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Synthesis of 18 F labelled FK960, a candidate anti‐dementia drug, and PET studies in conscious monkeys
The present study demonstrated the synthesis and in vivo study of 18 F‐labeled N ‐(4‐acetyl‐1‐piperazinyl)‐ p ‐fluorobenzamide (FK960) which is a novel anti‐dementia drug candidate. [ 18 F]FK960 was prepared by a one‐pot, three reaction sequence, using nucleophilic fluorination, with an automated sy...
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| Published in: | Journal of labelled compounds & radiopharmaceuticals 2002-12, Vol.45 (14), p.1219-1228 |
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| Main Authors: | , , , , |
| Format: | Article |
| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c723-7b39c3ad0a037953495637e563261cd53062c12ffd964320a56e2cc56ee4a8223 |
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| cites | cdi_FETCH-LOGICAL-c723-7b39c3ad0a037953495637e563261cd53062c12ffd964320a56e2cc56ee4a8223 |
| container_end_page | 1228 |
| container_issue | 14 |
| container_start_page | 1219 |
| container_title | Journal of labelled compounds & radiopharmaceuticals |
| container_volume | 45 |
| creator | Murakami, Yoshihiro Nishimura, Shintaro Noda, Akihiro Harada, Norihiro Tsukada, Hideo |
| description | The present study demonstrated the synthesis and
in vivo
study of
18
F‐labeled
N
‐(4‐acetyl‐1‐piperazinyl)‐
p
‐fluorobenzamide (FK960) which is a novel anti‐dementia drug candidate. [
18
F]FK960 was prepared by a one‐pot, three reaction sequence, using nucleophilic fluorination, with an automated synthetic apparatus using either ethyl‐4‐trimethylammonium triflate (
1a
) or ethyl‐4‐nitrobenzoate (
1b
) as the precursor for labeling. Though
1a
gave a higher yield, the specific activity was 50–100 fold higher with
1b
. The radiochemical yield of [
18
F]FK960 was 7–15% (EOB) and the specific activity ranged from 2.0–60.2 GBq/μmol depending on the amount of F‐18 used. The synthesis time was 2.2–2.9 h. The obtained [
18
F]FK960 was injected into 3 conscious monkeys (100–120 MBq/kg body weight), and distribution images and pharmacokinetic data for [
18
F]FK960 showed similar uptake in different brain regions and 3‐fold higher levels of [
18
F]FK960 in blood relative to brain. Copyright © 2002 John Wiley & Sons, Ltd. |
| doi_str_mv | 10.1002/jlcr.633 |
| format | article |
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in vivo
study of
18
F‐labeled
N
‐(4‐acetyl‐1‐piperazinyl)‐
p
‐fluorobenzamide (FK960) which is a novel anti‐dementia drug candidate. [
18
F]FK960 was prepared by a one‐pot, three reaction sequence, using nucleophilic fluorination, with an automated synthetic apparatus using either ethyl‐4‐trimethylammonium triflate (
1a
) or ethyl‐4‐nitrobenzoate (
1b
) as the precursor for labeling. Though
1a
gave a higher yield, the specific activity was 50–100 fold higher with
1b
. The radiochemical yield of [
18
F]FK960 was 7–15% (EOB) and the specific activity ranged from 2.0–60.2 GBq/μmol depending on the amount of F‐18 used. The synthesis time was 2.2–2.9 h. The obtained [
18
F]FK960 was injected into 3 conscious monkeys (100–120 MBq/kg body weight), and distribution images and pharmacokinetic data for [
18
F]FK960 showed similar uptake in different brain regions and 3‐fold higher levels of [
18
F]FK960 in blood relative to brain. Copyright © 2002 John Wiley & Sons, Ltd.</description><identifier>ISSN: 0362-4803</identifier><identifier>EISSN: 1099-1344</identifier><identifier>DOI: 10.1002/jlcr.633</identifier><language>eng</language><ispartof>Journal of labelled compounds & radiopharmaceuticals, 2002-12, Vol.45 (14), p.1219-1228</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c723-7b39c3ad0a037953495637e563261cd53062c12ffd964320a56e2cc56ee4a8223</citedby><cites>FETCH-LOGICAL-c723-7b39c3ad0a037953495637e563261cd53062c12ffd964320a56e2cc56ee4a8223</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27923,27924</link.rule.ids></links><search><creatorcontrib>Murakami, Yoshihiro</creatorcontrib><creatorcontrib>Nishimura, Shintaro</creatorcontrib><creatorcontrib>Noda, Akihiro</creatorcontrib><creatorcontrib>Harada, Norihiro</creatorcontrib><creatorcontrib>Tsukada, Hideo</creatorcontrib><title>Synthesis of 18 F labelled FK960, a candidate anti‐dementia drug, and PET studies in conscious monkeys</title><title>Journal of labelled compounds & radiopharmaceuticals</title><description>The present study demonstrated the synthesis and
in vivo
study of
18
F‐labeled
N
‐(4‐acetyl‐1‐piperazinyl)‐
p
