Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humans
Purpose A new PET ligand, 3-fluoro-5-(2-(2- 18 F-(fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile ( 18 F-SP203), is a positron emission tomographic radioligand selective for metabotropic glutamate subtype 5 receptors. The purposes of this study were to estimate the radiation-absorbed doses of 18 F-S...
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| Veröffentlicht in: | European journal of nuclear medicine and molecular imaging 2010-10, Vol.37 (10), p.1943-1949 |
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| container_issue | 10 |
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| container_title | European journal of nuclear medicine and molecular imaging |
| container_volume | 37 |
| creator | Kimura, Yasuyuki Siméon, Fabrice G. Hatazawa, Jun Mozley, P. David Pike, Victor W. Innis, Robert B. Fujita, Masahiro |
| description | Purpose
A new PET ligand, 3-fluoro-5-(2-(2-
18
F-(fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile (
18
F-SP203), is a positron emission tomographic radioligand selective for metabotropic glutamate subtype 5 receptors. The purposes of this study were to estimate the radiation-absorbed doses of
18
F-SP203 in humans and to determine from the distribution of radioactivity in bone structures with various proportions of bone and red marrow whether
18
F-SP203 undergoes defluorination.
Methods
Whole-body images were acquired for 5 h after injecting
18
F-SP203 in seven healthy humans. Urine was collected at various time points. Radiation-absorbed doses were estimated by the Medical Internal Radiation Dose scheme.
Results
After injecting
18
F-SP203, the two organs with highest radiation exposure were urinary bladder wall and gallbladder wall, consistent with both urinary and fecal excretion. In the skeleton, most of the radioactivity was in bone structures that contain red marrow and not in those without red marrow. Although the dose to red marrow (30.9 μSv/MBq) was unusually high, the effective dose (17.8 μSv/MBq) of
18
F-SP203 was typical of that of other
18
F radiotracers.
Conclusion
18
F-SP203 causes an effective dose in humans typical of several other
18
F radioligands and undergoes little defluorination. |
| doi_str_mv | 10.1007/s00259-010-1447-8 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_pubme</sourceid><recordid>TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_3207261</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2136005301</sourcerecordid><originalsourceid>FETCH-LOGICAL-c3798-a0f561d2308caa6ec03e5fb43f5f58af196ae958208412fa212f84da1286b2b73</originalsourceid><addsrcrecordid>eNp1UcFu1DAUtBCIlsIHcEEW5waenTi2L0hQUUCq1ErA2XpJ7KyrTRxsB2m_hZ_Fy5alPXCxPX4z80YaQl4yeMMA5NsEwIWugEHFmkZW6hE5ZS3TlQSlHx_fEk7Is5RuAZjiSj8lJxyEElK2p-TXBx8Gn3L03Zp9mCnOA404ePyDhpD8ZHPc0eAo0qXAHMu_nXxKe0IOUxgjLhvf060fi_qcMnVZfb3hUJ-XMfUTjpYWE-xC0S6FOG7XjBNmS9Pa5d1iqaDR9nbJISbqZ7pZJ5zTc_LE4TbZF3f3Gfl--fHbxefq6vrTl4v3V1VfS60qBCdaNvAaVI_Y2h5qK1zX1E44odAx3aLVQnFQDeMOeTlUMyDjqu14J-sz8u7gu6zdZIfezjni1iyxRI87E9Cbh5PZb8wYfpqag-QtKwav7wxi-LHalM1tWONcMhspgLdKM11I7EDqY0gpWndcwMDs6zSHOg3scanTqKJ5dT_ZUfG3v0LgB0Iqo3m08d_m_7v-BnGnrjw</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>750268919</pqid></control><display><type>article</type><title>Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humans</title><source>MEDLINE</source><source>SpringerLink Journals</source><creator>Kimura, Yasuyuki ; Siméon, Fabrice G. ; Hatazawa, Jun ; Mozley, P. David ; Pike, Victor W. ; Innis, Robert B. ; Fujita, Masahiro</creator><creatorcontrib>Kimura, Yasuyuki ; Siméon, Fabrice G. ; Hatazawa, Jun ; Mozley, P. David ; Pike, Victor W. ; Innis, Robert B. ; Fujita, Masahiro</creatorcontrib><description>Purpose
A new PET ligand, 3-fluoro-5-(2-(2-
18
F-(fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile (
18
F-SP203), is a positron emission tomographic radioligand selective for metabotropic glutamate subtype 5 receptors. The purposes of this study were to estimate the radiation-absorbed doses of
18
F-SP203 in humans and to determine from the distribution of radioactivity in bone structures with various proportions of bone and red marrow whether
18
F-SP203 undergoes defluorination.
