reischl, G. Ehrlichmann, W. Bieg, C. Solbach, C. Kumar, P. Wiebe, L.I. Machulla, H.-J. |
| description | 18F-labeling of the nitroimidazole nucleoside analogue 1-(5-fluoro-5-deoxy-
α-
D-arabinofuranosyl)-2-nitroimidazole (FAZA) was developed to use this tracer in PET for detection of hypoxia. Parameters for labeling and hydrolysis were optimized with regard to amount of precursor, temperature and time. Labeling yields reached a maximum of 62±4% at 100
°C within 5
min using 5
mg of precursor. Hydrolysis was best performed with 1
mL of 0.1
N NaOH at 20
°C for 2
min. Transfer of these conditions to an automated synthesizer resulted in an overall radiochemical yield of 20.7±3.5%. Absolute yields at EOS were 9.8±2.3
GBq of [
18F]FAZA ready for injection (
n=21; 50
min after EOB; irradiation parameters: 35
μA, 60
min). Thus, a convenient approach suitable for large-scale production of [
18F]FAZA was developed by an automated process. |
| doi_str_mv | 10.1016/j.apradiso.2004.12.004 |
| format | Article |
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α-
D-arabinofuranosyl)-2-nitroimidazole (FAZA) was developed to use this tracer in PET for detection of hypoxia. Parameters for labeling and hydrolysis were optimized with regard to amount of precursor, temperature and time. Labeling yields reached a maximum of 62±4% at 100
°C within 5
min using 5
mg of precursor. Hydrolysis was best performed with 1
mL of 0.1
N NaOH at 20
°C for 2
min. Transfer of these conditions to an automated synthesizer resulted in an overall radiochemical yield of 20.7±3.5%. Absolute yields at EOS were 9.8±2.3
GBq of [
18F]FAZA ready for injection (
n=21; 50
min after EOB; irradiation parameters: 35
μA, 60
min). Thus, a convenient approach suitable for large-scale production of [
18F]FAZA was developed by an automated process.</description><identifier>ISSN: 0969-8043</identifier><identifier>EISSN: 1872-9800</identifier><identifier>DOI: 10.1016/j.apradiso.2004.12.004</identifier><identifier>PMID: 15799867</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>[ 18F]FAZA ; Automation ; Cell Hypoxia ; Fluorine Radioisotopes ; Hypoxia ; Nitroimidazole ; Nitroimidazoles - chemistry ; Positron emission tomography ; Radioisotopes - chemistry</subject><ispartof>Applied radiation and isotopes, 2005-06, Vol.62 (6), p.897-901</ispartof><rights>2005 Elsevier Ltd</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c463t-5c6df9cc6d1c337c0c9a23540290f23668e33ee6ff5473be355eedf27d9d235e3</citedby><cites>FETCH-LOGICAL-c463t-5c6df9cc6d1c337c0c9a23540290f23668e33ee6ff5473be355eedf27d9d235e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.apradiso.2004.12.004$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15799867$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Reischl, G.</creatorcontrib><creatorcontrib>Ehrlichmann, W.</creatorcontrib><creatorcontrib>Bieg, C.</creatorcontrib><creatorcontrib>Solbach, C.</creatorcontrib><creatorcontrib>Kumar, P.</creatorcontrib><creatorcontrib>Wiebe, L.I.</creatorcontrib><creatorcontrib>Machulla, H.-J.</creatorcontrib><title>Preparation of the hypoxia imaging PET tracer [ 18F]FAZA: reaction parameters and automation</title><title>Applied radiation and isotopes</title><addtitle>Appl Radiat Isot</addtitle><description>18F-labeling of the nitroimidazole nucleoside analogue 1-(5-fluoro-5-deoxy-
α-
D-arabinofuranosyl)-2-nitroimidazole (FAZA) was developed to use this tracer in PET for detection of hypoxia. Parameters for labeling and hydrolysis were optimized with regard to amount of precursor, temperature and time. Labeling yields reached a maximum of 62±4% at 100
°C within 5
min using 5
mg of precursor. Hydrolysis was best performed with 1
mL of 0.1
N NaOH at 20
°C for 2
min. Transfer of these conditions to an automated synthesizer resulted in an overall radiochemical yield of 20.7±3.5%. Absolute yields at EOS were 9.8±2.3
GBq of [
18F]FAZA ready for injection (
n=21; 50
min after EOB; irradiation parameters: 35
μA, 60
min). Thus, a convenient approach suitable for large-scale production of [
