Evaluation of 3-[ 18F]Fluoro-α-fluoromethyl- p-tyrosine as a tracer for striatal tyrosine hydroxylase activity
3-[ 18F]Fluoro-α-fluoromethyl- p-tyrosine (3-F-FMPT) was evaluated as a tracer for CNS tyrosine hydroxylase (TH) activity in rodents and in a rhesus monkey. Results of in vitro experiments using rat striatal homogenates showed that the introduction of fluorine into the 3-phenyl position did not sign...
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| Veröffentlicht in: | Nuclear medicine and biology 1994-05, Vol.21 (4), p.663-667 |
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| creator | Dejesus, O.T. Murali, D. Kitchen, R. Endres, C. Oakes, T.R. Shelton, S.E. Freund, L. Houser, D. Uno, H. Holden, J.E. Nickles, R.J. |
| description | 3-[
18F]Fluoro-α-fluoromethyl-
p-tyrosine (3-F-FMPT) was evaluated as a tracer for CNS tyrosine hydroxylase (TH) activity in rodents and in a rhesus monkey. Results of
in vitro experiments using rat striatal homogenates showed that the introduction of fluorine into the 3-phenyl position did not significantly alter the ability of FMPT to act as a TH-activated
l-aromatic amino acid decarboxylase (
l-AAAD) inhibitor. These studies further showed that 3-F-FMPT-induced
l-AAAD inhibition was dose-dependent. Furthermore, striatal homogenates prepared from rats pretreated with the potent TH inhibitor α-methyl-
p-tyrosine was found to have diminished 3-F-FMPT-induced
l-AAAD inhibition. However, despite these promising
in vitro results, the biodistribution of this compound in mice showed low brain uptake and fast clearance through the kidneys. A PET study using a Rhesus monkey injected with 3-[
18F]F-FMPT confirmed the results obtained in mice, i.e. negligible brain uptake but high localization in the bladder. We conclude that 3-[
18F]F-FMPT would not be useful as a tracer for cerebral TH activity. |
| doi_str_mv | 10.1016/0969-8051(94)90033-7 |
| format | Article |
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18F]Fluoro-α-fluoromethyl-
p-tyrosine (3-F-FMPT) was evaluated as a tracer for CNS tyrosine hydroxylase (TH) activity in rodents and in a rhesus monkey. Results of
in vitro experiments using rat striatal homogenates showed that the introduction of fluorine into the 3-phenyl position did not significantly alter the ability of FMPT to act as a TH-activated
l-aromatic amino acid decarboxylase (
l-AAAD) inhibitor. These studies further showed that 3-F-FMPT-induced
l-AAAD inhibition was dose-dependent. Furthermore, striatal homogenates prepared from rats pretreated with the potent TH inhibitor α-methyl-
p-tyrosine was found to have diminished 3-F-FMPT-induced
l-AAAD inhibition. However, despite these promising
in vitro results, the biodistribution of this compound in mice showed low brain uptake and fast clearance through the kidneys. A PET study using a Rhesus monkey injected with 3-[
18F]F-FMPT confirmed the results obtained in mice, i.e. negligible brain uptake but high localization in the bladder. We conclude that 3-[
18F]F-FMPT would not be useful as a tracer for cerebral TH activity.</description><identifier>ISSN: 0969-8051</identifier><identifier>EISSN: 1872-9614</identifier><identifier>DOI: 10.1016/0969-8051(94)90033-7</identifier><identifier>PMID: 9234325</identifier><language>eng</language><publisher>Amsterdam: Elsevier Inc</publisher><subject>Animals ; Aromatic Amino Acid Decarboxylase Inhibitors ; Biological and medical sciences ; Brain - metabolism ; Contrast media. Radiopharmaceuticals ; Corpus Striatum - enzymology ; Enzyme Inhibitors - pharmacology ; Evaluation Studies as Topic ; Fluorine Radioisotopes - chemistry ; Macaca mulatta ; Male ; Medical sciences ; Methyltyrosines - pharmacokinetics ; Methyltyrosines - pharmacology ; Mice ; Mice, Inbred ICR ; Pharmacology. Drug treatments ; Rats ; Rats, Sprague-Dawley ; Tissue Distribution ; Tomography, Emission-Computed ; Tyrosine - analogs & derivatives ; Tyrosine - pharmacokinetics ; Tyrosine 3-Monooxygenase - metabolism</subject><ispartof>Nuclear medicine and biology, 1994-05, Vol.21 (4), p.663-667</ispartof><rights>1994</rights><rights>1994 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-861538b3fe0c68e265f09c7a1afb8412ba05560cf8ba97e2f1888440eb8ff6913</citedby><cites>FETCH-LOGICAL-c386t-861538b3fe0c68e265f09c7a1afb8412ba05560cf8ba97e2f1888440eb8ff6913</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0969-8051(94)90033-7$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,782,786,3552,27931,27932,46002</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=4137212$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9234325$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Dejesus, O.T.