Radiolabelling of glucose-Tyr3-octreotate with 125I and analysis of its metabolism in rats: comparison with radiolabelled DOTA-Tyr3-octreotate.
Identifieur interne : 007D87 ( Main/Exploration ); précédent : 007D86; suivant : 007D88Radiolabelling of glucose-Tyr3-octreotate with 125I and analysis of its metabolism in rats: comparison with radiolabelled DOTA-Tyr3-octreotate.
Auteurs : RBID : pubmed:18225554English descriptors
- KwdEn :
- Animals, Blood Proteins (metabolism), Chromatography, High Pressure Liquid, Glucose (analogs & derivatives), Glucose (metabolism), Heterocyclic Compounds, 1-Ring (chemistry), Heterocyclic Compounds, 1-Ring (metabolism), Indium Radioisotopes (chemistry), Iodine Radioisotopes (chemistry), Isotope Labeling, Lutetium (chemistry), Male, Peptides, Cyclic (chemistry), Peptides, Cyclic (metabolism), Protein Binding, Radioisotopes (chemistry), Radiopharmaceuticals (chemical synthesis), Radiopharmaceuticals (metabolism), Rats, Rats, Wistar.
- MESH :
- chemical , analogs & derivatives : Glucose.
- chemical , chemical synthesis : Radiopharmaceuticals.
- chemical , chemistry : Heterocyclic Compounds, 1-Ring, Indium Radioisotopes, Iodine Radioisotopes, Lutetium, Peptides, Cyclic, Radioisotopes.
- chemical , metabolism : Blood Proteins, Glucose, Heterocyclic Compounds, 1-Ring, Peptides, Cyclic, Radiopharmaceuticals.
- Animals, Chromatography, High Pressure Liquid, Isotope Labeling, Male, Protein Binding, Rats, Rats, Wistar.
Abstract
Somatostatin analogues labelled with radiometals or radiohalogens are useful for the imaging and treatment of somatostatin receptor-containing tumours. In this study, the procedures for the radioiodination of glucose-Tyr3-octreotate (gluc-Tyr3-tate) and radiolabelling of DOTA-Tyr3-octreotate (DOTA-Tyr3-tate) with 111In, 177Lu and 125I were compared and their metabolism in rats was analyzed. The usefulness of high performance liquid chromatography (HPLC) analysis and instant thin-layer chromatography on silica gel (ITLC-SG) for both radiochemical purity determination and analysis of metabolism in urine was investigated. MATERIALS AND METHODs: For labelling with radiometals, the formation of a complex with the 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) functionality of the peptide was employed. Radioiodination was performed by the chloramime-T method. The radiochemical purity of radiolabelled peptides and the analyses of rat urine were determined by HPLC and/or ITLC-SG methods. Male Wistar rats were used in the elimination studies.
