Complexation and biodistribution study of 111In and 90Y complexes of bifunctional phosphinic acid analogs of H4dota.
Identifieur interne : 001F85 ( Main/Exploration ); précédent : 001F84; suivant : 001F86Complexation and biodistribution study of 111In and 90Y complexes of bifunctional phosphinic acid analogs of H4dota.
Auteurs : RBID : pubmed:18951809English descriptors
- KwdEn :
- Animals, Heterocyclic Compounds, 1-Ring (chemistry), Heterocyclic Compounds, 1-Ring (pharmacokinetics), Indium Radioisotopes (chemistry), Indium Radioisotopes (pharmacokinetics), Organometallic Compounds (chemistry), Organometallic Compounds (pharmacokinetics), Phosphinic Acids (chemistry), Phosphinic Acids (pharmacokinetics), Radiopharmaceuticals (chemistry), Radiopharmaceuticals (pharmacokinetics), Rats, Tissue Distribution, Yttrium Radioisotopes (chemistry), Yttrium Radioisotopes (pharmacokinetics).
- MESH :
- chemical , chemistry : Heterocyclic Compounds, 1-Ring, Indium Radioisotopes, Organometallic Compounds, Phosphinic Acids, Radiopharmaceuticals, Yttrium Radioisotopes.
- chemical , pharmacokinetics : Heterocyclic Compounds, 1-Ring, Indium Radioisotopes, Organometallic Compounds, Phosphinic Acids, Radiopharmaceuticals, Yttrium Radioisotopes.
- Animals, Rats, Tissue Distribution.
Abstract
In this study, the complexation rates of two new phosphinate H(4)dota (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) analogs, H(5)do3ap(PrA) and H(4)do3ap(ABn), and H(4)dota itself were compared under identical conditions (H(5)do3ap(PrA)=10-{[(2-carboxyethyl)hydroxyphosphoryl]methyl}-1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid; H(4)do3ap(ABn)=10-{[(4-aminophenyl)hydroxyphosphoryl]methyl}-1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid). The biodistribution of their (111)In and (90)Y complexes in healthy rats was also studied. Unlike the observation obtained under "chemical" conditions where differences between the ligands were observed no such differences in complexation rates were found under radiochemical conditions. The ligands bind the radiometals similarly to H(4)dota. So, "chemical" formation kinetic data should be transferred into radiochemical conditions only with high care and "radiochemical" complexation experiments should be run as part of standard in vitro studies with new ligands considered as potential radiopharmaceuticals. Pharmacokinetic studies in rats showed similar distribution characteristics for both phosphinate H(4)dota analogs radiolabelled with (111)In and (90)Y when compared with that of the (111)In-H(4)dota complex. No specific uptake in any organ and tissue of rats was determined. The phosphinate complexes are not accumulated in calcified tissues.
DOI: 10.1016/j.apradiso.2008.08.013
PubMed: 18951809
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Complexation and biodistribution study of 111In and 90Y complexes of bifunctional phosphinic acid analogs of H4dota.</title><author><name sortKey="F Rsterov, Michaela" uniqKey="F Rsterov M">Michaela Försterová</name><affiliation wicri:level="1"><nlm:affiliation>Department of Inorganic Chemistry, Faculty of Science, Universita Karlova (Charles University), Hlavova 2030, 128 40 Prague 2, Czech Republic.</nlm:affiliation><country xml:lang="fr">République tchèque</country><wicri:regionArea>Department of Inorganic Chemistry, Faculty of Science, Universita Karlova (Charles University), Hlavova 2030, 128 40 Prague 2</wicri:regionArea></affiliation></author><author><name sortKey="Petr K, Milos" uniqKey="Petr K M">Milos Petrík</name></author><author><name sortKey="L Znickov, Alice" uniqKey="L Znickov A">Alice Láznicková</name></author><author><name sortKey="L Zn Cek, Milan" uniqKey="L Zn Cek M">Milan Láznícek</name></author><author><name sortKey="Hermann, Petr" uniqKey="Hermann P">Petr Hermann</name></author><author><name sortKey="Lukes, Ivan" uniqKey="Lukes I">Ivan Lukes</name></author><author><name sortKey="Melichar, Frantisek" uniqKey="Melichar F">Frantisek Melichar</name></author></titleStmt><publicationStmt><date when="2009">2009</date><idno type="doi">10.1016/j.apradiso.2008.08.013</idno><idno type="RBID">pubmed:18951809</idno><idno type="pmid">18951809</idno><idno type="wicri:Area/Main/Corpus">002192</idno><idno type="wicri:Area/Main/Curation">002192</idno><idno type="wicri:Area/Main/Exploration">001F85</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Heterocyclic Compounds, 1-Ring (chemistry)</term><term>Heterocyclic Compounds, 1-Ring (pharmacokinetics)</term><term>Indium Radioisotopes (chemistry)</term><term>Indium Radioisotopes (pharmacokinetics)</term><term>Organometallic Compounds (chemistry)</term><term>Organometallic Compounds (pharmacokinetics)</term><term>Phosphinic Acids (chemistry)</term><term>Phosphinic Acids (pharmacokinetics)</term><term>Radiopharmaceuticals (chemistry)</term><term>Radiopharmaceuticals (pharmacokinetics)</term><term>Rats</term><term>Tissue Distribution</term><term>Yttrium Radioisotopes (chemistry)</term><term>Yttrium Radioisotopes (pharmacokinetics)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Heterocyclic Compounds, 1-Ring</term><term>Indium Radioisotopes</term><term>Organometallic Compounds</term><term>Phosphinic Acids</term><term>Radiopharmaceuticals</term><term>Yttrium Radioisotopes</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Heterocyclic Compounds, 1-Ring</term><term>Indium Radioisotopes</term><term>Organometallic Compounds</term><term>Phosphinic Acids</term><term>Radiopharmaceuticals</term><term>Yttrium Radioisotopes</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Rats</term><term>Tissue Distribution</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">In this study, the