</creatorcontrib><creatorcontrib>Murali, D.</creatorcontrib><creatorcontrib>Kitchen, R.</creatorcontrib><creatorcontrib>Endres, C.</creatorcontrib><creatorcontrib>Oakes, T.R.</creatorcontrib><creatorcontrib>Shelton, S.E.</creatorcontrib><creatorcontrib>Freund, L.</creatorcontrib><creatorcontrib>Houser, D.</creatorcontrib><creatorcontrib>Uno, H.</creatorcontrib><creatorcontrib>Holden, J.E.</creatorcontrib><creatorcontrib>Nickles, R.J.</creatorcontrib><title>Evaluation of 3-[ 18F]Fluoro-α-fluoromethyl- p-tyrosine as a tracer for striatal tyrosine hydroxylase activity</title><title>Nuclear medicine and biology</title><addtitle>Nucl Med Biol</addtitle><description>3-[
18F]Fluoro-α-fluoromethyl-
p-tyrosine (3-F-FMPT) was evaluated as a tracer for CNS tyrosine hydroxylase (TH) activity in rodents and in a rhesus monkey. Results of
in vitro experiments using rat striatal homogenates showed that the introduction of fluorine into the 3-phenyl position did not significantly alter the ability of FMPT to act as a TH-activated
l-aromatic amino acid decarboxylase (
l-AAAD) inhibitor. These studies further showed that 3-F-FMPT-induced
l-AAAD inhibition was dose-dependent. Furthermore, striatal homogenates prepared from rats pretreated with the potent TH inhibitor α-methyl-
p-tyrosine was found to have diminished 3-F-FMPT-induced
l-AAAD inhibition. However, despite these promising
in vitro results, the biodistribution of this compound in mice showed low brain uptake and fast clearance through the kidneys. A PET study using a Rhesus monkey injected with 3-[
18F]F-FMPT confirmed the results obtained in mice, i.e. negligible brain uptake but high localization in the bladder. We conclude that 3-[
18F]F-FMPT would not be useful as a tracer for cerebral TH activity.</description><subject>Animals</subject><subject>Aromatic Amino Acid Decarboxylase Inhibitors</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Contrast media. Radiopharmaceuticals</subject><subject>Corpus Striatum - enzymology</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Evaluation Studies as Topic</subject><subject>Fluorine Radioisotopes - chemistry</subject><subject>Macaca mulatta</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Methyltyrosines - pharmacokinetics</subject><subject>Methyltyrosines - pharmacology</subject><subject>Mice</subject><subject>Mice, Inbred ICR</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Tissue Distribution</subject><subject>Tomography, Emission-Computed</subject><subject>Tyrosine - analogs & derivatives</subject><subject>Tyrosine - pharmacokinetics</subject><subject>Tyrosine 3-Monooxygenase - metabolism</subject><issn>0969-8051</issn><issn>1872-9614</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1994</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMGKFDEQhoMo6-zqGyjkIKKHaNJJp5OLIMvOKix40ZNIqM5U2EhPZ0zSg_1YvojPZM_OMEdPVVDf_1N8hLwQ_J3gQr_nVltmeCveWPXWci4l6x6RlTBdw6wW6jFZnZGn5LKUn3yJKcEvyIVtpJJNuyLpZg_DBDWmkaZAJftOhVn_WA9Tyon9_cPCw7bFej8PjO5YnXMqcUQKhQKtGTxmGlKmpeYIFQZ6Ju7nTU6_5wHKQvsa97HOz8iTAEPB56d5Rb6tb75ef2J3X24_X3-8Y14aXZnRopWmlwG51wYb3QZufQcCQm-UaHrgbau5D6YH22EThDFGKY69CUFbIa_I62PvLqdfE5bqtrF4HAYYMU3FdZ3gxmqzgOoI-uXrkjG4XY5byLMT3B08u4NEd5DorHIPnl23xF6e-qd-i5tz6CR2ub863aF4GEKG0cdyxpSQXSOaBftwxHBxsY-YXfERR4-bmNFXt0nx_3_8A_rTmrQ</recordid><startdate>19940501</startdate><enddate>19940501</enddate><creator>Dejesus, O.T.</creator><creator>Murali, D.</creator><creator>Kitchen, R.</creator><creator>Endres, C.</creator><creator>Oakes, T.R.</creator><creator>Shelton, S.E.</creator><creator>Freund, L.</creator><creator>Houser, D.</creator><creator>Uno, H.</creator><creator>Holden, J.E.</creator><creator>Nickles, R.J.