PubMed: 18225554
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Radiolabelling of glucose-Tyr3-octreotate with 125I and analysis of its metabolism in rats: comparison with radiolabelled DOTA-Tyr3-octreotate.</title><author><name sortKey="Petrik, Milos" uniqKey="Petrik M">Milos Petrik</name><affiliation wicri:level="1"><nlm:affiliation>Department of Biophysics and Physical Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.</nlm:affiliation><country xml:lang="fr">République tchèque</country><wicri:regionArea>Department of Biophysics and Physical Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove</wicri:regionArea></affiliation></author><author><name sortKey="Laznickova, Alice" uniqKey="Laznickova A">Alice Laznickova</name></author><author><name sortKey="Laznicek, Milan" uniqKey="Laznicek M">Milan Laznicek</name></author><author><name sortKey="Zalutsky, Michael R" uniqKey="Zalutsky M">Michael R Zalutsky</name></author></titleStmt><publicationStmt><date when="????"><PubDate><MedlineDate>2007 Nov-Dec</MedlineDate></PubDate></date><idno type="RBID">pubmed:18225554</idno><idno type="pmid">18225554</idno><idno type="wicri:Area/Main/Corpus">002514</idno><idno type="wicri:Area/Main/Curation">002514</idno><idno type="wicri:Area/Main/Exploration">007D87</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Blood Proteins (metabolism)</term><term>Chromatography, High Pressure Liquid</term><term>Glucose (analogs & derivatives)</term><term>Glucose (metabolism)</term><term>Heterocyclic Compounds, 1-Ring (chemistry)</term><term>Heterocyclic Compounds, 1-Ring (metabolism)</term><term>Indium Radioisotopes (chemistry)</term><term>Iodine Radioisotopes (chemistry)</term><term>Isotope Labeling</term><term>Lutetium (chemistry)</term><term>Male</term><term>Peptides, Cyclic (chemistry)</term><term>Peptides, Cyclic (metabolism)</term><term>Protein Binding</term><term>Radioisotopes (chemistry)</term><term>Radiopharmaceuticals (chemical synthesis)</term><term>Radiopharmaceuticals (metabolism)</term><term>Rats</term><term>Rats, Wistar</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Glucose</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Heterocyclic Compounds, 1-Ring</term><term>Indium Radioisotopes</term><term>Iodine Radioisotopes</term><term>Lutetium</term><term>Peptides, Cyclic</term><term>Radioisotopes</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Blood Proteins</term><term>Glucose</term><term>Heterocyclic Compounds, 1-Ring</term><term>Peptides, Cyclic</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Chromatography, High Pressure Liquid</term><term>Isotope Labeling</term><term>Male</term><term>Protein Binding</term><term>Rats</term><term>Rats, Wistar</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Somatostatin analogues labelled with radiometals or radiohalogens are useful for the imaging and treatment of somatostatin receptor-containing tumours. In this study, the procedures for the radioiodination of glucose-Tyr3-octreotate (gluc-Tyr3-tate) and radiolabelling of DOTA-Tyr3-octreotate (DOTA-Tyr3-tate) with 111In, 177Lu and 125I were compared and their metabolism in rats was analyzed. The usefulness of high performance liquid chromatography (HPLC) analysis and instant thin-layer chromatography on silica gel (ITLC-SG) for both radiochemical purity determination and analysis of metabolism in urine was investigated. MATERIALS AND METHODs: For labelling with radiometals, the formation of a complex with the 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) functionality of the peptide was employed. Radioiodination was performed by the chloramime-T method. The radiochemical purity of radiolabelled peptides and the analyses of rat urine were determined by HPLC and/or ITLC-SG methods. Male Wistar rats were used in the elimination studies.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">18225554</PMID><DateCreated><Year>2008</Year><Month>01</Month><Day>29</Day></DateCreated><DateCompleted><Year>2008</Year><Month>02</Month><Day>12</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Print">0250-7005</ISSN><JournalIssue CitedMedium="Print"><Volume>27</Volume><Issue>6B</Issue><PubDate><MedlineDate>2007 Nov-Dec</MedlineDate></PubDate></JournalIssue><Title>Anticancer research</Title><ISOAbbreviation>Anticancer Res.</ISOAbbreviation></Journal><ArticleTitle>Radiolabelling of glucose-Tyr3-octreotate with 125I and analysis of its metabolism in rats: comparison with radiolabelled DOTA-Tyr3-octreotate.