complexation rates of two new phosphinate H(4)dota (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) analogs, H(5)do3ap(PrA) and H(4)do3ap(ABn), and H(4)dota itself were compared under identical conditions (H(5)do3ap(PrA)=10-{[(2-carboxyethyl)hydroxyphosphoryl]methyl}-1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid; H(4)do3ap(ABn)=10-{[(4-aminophenyl)hydroxyphosphoryl]methyl}-1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid). The biodistribution of their (111)In and (90)Y complexes in healthy rats was also studied. Unlike the observation obtained under "chemical" conditions where differences between the ligands were observed no such differences in complexation rates were found under radiochemical conditions. The ligands bind the radiometals similarly to H(4)dota. So, "chemical" formation kinetic data should be transferred into radiochemical conditions only with high care and "radiochemical" complexation experiments should be run as part of standard in vitro studies with new ligands considered as potential radiopharmaceuticals. Pharmacokinetic studies in rats showed similar distribution characteristics for both phosphinate H(4)dota analogs radiolabelled with (111)In and (90)Y when compared with that of the (111)In-H(4)dota complex. No specific uptake in any organ and tissue of rats was determined. The phosphinate complexes are not accumulated in calcified tissues.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">18951809</PMID><DateCreated><Year>2008</Year><Month>11</Month><Day>26</Day></DateCreated><DateCompleted><Year>2009</Year><Month>01</Month><Day>12</Day></DateCompleted><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1872-9800</ISSN><JournalIssue CitedMedium="Internet"><Volume>67</Volume><Issue>1</Issue><PubDate><Year>2009</Year><Month>Jan</Month></PubDate></JournalIssue><Title>Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine</Title><ISOAbbreviation>Appl Radiat Isot</ISOAbbreviation></Journal><ArticleTitle>Complexation and biodistribution study of 111In and 90Y complexes of bifunctional phosphinic acid analogs of H4dota.</ArticleTitle><Pagination><MedlinePgn>21-9</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1016/j.apradiso.2008.08.013</ELocationID><Abstract><AbstractText>In this study, the complexation rates of two new phosphinate H(4)dota (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) analogs, H(5)do3ap(PrA) and H(4)do3ap(ABn), and H(4)dota itself were compared under identical conditions (H(5)do3ap(PrA)=10-{[(2-carboxyethyl)hydroxyphosphoryl]methyl}-1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid; H(4)do3ap(ABn)=10-{[(4-aminophenyl)hydroxyphosphoryl]methyl}-1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid). The biodistribution of their (111)In and (90)Y complexes in healthy rats was also studied. Unlike the observation obtained under "chemical" conditions where differences between the ligands were observed no such differences in complexation rates were found under radiochemical conditions. The ligands bind the radiometals similarly to H(4)dota. So, "chemical" formation kinetic data should be transferred into radiochemical conditions only with high care and "radiochemical" complexation experiments should be run as part of standard in vitro studies with new ligands considered as potential radiopharmaceuticals. Pharmacokinetic studies in rats showed similar distribution characteristics for both phosphinate H(4)dota analogs radiolabelled with (111)In and (90)Y when compared with that of the (111)In-H(4)dota complex. No specific uptake in any organ and tissue of rats was determined. The phosphinate complexes are not accumulated in calcified tissues.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Försterová</LastName><ForeName>Michaela</ForeName><Initials>M</Initials><Affiliation>Department of Inorganic Chemistry, Faculty of Science, Universita Karlova (Charles University), Hlavova 2030, 128 40 Prague 2, Czech Republic.</Affiliation></Author><Author ValidYN="Y"><LastName>Petrík</LastName><ForeName>Milos</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Láznicková</LastName><ForeName>Alice</ForeName><Initials>A</Initials></Author><Author ValidYN="Y"><LastName>Láznícek</LastName><ForeName>Milan</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Hermann</LastName><ForeName>Petr</ForeName><Initials>P</Initials></Author><Author ValidYN="Y"><LastName>Lukes</LastName><ForeName>Ivan</ForeName><Initials>I</Initials></Author><Author 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Compounds</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Phosphinic Acids</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Yttrium Radioisotopes</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Heterocyclic Compounds, 1-Ring</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName 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MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="received"><Year>2008</Year><Month>2</Month><Day>7</Day></PubMedPubDate><PubMedPubDate PubStatus="revised"><Year>2008</Year><Month>8</Month><Day>5</Day></PubMedPubDate><PubMedPubDate PubStatus="accepted"><Year>2008</Year><Month>8</Month><Day>26</Day></PubMedPubDate><PubMedPubDate PubStatus="aheadofprint"><Year>2008</Year><Month>9</Month><Day>6</Day></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2008</Year><Month>10</Month><Day>28</Day><Hour>9</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2009</Year><Month>1</Month><Day>13</Day><Hour>9</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2008</Year><Month>10</Month><Day>28</Day><Hour>9</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId 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