Biodistribution of two octreotate analogs radiolabeled with indium and yttrium in rats.
Identifieur interne : 001B00 ( Main/Exploration ); précédent : 001A99; suivant : 001B01Biodistribution of two octreotate analogs radiolabeled with indium and yttrium in rats.
Auteurs : RBID : pubmed:20651367English descriptors
- KwdEn :
- Animals, Indium Radioisotopes (diagnostic use), Kidney (metabolism), Male, Octreotide (analogs & derivatives), Octreotide (chemistry), Octreotide (pharmacokinetics), Radiopharmaceuticals (chemistry), Radiopharmaceuticals (pharmacokinetics), Rats, Rats, Wistar, Tissue Distribution, Yttrium Radioisotopes (diagnostic use).
- MESH :
- chemical , analogs & derivatives : Octreotide.
- chemical , chemistry : Octreotide, Radiopharmaceuticals.
- chemical , diagnostic use : Indium Radioisotopes, Yttrium Radioisotopes.
- metabolism : Kidney.
- chemical , pharmacokinetics : Octreotide, Radiopharmaceuticals.
- Animals, Male, Rats, Rats, Wistar, Tissue Distribution.
Abstract
In this study, two octreotate derivatives N-[4-carboxy-4-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane-1-yl]butanoyl]-Tyr(3)-octreotate (DOTAGA-tate) and N-[[4,10-bis(carboxymethyl)-7-(1(1,3-dicarboxypropyl))-1,4,7,10-tetraaza-cyclododec-1-yl]acetyl]-Tyr(3)-octreotate (DOTA-t-GA-tate) were radio-labeled with (111)In or (88)Y and their biodistribution profiles together with their elimination characteristics in rats were compared.
PubMed: 20651367
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Biodistribution of two octreotate analogs radiolabeled with indium and yttrium in rats.</title><author><name sortKey="Laznickova, A" uniqKey="Laznickova A">A Laznickova</name><affiliation wicri:level="1"><nlm:affiliation>Charles University, Faculty of Pharmacy, Heyrovskeho 1203, CZ-500 05 Hradec Kralove, Czech Republic. laznickova@faf.cuni.cz</nlm:affiliation><country xml:lang="fr">République tchèque</country><wicri:regionArea>Charles University, Faculty of Pharmacy, Heyrovskeho 1203, CZ-500 05 Hradec Kralove</wicri:regionArea></affiliation></author><author><name sortKey="Laznicek, M" uniqKey="Laznicek M">M Laznicek</name></author><author><name sortKey="Trejtnar, F" uniqKey="Trejtnar F">F Trejtnar</name></author><author><name sortKey="Maecke, H R" uniqKey="Maecke H">H R Maecke</name></author><author><name sortKey="Eisenwiener, K P" uniqKey="Eisenwiener K">K P Eisenwiener</name></author><author><name sortKey="Reubi, J C" uniqKey="Reubi J">J C Reubi</name></author></titleStmt><publicationStmt><date when="2010">2010</date><idno type="RBID">pubmed:20651367</idno><idno type="pmid">20651367</idno><idno type="wicri:Area/Main/Corpus">001839</idno><idno type="wicri:Area/Main/Curation">001839</idno><idno type="wicri:Area/Main/Exploration">001B00</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Indium Radioisotopes (diagnostic use)</term><term>Kidney (metabolism)</term><term>Male</term><term>Octreotide (analogs & derivatives)</term><term>Octreotide (chemistry)</term><term>Octreotide (pharmacokinetics)</term><term>Radiopharmaceuticals (chemistry)</term><term>Radiopharmaceuticals (pharmacokinetics)</term><term>Rats</term><term>Rats, Wistar</term><term>Tissue Distribution</term><term>Yttrium Radioisotopes (diagnostic use)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Octreotide</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Octreotide</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" qualifier="diagnostic use" xml:lang="en"><term>Indium Radioisotopes</term><term>Yttrium Radioisotopes</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Kidney</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Octreotide</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Male</term><term>Rats</term><term>Rats, Wistar</term><term>Tissue Distribution</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">In this study, two octreotate derivatives N-[4-carboxy-4-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane-1-yl]butanoyl]-Tyr(3)-octreotate (DOTAGA-tate) and N-[[4,10-bis(carboxymethyl)-7-(1(1,3-dicarboxypropyl))-1,4,7,10-tetraaza-cyclododec-1-yl]acetyl]-Tyr(3)-octreotate (DOTA-t-GA-tate) were radio-labeled with (111)In or (88)Y and their biodistribution profiles together with their elimination characteristics in rats were compared.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">20651367</PMID><DateCreated><Year>2010</Year><Month>07</Month><Day>23</Day></DateCreated><DateCompleted><Year>2010</Year><Month>08</Month><Day>24</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Electronic">1791-7530</ISSN><JournalIssue CitedMedium="Internet"><Volume>30</Volume><Issue>6</Issue><PubDate><Year>2010</Year><Month>Jun</Month></PubDate></JournalIssue><Title>Anticancer research</Title><ISOAbbreviation>Anticancer Res.