Methods
Whole-body images were acquired for 5 h after injecting
18
F-SP203 in seven healthy humans. Urine was collected at various time points. Radiation-absorbed doses were estimated by the Medical Internal Radiation Dose scheme.
Results
After injecting
18
F-SP203, the two organs with highest radiation exposure were urinary bladder wall and gallbladder wall, consistent with both urinary and fecal excretion. In the skeleton, most of the radioactivity was in bone structures that contain red marrow and not in those without red marrow. Although the dose to red marrow (30.9 μSv/MBq) was unusually high, the effective dose (17.8 μSv/MBq) of
18
F-SP203 was typical of that of other
18
F radiotracers.
Conclusion
18
F-SP203 causes an effective dose in humans typical of several other
18
F radioligands and undergoes little defluorination.</description><identifier>ISSN: 1619-7070</identifier><identifier>EISSN: 1619-7089</identifier><identifier>DOI: 10.1007/s00259-010-1447-8</identifier><identifier>PMID: 20585776</identifier><language>eng</language><publisher>Berlin/Heidelberg: Springer-Verlag</publisher><subject>Adult ; Bone and Bones - metabolism ; Bone and Bones - radiation effects ; Bone marrow ; Bone Marrow - metabolism ; Bone Marrow - radiation effects ; Cardiology ; Estimating techniques ; Female ; Fluorine Radioisotopes - chemistry ; Halogenation ; Human exposure ; Humans ; Imaging ; Ligands ; Male ; Medicine ; Medicine & Public Health ; Nitriles - chemistry ; Nitriles - metabolism ; Nitriles - pharmacokinetics ; Nuclear Medicine ; Oncology ; Original Article ; Orthopedics ; Positron-Emission Tomography - methods ; Radiation Dosage ; Radioactivity ; Radiology ; Radiometry ; Receptor, Metabotropic Glutamate 5 ; Receptors, Metabotropic Glutamate - metabolism ; Thiazoles - chemistry ; Thiazoles - metabolism ; Thiazoles - pharmacokinetics ; Tomography</subject><ispartof>European journal of nuclear medicine and molecular imaging, 2010-10, Vol.37 (10), p.1943-1949</ispartof><rights>US Government 2010</rights><rights>Springer-Verlag 2010</rights><rights>US Government 2010 2010</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3798-a0f561d2308caa6ec03e5fb43f5f58af196ae958208412fa212f84da1286b2b73</citedby><cites>FETCH-LOGICAL-c3798-a0f561d2308caa6ec03e5fb43f5f58af196ae958208412fa212f84da1286b2b73</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s00259-010-1447-8$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s00259-010-1447-8$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>230,314,776,780,881,27901,27902,41464,42533,51294</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20585776$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kimura, Yasuyuki</creatorcontrib><creatorcontrib>Siméon, Fabrice G.</creatorcontrib><creatorcontrib>Hatazawa, Jun</creatorcontrib><creatorcontrib>Mozley, P. David</creatorcontrib><creatorcontrib>Pike, Victor W.</creatorcontrib><creatorcontrib>Innis, Robert B.</creatorcontrib><creatorcontrib>Fujita, Masahiro</creatorcontrib><title>Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humans</title><title>European journal of nuclear medicine and molecular imaging</title><addtitle>Eur J Nucl Med Mol Imaging</addtitle><addtitle>Eur J Nucl Med Mol Imaging</addtitle><description>Purpose
A new PET ligand, 3-fluoro-5-(2-(2-
18
F-(fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile (
18
F-SP203), is a positron emission tomographic radioligand selective for metabotropic glutamate subtype 5 receptors. The purposes of this study were to estimate the radiation-absorbed doses of
18
F-SP203 in humans and to determine from the distribution of radioactivity in bone structures with various proportions of bone and red marrow whether
18
F-SP203 undergoes defluorination.
Methods
Whole-body images were acquired for 5 h after injecting
18
F-SP203 in seven healthy humans. Urine was collected at various time points. Radiation-absorbed doses were estimated by the Medical Internal Radiation Dose scheme.
Results
After injecting
18
F-SP203, the two organs with highest radiation exposure were urinary bladder wall and gallbladder wall, consistent with both urinary and fecal excretion. In the skeleton, most of the radioactivity was in bone structures that contain red marrow and not in those without red marrow. Although the dose to red marrow (30.9 μSv/MBq) was unusually high, the effective dose (17.8 μSv/MBq) of
18
F-SP203 was typical of that of other
18
F radiotracers.