</ArticleTitle><Pagination><MedlinePgn>3941-6</MedlinePgn></Pagination><Abstract><AbstractText Label="BACKGROUND" NlmCategory="BACKGROUND">Somatostatin analogues labelled with radiometals or radiohalogens are useful for the imaging and treatment of somatostatin receptor-containing tumours. In this study, the procedures for the radioiodination of glucose-Tyr3-octreotate (gluc-Tyr3-tate) and radiolabelling of DOTA-Tyr3-octreotate (DOTA-Tyr3-tate) with 111In, 177Lu and 125I were compared and their metabolism in rats was analyzed. The usefulness of high performance liquid chromatography (HPLC) analysis and instant thin-layer chromatography on silica gel (ITLC-SG) for both radiochemical purity determination and analysis of metabolism in urine was investigated. MATERIALS AND METHODs: For labelling with radiometals, the formation of a complex with the 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) functionality of the peptide was employed. Radioiodination was performed by the chloramime-T method. The radiochemical purity of radiolabelled peptides and the analyses of rat urine were determined by HPLC and/or ITLC-SG methods. Male Wistar rats were used in the elimination studies.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">DOTA-Tyr3-tate was simply radiolabelled with radiometals with high yield and high radiochemical purity. Stopping of the reaction was a critical step for radioiodination, therefore labelling of gluc-Tyr3-tate and DOTA-Tyr3-tate with 125I was not so simple and the reaction product had to be purified by preparative HPLC analysis. Whereas 111In-DOTA-Tyr3-tate and 177Lu-DOTA-Tyr3-tate were eliminated in rat urine in a practically unchanged form, a significant proportion of metabolites was observed with radioiodinated peptides, particularly at longer time intervals.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">Labelling of DOTA-Tyr3-tate with radiometals is simple and the radiochemical purity of prepared compounds is very high, while iodination of the peptides demands purification of the product by preparative HPLC. The analysis of rat urine showed that excretion of radioiodinated peptides included a significant proportion of metabolites.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Petrik</LastName><ForeName>Milos</ForeName><Initials>M</Initials><Affiliation>Department of Biophysics and Physical Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.</Affiliation></Author><Author ValidYN="Y"><LastName>Laznickova</LastName><ForeName>Alice</ForeName><Initials>A</Initials></Author><Author ValidYN="Y"><LastName>Laznicek</LastName><ForeName>Milan</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Zalutsky</LastName><ForeName>Michael R</ForeName><Initials>MR</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Comparative Study</PublicationType><PublicationType>Journal Article</PublicationType><PublicationType>Research Support, Non-U.S. Gov't</PublicationType></PublicationTypeList></Article><MedlineJournalInfo><Country>Greece</Country><MedlineTA>Anticancer Res</MedlineTA><NlmUniqueID>8102988</NlmUniqueID><ISSNLinking>0250-7005</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Blood Proteins</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Heterocyclic Compounds, 1-Ring</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Indium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Iodine Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Peptides, Cyclic</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>octreotate, Tyr(3)-</NameOfSubstance></Chemical><Chemical><RegistryNumber>5H0DOZ21UJ</RegistryNumber><NameOfSubstance>Lutetium</NameOfSubstance></Chemical><Chemical><RegistryNumber>60239-18-1</RegistryNumber><NameOfSubstance>1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid</NameOfSubstance></Chemical><Chemical><RegistryNumber>IY9XDZ35W2</RegistryNumber><NameOfSubstance>Glucose</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Blood Proteins</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Chromatography, High Pressure Liquid</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Glucose</DescriptorName><QualifierName MajorTopicYN="Y">analogs & derivatives</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Heterocyclic Compounds, 1-Ring</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Iodine Radioisotopes</DescriptorName><QualifierName MajorTopicYN="Y">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Isotope Labeling</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Lutetium</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Male</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Peptides, Cyclic</DescriptorName><QualifierName MajorTopicYN="Y">chemistry</QualifierName><QualifierName MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Protein Binding</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radiopharmaceuticals</DescriptorName><QualifierName MajorTopicYN="Y">chemical synthesis</QualifierName><QualifierName MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Rats</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Rats, Wistar</DescriptorName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="pubmed"><Year>2008</Year><Month>1</Month><Day>30</Day><Hour>9</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2008</Year><Month>2</Month><Day>13</Day><Hour>9</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2008</Year><Month>1</Month><Day>30</Day><Hour>9</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pubmed">18225554</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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