</ISOAbbreviation></Journal><ArticleTitle>Biodistribution of two octreotate analogs radiolabeled with indium and yttrium in rats.</ArticleTitle><Pagination><MedlinePgn>2177-84</MedlinePgn></Pagination><Abstract><AbstractText Label="BACKGROUND" NlmCategory="BACKGROUND">In this study, two octreotate derivatives N-[4-carboxy-4-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane-1-yl]butanoyl]-Tyr(3)-octreotate (DOTAGA-tate) and N-[[4,10-bis(carboxymethyl)-7-(1(1,3-dicarboxypropyl))-1,4,7,10-tetraaza-cyclododec-1-yl]acetyl]-Tyr(3)-octreotate (DOTA-t-GA-tate) were radio-labeled with (111)In or (88)Y and their biodistribution profiles together with their elimination characteristics in rats were compared.</AbstractText><AbstractText Label="MATERIALS AND METHODS" NlmCategory="METHODS">Radiolabeling of the peptides with high radiochemical purity was carried out in an acetate buffer with gentisic acid as radioprotective compound. Biodistribution profiles of the radiolabeled peptides were determined in intact male Wistar rats after an intravenous dose of 1 microg/kg. For elimination pathways analysis, studies in intact rats in metabolic cages and perfused rat kidney and liver were carried out.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">Fast radioactivity clearance from rat tissues (excepting somatostatin receptor-rich organs and the kidney) was determined for all agents under study. Profound radioactivity uptake in organs with a high density of somatostatin receptors (namely the adrenals and pancreas as biomarkers of somatostatin receptor-positive tissue) was slightly higher for radiolabeled DOTAGA-tate when compared with DOTA-t-GA-tate. Significantly higher accumulation in kidney and somewhat lower urinary elimination of (111)In-labeled peptides in comparison with that of (88)Y-agents were determined. Perfused rat kidney experiments confirmed that glomerular filtration was the main elimination mechanism for the compounds under study; their bile clearances in the perfused rat liver were negligible.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">(111)In((88)Y)-DOTAGA-tates exhibited higher distribution into somatostatin receptor-rich organs when compared with the corresponding radiolabeled DOTA-t-GA-tates. Higher uptake of (111)In-labeled peptides in the kidney is attributed to its different coordination properties.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Laznickova</LastName><ForeName>A</ForeName><Initials>A</Initials><Affiliation>Charles University, Faculty of Pharmacy, Heyrovskeho 1203, CZ-500 05 Hradec Kralove, Czech Republic. laznickova@faf.cuni.cz</Affiliation></Author><Author ValidYN="Y"><LastName>Laznicek</LastName><ForeName>M</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Trejtnar</LastName><ForeName>F</ForeName><Initials>F</Initials></Author><Author ValidYN="Y"><LastName>Maecke</LastName><ForeName>H R</ForeName><Initials>HR</Initials></Author><Author ValidYN="Y"><LastName>Eisenwiener</LastName><ForeName>K P</ForeName><Initials>KP</Initials></Author><Author ValidYN="Y"><LastName>Reubi</LastName><ForeName>J C</ForeName><Initials>JC</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><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>Indium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Y-DOTA-t-GA-tate</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Y-DOTAGA-tate</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Yttrium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>RWM8CCW8GP</RegistryNumber><NameOfSubstance>Octreotide</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Kidney</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Male</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Octreotide</DescriptorName><QualifierName MajorTopicYN="Y">analogs & derivatives</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radiopharmaceuticals</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Rats</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Rats, Wistar</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tissue Distribution</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Yttrium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="entrez"><Year>2010</Year><Month>7</Month><Day>24</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2010</Year><Month>7</Month><Day>24</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2010</Year><Month>8</Month><Day>25</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pii">30/6/2177</ArticleId><ArticleId IdType="pubmed">20651367</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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