Conclusion
18
F-SP203 causes an effective dose in humans typical of several other
18
F radioligands and undergoes little defluorination.</description><subject>Adult</subject><subject>Bone and Bones - metabolism</subject><subject>Bone and Bones - radiation effects</subject><subject>Bone marrow</subject><subject>Bone Marrow - metabolism</subject><subject>Bone Marrow - radiation effects</subject><subject>Cardiology</subject><subject>Estimating techniques</subject><subject>Female</subject><subject>Fluorine Radioisotopes - chemistry</subject><subject>Halogenation</subject><subject>Human exposure</subject><subject>Humans</subject><subject>Imaging</subject><subject>Ligands</subject><subject>Male</subject><subject>Medicine</subject><subject>Medicine & Public Health</subject><subject>Nitriles - chemistry</subject><subject>Nitriles - metabolism</subject><subject>Nitriles - pharmacokinetics</subject><subject>Nuclear Medicine</subject><subject>Oncology</subject><subject>Original Article</subject><subject>Orthopedics</subject><subject>Positron-Emission Tomography - methods</subject><subject>Radiation Dosage</subject><subject>Radioactivity</subject><subject>Radiology</subject><subject>Radiometry</subject><subject>Receptor, Metabotropic Glutamate 5</subject><subject>Receptors, Metabotropic Glutamate - metabolism</subject><subject>Thiazoles - chemistry</subject><subject>Thiazoles - metabolism</subject><subject>Thiazoles - pharmacokinetics</subject><subject>Tomography</subject><issn>1619-7070</issn><issn>1619-7089</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>BENPR</sourceid><recordid>eNp1UcFu1DAUtBCIlsIHcEEW5waenTi2L0hQUUCq1ErA2XpJ7KyrTRxsB2m_hZ_Fy5alPXCxPX4z80YaQl4yeMMA5NsEwIWugEHFmkZW6hE5ZS3TlQSlHx_fEk7Is5RuAZjiSj8lJxyEElK2p-TXBx8Gn3L03Zp9mCnOA404ePyDhpD8ZHPc0eAo0qXAHMu_nXxKe0IOUxgjLhvf060fi_qcMnVZfb3hUJ-XMfUTjpYWE-xC0S6FOG7XjBNmS9Pa5d1iqaDR9nbJISbqZ7pZJ5zTc_LE4TbZF3f3Gfl--fHbxefq6vrTl4v3V1VfS60qBCdaNvAaVI_Y2h5qK1zX1E44odAx3aLVQnFQDeMOeTlUMyDjqu14J-sz8u7gu6zdZIfezjni1iyxRI87E9Cbh5PZb8wYfpqag-QtKwav7wxi-LHalM1tWONcMhspgLdKM11I7EDqY0gpWndcwMDs6zSHOg3scanTqKJ5dT_ZUfG3v0LgB0Iqo3m08d_m_7v-BnGnrjw</recordid><startdate>201010</startdate><enddate>201010</enddate><creator>Kimura, Yasuyuki</creator><creator>Siméon, Fabrice G.</creator><creator>Hatazawa, Jun</creator><creator>Mozley, P. David</creator><creator>Pike, Victor W.</creator><creator>Innis, Robert B.</creator><creator>Fujita, Masahiro</creator><general>Springer-Verlag</general><general>Springer Nature B.V</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>3V.</scope><scope>7RV</scope><scope>7TK</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FE</scope><scope>8FG</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>ARAPS</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>BHPHI</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>KB0</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M7P</scope><scope>NAPCQ</scope><scope>P5Z</scope><scope>P62</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>5PM</scope></search><sort><creationdate>201010</creationdate><title>Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humans</title><author>Kimura, Yasuyuki ; Siméon, Fabrice G. ; Hatazawa, Jun ; Mozley, P. David ; Pike, Victor W. ; Innis, Robert B. ; Fujita, Masahiro</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3798-a0f561d2308caa6ec03e5fb43f5f58af196ae958208412fa212f84da1286b2b73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Adult</topic><topic>Bone and Bones - metabolism</topic><topic>Bone and Bones - radiation effects</topic><topic>Bone marrow</topic><topic>Bone Marrow - metabolism</topic><topic>Bone Marrow - radiation effects</topic><topic>Cardiology</topic><topic>Estimating techniques</topic><topic>Female</topic><topic>Fluorine Radioisotopes - chemistry</topic><topic>Halogenation</topic><topic>Human exposure</topic><topic>Humans</topic><topic>Imaging</topic><topic>Ligands</topic><topic>Male</topic><topic>Medicine</topic><topic>Medicine & Public Health</topic><topic>Nitriles - chemistry</topic><topic>Nitriles - metabolism</topic><topic>Nitriles - pharmacokinetics</topic><topic>Nuclear Medicine</topic><topic>Oncology</topic><topic>Original Article</topic><topic>Orthopedics</topic><topic>Positron-Emission Tomography - methods</topic><topic>Radiation Dosage</topic><topic>Radioactivity</topic><topic>Radiology</topic><topic>Radiometry</topic><topic>Receptor, Metabotropic Glutamate 5</topic><topic>Receptors, Metabotropic Glutamate - metabolism</topic><topic>Thiazoles - chemistry</topic><topic>Thiazoles - metabolism</topic><topic>Thiazoles - pharmacokinetics</topic><topic>Tomography</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kimura, Yasuyuki</creatorcontrib><creatorcontrib>Siméon, Fabrice G.