N-[ 18f]fluoroethylpiperidinyl, n-[ 18f]fluoroethylpiperidinemethyl and n-[ 18f]fluoroethylpyrrolidinyl esters as radiotracers for acetylcholinesterase
A series of N-fluoroethylpiperidinyl (1), N-fluoroethylpiperidinemethyl (2) and N-fluoroethylpyrrolidinyl (3) esters were synthesized and examined as new 18F-labeled radiotracers for measuring brain cholinesterase activity. The fluoroethyl group, instead of methyl group, results in slower in vitro e...
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| Veröffentlicht in: | Nuclear medicine and biology 2003-07, Vol.30 (5), p.491-500 |
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| creator | Shao, Xia Butch, Elizabeth R Kilbourn, Michael R Snyder, Scott E |
| description | A series of
N-fluoroethylpiperidinyl (1),
N-fluoroethylpiperidinemethyl (2) and
N-fluoroethylpyrrolidinyl (3) esters were synthesized and examined as new
18F-labeled radiotracers for measuring brain cholinesterase activity. The fluoroethyl group, instead of methyl group, results in slower
in vitro enzymatic cleavage rates and higher selectivity for AChE. Based on metabolism in mouse blood and PET time-activity curves in rats, two radiotracers were identified as potential candidates for further
in vivo evaluation in higher species. |
| doi_str_mv | 10.1016/S0969-8051(03)00031-3 |
| format | Article |
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N-fluoroethylpiperidinyl (1),
N-fluoroethylpiperidinemethyl (2) and
N-fluoroethylpyrrolidinyl (3) esters were synthesized and examined as new
18F-labeled radiotracers for measuring brain cholinesterase activity. The fluoroethyl group, instead of methyl group, results in slower
in vitro enzymatic cleavage rates and higher selectivity for AChE. Based on metabolism in mouse blood and PET time-activity curves in rats, two radiotracers were identified as potential candidates for further
in vivo evaluation in higher species.</description><identifier>ISSN: 0969-8051</identifier><identifier>EISSN: 1872-9614</identifier><identifier>DOI: 10.1016/S0969-8051(03)00031-3</identifier><identifier>PMID: 12831986</identifier><language>eng</language><publisher>Amsterdam: Elsevier Inc</publisher><subject>Acetylcholinesterase ; Acetylcholinesterase - metabolism ; Alzheimer’s disease ; Animals ; Biological and medical sciences ; Brain - diagnostic imaging ; Brain - metabolism ; Cerebral Cortex - diagnostic imaging ; Cerebral Cortex - metabolism ; Corpus Striatum - diagnostic imaging ; Corpus Striatum - metabolism ; Electrophorus ; Emission computed ; Esters - blood ; Esters - chemistry ; Esters - pharmacokinetics ; Female ; Fluorine-18 ; Horses ; Hydrolysis ; Isotope Labeling - methods ; Medical sciences ; Metabolic Clearance Rate ; Mice ; Piperidines - blood ; Piperidines - chemistry ; Piperidines - pharmacokinetics ; Protein Binding ; Pyrrolidines - blood ; Pyrrolidines - chemistry ; Pyrrolidines - pharmacokinetics ; Radionuclide Imaging ; Radiopharmaceuticals - blood ; Radiopharmaceuticals - chemistry ; Radiopharmaceuticals - pharmacokinetics ; Tissue Distribution ; Tomography</subject><ispartof>Nuclear medicine and biology, 2003-07, Vol.30 (5), p.491-500</ispartof><rights>2003 Elsevier Inc.</rights><rights>2003 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c391t-a8a44a648f9a056352fca740e926cd234be2fcb0b811d9a98f9fbd1b86b3ebd93</citedby><cites>FETCH-LOGICAL-c391t-a8a44a648f9a056352fca740e926cd234be2fcb0b811d9a98f9fbd1b86b3ebd93</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0969805103000313$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14974856$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12831986$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shao, Xia</creatorcontrib><creatorcontrib>Butch, Elizabeth R</creatorcontrib><creatorcontrib>Kilbourn, Michael R</creatorcontrib><creatorcontrib>Snyder, Scott E</creatorcontrib><title>N-[ 18f]fluoroethylpiperidinyl, n-[ 18f]fluoroethylpiperidinemethyl and n-[ 18f]fluoroethylpyrrolidinyl esters as radiotracers for acetylcholinesterase</title><title>Nuclear medicine and biology</title><addtitle>Nucl Med Biol</addtitle><description>A series of