</creator><general>Elsevier Inc</general><general>Elsevier</general><scope>IQODW</scope><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>7X8</scope></search><sort><creationdate>19940501</creationdate><title>Evaluation of 3-[ 18F]Fluoro-α-fluoromethyl- p-tyrosine as a tracer for striatal tyrosine hydroxylase activity</title><author>Dejesus, O.T. ; Murali, D. ; Kitchen, R. ; Endres, C. ; Oakes, T.R. ; Shelton, S.E. ; Freund, L. ; Houser, D. ; Uno, H. ; Holden, J.E. ; Nickles, R.J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-861538b3fe0c68e265f09c7a1afb8412ba05560cf8ba97e2f1888440eb8ff6913</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1994</creationdate><topic>Animals</topic><topic>Aromatic Amino Acid Decarboxylase Inhibitors</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Contrast media. Radiopharmaceuticals</topic><topic>Corpus Striatum - enzymology</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>Evaluation Studies as Topic</topic><topic>Fluorine Radioisotopes - chemistry</topic><topic>Macaca mulatta</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Methyltyrosines - pharmacokinetics</topic><topic>Methyltyrosines - pharmacology</topic><topic>Mice</topic><topic>Mice, Inbred ICR</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Tissue Distribution</topic><topic>Tomography, Emission-Computed</topic><topic>Tyrosine - analogs & derivatives</topic><topic>Tyrosine - pharmacokinetics</topic><topic>Tyrosine 3-Monooxygenase - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Dejesus, O.T.</creatorcontrib><creatorcontrib>Murali, D.</creatorcontrib><creatorcontrib>Kitchen, R.</creatorcontrib><creatorcontrib>Endres, C.</creatorcontrib><creatorcontrib>Oakes, T.R.</creatorcontrib><creatorcontrib>Shelton, S.E.</creatorcontrib><creatorcontrib>Freund, L.</creatorcontrib><creatorcontrib>Houser, D.</creatorcontrib><creatorcontrib>Uno, H.</creatorcontrib><creatorcontrib>Holden, J.E.</creatorcontrib><creatorcontrib>Nickles, R.J.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Nuclear medicine and biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Dejesus, O.T.</au><au>Murali, D.</au><au>Kitchen, R.</au><au>Endres, C.</au><au>Oakes, T.R.</au><au>Shelton, S.E.</au><au>Freund, L.</au><au>Houser, D.</au><au>Uno, H.</au><au>Holden, J.E.</au><au>Nickles, R.J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evaluation of 3-[ 18F]Fluoro-α-fluoromethyl- p-tyrosine as a tracer for striatal tyrosine hydroxylase activity</atitle><jtitle>Nuclear medicine and biology</jtitle><addtitle>Nucl Med Biol</addtitle><date>1994-05-01</date><risdate>1994</risdate><volume>21</volume><issue>4</issue><spage>663</spage><epage>667</epage><pages>663-667</pages><issn>0969-8051</issn><eissn>1872-9614</eissn><abstract>3-[
18F]Fluoro-α-fluoromethyl-
p-tyrosine (3-F-FMPT) was evaluated as a tracer for CNS tyrosine hydroxylase (TH) activity in rodents and in a rhesus monkey. Results of
in vitro experiments using rat striatal homogenates showed that the introduction of fluorine into the 3-phenyl position did not significantly alter the ability of FMPT to act as a TH-activated
l-aromatic amino acid decarboxylase (
l-AAAD) inhibitor. These studies further showed that 3-F-FMPT-induced
l-AAAD inhibition was dose-dependent. Furthermore, striatal homogenates prepared from rats pretreated with the potent TH inhibitor α-methyl-
p-tyrosine was found to have diminished 3-F-FMPT-induced
l-AAAD inhibition. However, despite these promising
in vitro results, the biodistribution of this compound in mice showed low brain uptake and fast clearance through the kidneys. A PET study using a Rhesus monkey injected with 3-[
18F]F-FMPT confirmed the results obtained in mice, i.e. negligible brain uptake but high localization in the bladder. We conclude that 3-[
18F]F-FMPT would not be useful as a tracer for cerebral TH activity.</abstract><cop>Amsterdam</cop><pub>Elsevier Inc</pub><pmid>9234325</pmid><doi>10.1016/0969-8051(94)90033-7</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | Nuclear medicine and biology, 1994-05, Vol.21 (4), p.663-667 |
| issn | 0969-8051 1872-9614 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_77108968 |
| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Animals Aromatic Amino Acid Decarboxylase Inhibitors Biological and medical sciences Brain - metabolism Contrast media. Radiopharmaceuticals Corpus Striatum - enzymology Enzyme Inhibitors - pharmacology Evaluation Studies as Topic Fluorine Radioisotopes - chemistry Macaca mulatta Male Medical sciences Methyltyrosines - pharmacokinetics Methyltyrosines - pharmacology Mice Mice, Inbred ICR Pharmacology. Drug treatments Rats Rats, Sprague-Dawley Tissue Distribution Tomography, Emission-Computed Tyrosine - analogs & derivatives Tyrosine - pharmacokinetics Tyrosine 3-Monooxygenase - metabolism |
| title | Evaluation of 3-[ 18F]Fluoro-α-fluoromethyl- p-tyrosine as a tracer for striatal tyrosine hydroxylase activity |
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