</creatorcontrib><creatorcontrib>Hatazawa, Jun</creatorcontrib><creatorcontrib>Mozley, P. David</creatorcontrib><creatorcontrib>Pike, Victor W.</creatorcontrib><creatorcontrib>Innis, Robert B.</creatorcontrib><creatorcontrib>Fujita, Masahiro</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Nursing & Allied Health Database</collection><collection>Neurosciences Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Technology Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>Advanced Technologies & Aerospace Collection</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Technology Collection</collection><collection>Natural Science Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Biological Science Database</collection><collection>Nursing & Allied Health Premium</collection><collection>Advanced Technologies & Aerospace Database</collection><collection>ProQuest Advanced Technologies & Aerospace Collection</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>European journal of nuclear medicine and molecular imaging</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kimura, Yasuyuki</au><au>Siméon, Fabrice G.</au><au>Hatazawa, Jun</au><au>Mozley, P. David</au><au>Pike, Victor W.</au><au>Innis, Robert B.</au><au>Fujita, Masahiro</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humans</atitle><jtitle>European journal of nuclear medicine and molecular imaging</jtitle><stitle>Eur J Nucl Med Mol Imaging</stitle><addtitle>Eur J Nucl Med Mol Imaging</addtitle><date>2010-10</date><risdate>2010</risdate><volume>37</volume><issue>10</issue><spage>1943</spage><epage>1949</epage><pages>1943-1949</pages><issn>1619-7070</issn><eissn>1619-7089</eissn><abstract>Purpose
A new PET ligand, 3-fluoro-5-(2-(2-
18
F-(fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile (
18
F-SP203), is a positron emission tomographic radioligand selective for metabotropic glutamate subtype 5 receptors. The purposes of this study were to estimate the radiation-absorbed doses of
18
F-SP203 in humans and to determine from the distribution of radioactivity in bone structures with various proportions of bone and red marrow whether
18
F-SP203 undergoes defluorination.
Methods
Whole-body images were acquired for 5 h after injecting
18
F-SP203 in seven healthy humans. Urine was collected at various time points. Radiation-absorbed doses were estimated by the Medical Internal Radiation Dose scheme.
Results
After injecting
18
F-SP203, the two organs with highest radiation exposure were urinary bladder wall and gallbladder wall, consistent with both urinary and fecal excretion. In the skeleton, most of the radioactivity was in bone structures that contain red marrow and not in those without red marrow. Although the dose to red marrow (30.9 μSv/MBq) was unusually high, the effective dose (17.8 μSv/MBq) of
18
F-SP203 was typical of that of other
18
F radiotracers.
Conclusion
18
F-SP203 causes an effective dose in humans typical of several other
18
F radioligands and undergoes little defluorination.</abstract><cop>Berlin/Heidelberg</cop><pub>Springer-Verlag</pub><pmid>20585776</pmid><doi>10.1007/s00259-010-1447-8</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1619-7070 |
| ispartof | European journal of nuclear medicine and molecular imaging, 2010-10, Vol.37 (10), p.1943-1949 |
| issn | 1619-7070 1619-7089 |
| language | eng |
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| source | MEDLINE; SpringerLink Journals |
| subjects | Adult Bone and Bones - metabolism Bone and Bones - radiation effects Bone marrow Bone Marrow - metabolism Bone Marrow - radiation effects Cardiology Estimating techniques Female Fluorine Radioisotopes - chemistry Halogenation Human exposure Humans Imaging Ligands Male Medicine Medicine & Public Health Nitriles - chemistry Nitriles - metabolism Nitriles - pharmacokinetics Nuclear Medicine Oncology Original Article Orthopedics Positron-Emission Tomography - methods Radiation Dosage Radioactivity Radiology Radiometry Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate - metabolism Thiazoles - chemistry Thiazoles - metabolism Thiazoles - pharmacokinetics Tomography |
| title | Biodistribution and radiation dosimetry of a positron emission tomographic ligand, 18F-SP203, to image metabotropic glutamate subtype 5 receptors in humans |
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