N-fluoroethylpiperidinyl (1),
N-fluoroethylpiperidinemethyl (2) and
N-fluoroethylpyrrolidinyl (3) esters were synthesized and examined as new
18F-labeled radiotracers for measuring brain cholinesterase activity. The fluoroethyl group, instead of methyl group, results in slower
in vitro enzymatic cleavage rates and higher selectivity for AChE. Based on metabolism in mouse blood and PET time-activity curves in rats, two radiotracers were identified as potential candidates for further
in vivo evaluation in higher species.</description><subject>Acetylcholinesterase</subject><subject>Acetylcholinesterase - metabolism</subject><subject>Alzheimer’s disease</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Brain - diagnostic imaging</subject><subject>Brain - metabolism</subject><subject>Cerebral Cortex - diagnostic imaging</subject><subject>Cerebral Cortex - metabolism</subject><subject>Corpus Striatum - diagnostic imaging</subject><subject>Corpus Striatum - metabolism</subject><subject>Electrophorus</subject><subject>Emission computed</subject><subject>Esters - blood</subject><subject>Esters - chemistry</subject><subject>Esters - pharmacokinetics</subject><subject>Female</subject><subject>Fluorine-18</subject><subject>Horses</subject><subject>Hydrolysis</subject><subject>Isotope Labeling - methods</subject><subject>Medical sciences</subject><subject>Metabolic Clearance Rate</subject><subject>Mice</subject><subject>Piperidines - blood</subject><subject>Piperidines - chemistry</subject><subject>Piperidines - pharmacokinetics</subject><subject>Protein Binding</subject><subject>Pyrrolidines - blood</subject><subject>Pyrrolidines - chemistry</subject><subject>Pyrrolidines - pharmacokinetics</subject><subject>Radionuclide Imaging</subject><subject>Radiopharmaceuticals - blood</subject><subject>Radiopharmaceuticals - chemistry</subject><subject>Radiopharmaceuticals - pharmacokinetics</subject><subject>Tissue Distribution</subject><subject>Tomography</subject><issn>0969-8051</issn><issn>1872-9614</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkdtqFTEUhkNR2m3tI1TmRlFwNJlkspMrkeIJSnuhXpUS1iQrNJI92U1mC_Mkvq7ZB-yN6NU65PvXCusn5JzRN4wy-fYr1VK3ivbsJeWvKKWctfyILJhadq2WTDwiiz_ICXlSyg9adYLRY3LCOsWZVnJBfl21Nw1T_tbHTcoJp7s5rsMac3BhnOPrZvzHO652dQOj-ys355ziflCDZcJcGihNBhfSlMFua59yU7NpjvausuMOg4JPyWMPseDZIZ6S7x8_fLv43F5ef_py8f6ytVyzqQUFQoAUymugveR95y0sBUXdSes6LgasnYEOijGnQVfOD44NSg4cB6f5KXmxn7vO6X5Tt5tVKBZjhBHTppglF6yTWlSw34M2p1IyerPOYQV5NoyarSNm54jZnttQbnaOGF51zw4LNsMK3YPqYEEFnh8AKBaizzDaUB44oZdC9Vvu3Z7Deo6fAbMpNuBo0YWMdjIuhf985TetRa0H</recordid><startdate>20030701</startdate><enddate>20030701</enddate><creator>Shao, Xia</creator><creator>Butch, Elizabeth R</creator><creator>Kilbourn, Michael R</creator><creator>Snyder, Scott E</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>20030701</creationdate><title>N-[ 18f]fluoroethylpiperidinyl, n-[ 18f]fluoroethylpiperidinemethyl and n-[ 18f]fluoroethylpyrrolidinyl esters as radiotracers for acetylcholinesterase</title><author>Shao, Xia ; Butch, Elizabeth R ; Kilbourn, Michael R ; Snyder, Scott E</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c391t-a8a44a648f9a056352fca740e926cd234be2fcb0b811d9a98f9fbd1b86b3ebd93</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Acetylcholinesterase</topic><topic>Acetylcholinesterase - metabolism</topic><topic>Alzheimer’s disease</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Brain - diagnostic imaging</topic><topic>Brain - metabolism</topic><topic>Cerebral Cortex - diagnostic imaging</topic><topic>Cerebral Cortex - metabolism</topic><topic>Corpus Striatum - diagnostic imaging</topic><topic>Corpus Striatum - metabolism</topic><topic>Electrophorus</topic><topic>Emission computed</topic><topic>Esters - blood</topic><topic>Esters - chemistry</topic><topic>Esters - pharmacokinetics</topic><topic>Female</topic><topic>Fluorine-18</topic><topic>Horses</topic><topic>Hydrolysis</topic><topic>Isotope Labeling - methods</topic><topic>Medical sciences</topic><topic>Metabolic Clearance Rate</topic><topic>Mice</topic><topic>Piperidines - blood</topic><topic>Piperidines - chemistry</topic><topic>Piperidines - pharmacokinetics</topic><topic>Protein Binding</topic><topic>Pyrrolidines - blood</topic><topic>Pyrrolidines - chemistry</topic><topic>Pyrrolidines - pharmacokinetics</topic><topic>Radionuclide Imaging</topic><topic>Radiopharmaceuticals - blood</topic><topic>Radiopharmaceuticals - chemistry</topic><topic>Radiopharmaceuticals - pharmacokinetics</topic><topic>Tissue Distribution</topic><topic>Tomography</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shao, Xia</creatorcontrib><creatorcontrib>Butch, Elizabeth R</creatorcontrib><creatorcontrib>Kilbourn, Michael R</creatorcontrib><creatorcontrib>Snyder, Scott E</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>Shao, Xia</au><au>Butch, Elizabeth R</au><au>Kilbourn, Michael R</au><au>Snyder, Scott E</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>N-[ 18f]fluoroethylpiperidinyl, n-[ 18f]fluoroethylpiperidinemethyl and n-[ 18f]fluoroethylpyrrolidinyl esters as radiotracers for acetylcholinesterase</atitle><jtitle>Nuclear medicine and biology</jtitle><addtitle>Nucl Med Biol</addtitle><date>2003-07-01</date><risdate>2003</risdate><volume>30</volume><issue>5</issue><spage>491</spage><epage>500</epage><pages>491-500</pages><issn>0969-8051</issn><eissn>1872-9614</eissn><abstract>A series of
N-fluoroethylpiperidinyl (1),
N-fluoroethylpiperidinemethyl (2) and
N-fluoroethylpyrrolidinyl (3) esters were synthesized and examined as new
18F-labeled radiotracers for measuring brain cholinesterase activity. The fluoroethyl group, instead of methyl group, results in slower
in vitro enzymatic cleavage rates and higher selectivity for AChE. Based on metabolism in mouse blood and PET time-activity curves in rats, two radiotracers were identified as potential candidates for further
in vivo evaluation in higher species.</abstract><cop>Amsterdam</cop><pub>Elsevier Inc</pub><pmid>12831986</pmid><doi>10.1016/S0969-8051(03)00031-3</doi><tpages>10</tpages></addata></record> |
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| ispartof | Nuclear medicine and biology, 2003-07, Vol.30 (5), p.491-500 |
| issn | 0969-8051 1872-9614 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Acetylcholinesterase Acetylcholinesterase - metabolism Alzheimer’s disease Animals Biological and medical sciences Brain - diagnostic imaging Brain - metabolism Cerebral Cortex - diagnostic imaging Cerebral Cortex - metabolism Corpus Striatum - diagnostic imaging Corpus Striatum - metabolism Electrophorus Emission computed Esters - blood Esters - chemistry Esters - pharmacokinetics Female Fluorine-18 Horses Hydrolysis Isotope Labeling - methods Medical sciences Metabolic Clearance Rate Mice Piperidines - blood Piperidines - chemistry Piperidines - pharmacokinetics Protein Binding Pyrrolidines - blood Pyrrolidines - chemistry Pyrrolidines - pharmacokinetics Radionuclide Imaging Radiopharmaceuticals - blood Radiopharmaceuticals - chemistry Radiopharmaceuticals - pharmacokinetics Tissue Distribution Tomography |
| title | N-[ 18f]fluoroethylpiperidinyl, n-[ 18f]fluoroethylpiperidinemethyl and n-[ 18f]fluoroethylpyrrolidinyl esters as radiotracers for acetylcholinesterase |
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