‐fluorobenzamide (FK960) which is a novel anti‐dementia drug candidate. [
18
F]FK960 was prepared by a one‐pot, three reaction sequence, using nucleophilic fluorination, with an automated synthetic apparatus using either ethyl‐4‐trimethylammonium triflate (
1a
) or ethyl‐4‐nitrobenzoate (
1b
) as the precursor for labeling. Though
1a
gave a higher yield, the specific activity was 50–100 fold higher with
1b
. The radiochemical yield of [
18
F]FK960 was 7–15% (EOB) and the specific activity ranged from 2.0–60.2 GBq/μmol depending on the amount of F‐18 used. The synthesis time was 2.2–2.9 h. The obtained [
18
F]FK960 was injected into 3 conscious monkeys (100–120 MBq/kg body weight), and distribution images and pharmacokinetic data for [
18
F]FK960 showed similar uptake in different brain regions and 3‐fold higher levels of [
18
F]FK960 in blood relative to brain. Copyright © 2002 John Wiley & Sons, Ltd.</description><issn>0362-4803</issn><issn>1099-1344</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><recordid>eNotkEFOwzAURC0EEqEgcYS_ZEHKt7_j1EtUtYCoBBLdR67tUJfEQXG66I4jcEZOQirYzIw0o1k8xq45TjmiuNs1tp8qohOWcdQ65yTlKcuQlMjlDOmcXaS0Qxw7KTO2fTvEYetTSNDVwGewhMZsfNN4B8tnrfAWDFgTXXBm8GDiEH6-vp1v_ZgMuH7_Pi6ig9fFGtKwd8EnCBFsF5MN3T5B28UPf0iX7Kw2TfJX_z5h6-ViPX_MVy8PT_P7VW5LQXm5IW3JODRIpS5I6kJR6UcRiltXECphuahrp5UkgaZQXlg7qpdmJgRN2M3fre27lHpfV599aE1_qDhWR0DVEVA1AqJfdZhYMQ</recordid><startdate>200212</startdate><enddate>200212</enddate><creator>Murakami, Yoshihiro</creator><creator>Nishimura, Shintaro</creator><creator>Noda, Akihiro</creator><creator>Harada, Norihiro</creator><creator>Tsukada, Hideo</creator><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>200212</creationdate><title>Synthesis of 18 F labelled FK960, a candidate anti‐dementia drug, and PET studies in conscious monkeys</title><author>Murakami, Yoshihiro ; Nishimura, Shintaro ; Noda, Akihiro ; Harada, Norihiro ; Tsukada, Hideo</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c723-7b39c3ad0a037953495637e563261cd53062c12ffd964320a56e2cc56ee4a8223</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Murakami, Yoshihiro</creatorcontrib><creatorcontrib>Nishimura, Shintaro</creatorcontrib><creatorcontrib>Noda, Akihiro</creatorcontrib><creatorcontrib>Harada, Norihiro</creatorcontrib><creatorcontrib>Tsukada, Hideo</creatorcontrib><collection>CrossRef</collection><jtitle>Journal of labelled compounds & radiopharmaceuticals</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Murakami, Yoshihiro</au><au>Nishimura, Shintaro</au><au>Noda, Akihiro</au><au>Harada, Norihiro</au><au>Tsukada, Hideo</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of 18 F labelled FK960, a candidate anti‐dementia drug, and PET studies in conscious monkeys</atitle><jtitle>Journal of labelled compounds & radiopharmaceuticals</jtitle><date>2002-12</date><risdate>2002</risdate><volume>45</volume><issue>14</issue><spage>1219</spage><epage>1228</epage><pages>1219-1228</pages><issn>0362-4803</issn><eissn>1099-1344</eissn><abstract>The present study demonstrated the synthesis and
in vivo
study of
18
F‐labeled
N
‐(4‐acetyl‐1‐piperazinyl)‐
p
‐fluorobenzamide (FK960) which is a novel anti‐dementia drug candidate. [
18
F]FK960 was prepared by a one‐pot, three reaction sequence, using nucleophilic fluorination, with an automated synthetic apparatus using either ethyl‐4‐trimethylammonium triflate (
1a
) or ethyl‐4‐nitrobenzoate (
1b
) as the precursor for labeling. Though
1a
gave a higher yield, the specific activity was 50–100 fold higher with
1b
. The radiochemical yield of [
18
F]FK960 was 7–15% (EOB) and the specific activity ranged from 2.0–60.2 GBq/μmol depending on the amount of F‐18 used. The synthesis time was 2.2–2.9 h. The obtained [
18
F]FK960 was injected into 3 conscious monkeys (100–120 MBq/kg body weight), and distribution images and pharmacokinetic data for [
18
F]FK960 showed similar uptake in different brain regions and 3‐fold higher levels of [
18
F]FK960 in blood relative to brain. Copyright © 2002 John Wiley & Sons, Ltd.</abstract><doi>10.1002/jlcr.633</doi><tpages>10</tpages></addata></record> |
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| ispartof | Journal of labelled compounds & radiopharmaceuticals, 2002-12, Vol.45 (14), p.1219-1228 |
| issn | 0362-4803 1099-1344 |
| language | eng |
| recordid | cdi_crossref_primary_10_1002_jlcr_633 |
| source | Wiley-Blackwell Read & Publish Collection |
| title | Synthesis of 18 F labelled FK960, a candidate anti‐dementia drug, and PET studies in conscious monkeys |
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