18F]FAZA was developed by an automated process.</description><subject>[ 18F]FAZA</subject><subject>Automation</subject><subject>Cell Hypoxia</subject><subject>Fluorine Radioisotopes</subject><subject>Hypoxia</subject><subject>Nitroimidazole</subject><subject>Nitroimidazoles - chemistry</subject><subject>Positron emission tomography</subject><subject>Radioisotopes - chemistry</subject><issn>0969-8043</issn><issn>1872-9800</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkT9v2zAUxImiReOk_QoGp2xS-EcixU4xAjspEKAenCVtQTDkk0PDElVSDuJvXzp20THLu-V394A7hKaUlJRQcbUpzRCN8ymUjJCqpKzM8gFNaCNZoRpCPqIJUUIVDan4GTpPaUMy0Sj2GZ3RWirVCDlBv5YRBhPN6EOPQ4vHZ8DP-yG8eoN9Z9a-X-PlfIXHaCxE_BPTZvF7MXucfcMRjH2zHfwdjBATNr3DZjeG7i3wC_rUmm2Crye9QA-L-ermrrj_cfv9ZnZf2ErwsaitcK2y-VLLubTEKsN4XRGmSMu4EA1wDiDatq4kfwJe1wCuZdIplzngF-jymDvE8GcHadSdTxa2W9ND2CUtZC2JqNS7IJVcyEpUGRRH0MaQUoRWDzHXEfeaEn0YQG_0vwH0YQBNmc6SjdPTh91TB-6_7dR4Bq6PAORCXjxEnayH3oLzEeyoXfDv_fgLG16aQA</recordid><startdate>20050601</startdate><enddate>20050601</enddate><creator>Reischl, G.</creator><creator>Ehrlichmann, W.</creator><creator>Bieg, C.</creator><creator>Solbach, C.</creator><creator>Kumar, P.</creator><creator>Wiebe, L.I.</creator><creator>Machulla, H.-J.</creator><general>Elsevier Ltd</general><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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20050601</creationdate><title>Preparation of the hypoxia imaging PET tracer [ 18F]FAZA: reaction parameters and automation</title><author>Reischl, G. ; Ehrlichmann, W. ; Bieg, C. ; Solbach, C. ; Kumar, P. ; Wiebe, L.I. ; Machulla, H.-J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c463t-5c6df9cc6d1c337c0c9a23540290f23668e33ee6ff5473be355eedf27d9d235e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>[ 18F]FAZA</topic><topic>Automation</topic><topic>Cell Hypoxia</topic><topic>Fluorine Radioisotopes</topic><topic>Hypoxia</topic><topic>Nitroimidazole</topic><topic>Nitroimidazoles - chemistry</topic><topic>Positron emission tomography</topic><topic>Radioisotopes - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Reischl, G.</creatorcontrib><creatorcontrib>Ehrlichmann, W.</creatorcontrib><creatorcontrib>Bieg, C.</creatorcontrib><creatorcontrib>Solbach, C.</creatorcontrib><creatorcontrib>Kumar, P.</creatorcontrib><creatorcontrib>Wiebe, L.I.</creatorcontrib><creatorcontrib>Machulla, H.-J.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Applied radiation and isotopes</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Reischl, G.</au><au>Ehrlichmann, W.</au><au>Bieg, C.</au><au>Solbach, C.</au><au>Kumar, P.</au><au>Wiebe, L.I.</au><au>Machulla, H.-J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation of the hypoxia imaging PET tracer [ 18F]FAZA: reaction parameters and automation</atitle><jtitle>Applied radiation and isotopes</jtitle><addtitle>Appl Radiat Isot</addtitle><date>2005-06-01</date><risdate>2005</risdate><volume>62</volume><issue>6</issue><spage>897</spage><epage>901</epage><pages>897-901</pages><issn>0969-8043</issn><eissn>1872-9800</eissn><abstract>18F-labeling of the nitroimidazole nucleoside analogue 1-(5-fluoro-5-deoxy-
α-
D-arabinofuranosyl)-2-nitroimidazole (FAZA) was developed to use this tracer in PET for detection of hypoxia. Parameters for labeling and hydrolysis were optimized with regard to amount of precursor, temperature and time. Labeling yields reached a maximum of 62±4% at 100
°C within 5
min using 5
mg of precursor. Hydrolysis was best performed with 1
mL of 0.1
N NaOH at 20
°C for 2
min. Transfer of these conditions to an automated synthesizer resulted in an overall radiochemical yield of 20.7±3.5%. Absolute yields at EOS were 9.8±2.3
GBq of [
18F]FAZA ready for injection (
n=21; 50
min after EOB; irradiation parameters: 35
μA, 60
min). Thus, a convenient approach suitable for large-scale production of [
18F]FAZA was developed by an automated process.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>15799867</pmid><doi>10.1016/j.apradiso.2004.12.004</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0969-8043 |
| ispartof | Applied radiation and isotopes, 2005-06, Vol.62 (6), p.897-901 |
| issn | 0969-8043 1872-9800 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_67570649 |
| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | [ 18F]FAZA Automation Cell Hypoxia Fluorine Radioisotopes Hypoxia Nitroimidazole Nitroimidazoles - chemistry Positron emission tomography Radioisotopes - chemistry |
| title | Preparation of the hypoxia imaging PET tracer [ 18F]FAZA: reaction parameters and automation |
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