Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon
A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand ( S)-5-[ 123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-IA, has been developed. The two-step sequence produced [ 123I]-5-IA in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioact...
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| Veröffentlicht in: | Nuclear medicine and biology 1999-02, Vol.26 (2), p.201-207 |
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| container_title | Nuclear medicine and biology |
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| creator | Musachio, John L. Villemagne, Victor L. Scheffel, Ursula A. Dannals, Robert F. Dogan, A.Semih Yokoi, Fuji Wong, Dean F. |
| description | A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (
S)-5-[
123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-IA, has been developed. The two-step sequence produced [
123I]-5-IA in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (>8,500 mCi/μmol). Preliminary single photon emission computed tomography studies with [
123I]-5-IA in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [
123I]-5-IA uptake in all brain regions (78–59% reduction), demonstrating the specificity of the radiotracer. |
| doi_str_mv | 10.1016/S0969-8051(98)00101-2 |
| format | Article |
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S)-5-[
123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-IA, has been developed. The two-step sequence produced [
123I]-5-IA in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (>8,500 mCi/μmol). Preliminary single photon emission computed tomography studies with [
123I]-5-IA in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [
123I]-5-IA uptake in all brain regions (78–59% reduction), demonstrating the specificity of the radiotracer.</description><identifier>ISSN: 0969-8051</identifier><identifier>EISSN: 1872-9614</identifier><identifier>DOI: 10.1016/S0969-8051(98)00101-2</identifier><identifier>PMID: 10100220</identifier><language>eng</language><publisher>Amsterdam: Elsevier Inc</publisher><subject>Animals ; Azetidines - chemical synthesis ; Biological and medical sciences ; Brain - diagnostic imaging ; Investigative techniques, diagnostic techniques (general aspects) ; Iodine Radioisotopes ; Iodine-123 ; Male ; Medical sciences ; Molecular Structure ; Nervous system ; Nicotinic acetylcholine receptor ; Papio ; Radiochemistry ; Radioligand Assay ; Radionuclide investigations ; Rats ; Rats, Sprague-Dawley ; Receptors, Nicotinic - analysis ; SPECT ; Tomography, Emission-Computed, Single-Photon - methods</subject><ispartof>Nuclear medicine and biology, 1999-02, Vol.26 (2), p.201-207</ispartof><rights>1999 Elsevier Science Inc.</rights><rights>1999 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c584t-314d8ccffbbc8132be897c34a91c90456bca0323dc43d33529dc2094ad2b176f3</citedby><cites>FETCH-LOGICAL-c584t-314d8ccffbbc8132be897c34a91c90456bca0323dc43d33529dc2094ad2b176f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0969-8051(98)00101-2$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3549,27923,27924,45994</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1699111$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10100220$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Musachio, John L.</creatorcontrib><creatorcontrib>Villemagne, Victor L.</creatorcontrib><creatorcontrib>Scheffel, Ursula A.</creatorcontrib><creatorcontrib>Dannals, Robert F.</creatorcontrib><creatorcontrib>Dogan, A.Semih</creatorcontrib><creatorcontrib>Yokoi, Fuji</creatorcontrib><creatorcontrib>Wong, Dean F.</creatorcontrib><title>Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon</title><title>Nuclear medicine and biology</title><addtitle>Nucl Med Biol</addtitle><description>A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (
S)-5-[
123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-IA, has been developed. The two-step sequence produced [
123I]-5-IA in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (>8,500 mCi/μmol). Preliminary single photon emission computed tomography studies with [
123I]-5-IA in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [
123I]-5-IA uptake in all brain regions (78–59% reduction), demonstrating the specificity of the radiotracer.</description><subject>Animals</subject><subject>Azetidines - chemical synthesis</subject><subject>Biological and medical sciences</subject><subject>Brain - diagnostic imaging</subject><subject>Investigative techniques, diagnostic techniques (general aspects)</subject><subject>Iodine Radioisotopes</subject><subject>Iodine-123</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Molecular Structure</subject><subject>Nervous system</subject><subject>Nicotinic acetylcholine receptor</subject><subject>Papio</subject><subject>Radiochemistry</subject><subject>Radioligand Assay</subject><subject>Radionuclide investigations</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptors, Nicotinic - analysis</subject><subject>SPECT</subject><subject>Tomography, Emission-Computed, Single-Photon - methods</subject><issn>0969-8051</issn><issn>1872-9614</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1LXDEUhkNp0fHjJ1SyKMUurs3XzSQrkUGrIFgYXYfck1xNuZNMkzuF-fdmPlB33eSEl-eckzwIfaXkghIqf86JlrpRpKXnWv0gpIYN-4QmVE1ZoyUVn9HkDTlER6X8qZAUlBygwwoTwhiZoH6-juOLL6Hg1GMb8V1DGa8XO6TnTXTVqJYrUhOHl9kPYRGizWs8_309e8RhYZ9D3IIxQBpDPXH24JdjygWHiDvbpRRP0JfeDsWf7usxerq5fpzdNvcPv-5mV_cNtEqMDafCKYC-7zpQlLPOKz0FLqymoIloZQeWcMYdCO44b5l2wIgW1rGOTmXPj9H33dxlTn9XvoxmEQr4YbDRp1UxUkvJhdYVbHcg5FRK9r1Z5vqZvDaUmI1gsxVsNvaMVmYr2LDad7ZfsOoW3n3o2hmtwLc9YAvYoc82QijvnNSaUlqxyx3mq41_wWdTIPgI3oWqbzQuhf-85BXo4pUI</recordid><startdate>19990201</startdate><enddate>19990201</enddate><creator>Musachio, John L.</creator><creator>Villemagne, Victor L.</creator><creator>Scheffel, Ursula A.</creator><creator>Dannals, Robert F.</creator><creator>Dogan, A.Semih</creator><creator>Yokoi, Fuji</creator><creator>Wong, Dean F.</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>19990201</creationdate><title>Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon</title><author>Musachio, John L. ; Villemagne, Victor L. ; Scheffel, Ursula A. ; Dannals, Robert F. ; Dogan, A.Semih ; Yokoi, Fuji ; Wong, Dean F.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c584t-314d8ccffbbc8132be897c34a91c90456bca0323dc43d33529dc2094ad2b176f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Animals</topic><topic>Azetidines - chemical synthesis</topic><topic>Biological and medical sciences</topic><topic>Brain - diagnostic imaging</topic><topic>Investigative techniques, diagnostic techniques (general aspects)</topic><topic>Iodine Radioisotopes</topic><topic>Iodine-123</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Molecular Structure</topic><topic>Nervous system</topic><topic>Nicotinic acetylcholine receptor</topic><topic>Papio</topic><topic>Radiochemistry</topic><topic>Radioligand Assay</topic><topic>Radionuclide investigations</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptors, Nicotinic - analysis</topic><topic>SPECT</topic><topic>Tomography, Emission-Computed, Single-Photon - methods</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Musachio, John L.</creatorcontrib><creatorcontrib>Villemagne, Victor L.</creatorcontrib><creatorcontrib>Scheffel, Ursula A.</creatorcontrib><creatorcontrib>Dannals, Robert F.</creatorcontrib><creatorcontrib>Dogan, A.Semih</creatorcontrib><creatorcontrib>Yokoi, Fuji</creatorcontrib><creatorcontrib>Wong, Dean F.</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>Musachio, John L.</au><au>Villemagne, Victor L.</au><au>Scheffel, Ursula A.</au><au>Dannals, Robert F.</au><au>Dogan, A.Semih</au><au>Yokoi, Fuji</au><au>Wong, Dean F.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon</atitle><jtitle>Nuclear medicine and biology</jtitle><addtitle>Nucl Med Biol</addtitle><date>1999-02-01</date><risdate>1999</risdate><volume>26</volume><issue>2</issue><spage>201</spage><epage>207</epage><pages>201-207</pages><issn>0969-8051</issn><eissn>1872-9614</eissn><abstract>A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (
S)-5-[
123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-IA, has been developed. The two-step sequence produced [
123I]-5-IA in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (>8,500 mCi/μmol). Preliminary single photon emission computed tomography studies with [
123I]-5-IA in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [
123I]-5-IA uptake in all brain regions (78–59% reduction), demonstrating the specificity of the radiotracer.</abstract><cop>Amsterdam</cop><pub>Elsevier Inc</pub><pmid>10100220</pmid><doi>10.1016/S0969-8051(98)00101-2</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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| language | eng |
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| subjects | Animals Azetidines - chemical synthesis Biological and medical sciences Brain - diagnostic imaging Investigative techniques, diagnostic techniques (general aspects) Iodine Radioisotopes Iodine-123 Male Medical sciences Molecular Structure Nervous system Nicotinic acetylcholine receptor Papio Radiochemistry Radioligand Assay Radionuclide investigations Rats Rats, Sprague-Dawley Receptors, Nicotinic - analysis SPECT Tomography, Emission-Computed, Single-Photon - methods |
| title | Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon |
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