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Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studies
Epibatidine analogues have been labelled with I-123 for single photon emission computed tomography and with short half-life positron emitters (C-11 and F-18) for PET. For easier radiopharmacological studies the bromo analogue of epibatidine (norchlorobromoepibatidine or exo-7-azabicyclo-2-(2-bromo-5...
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| Published in: | Applied radiation and isotopes 2002-11, Vol.57 (5), p.713-717 |
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| Main Authors: | , , , , , , , |
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| cited_by | cdi_FETCH-LOGICAL-c361t-25103f402d321e61f744bb93879e54c4fd60d63338b8899857eee4f72c1418833 |
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| cites | cdi_FETCH-LOGICAL-c361t-25103f402d321e61f744bb93879e54c4fd60d63338b8899857eee4f72c1418833 |
| container_end_page | 717 |
| container_issue | 5 |
| container_start_page | 713 |
| container_title | Applied radiation and isotopes |
| container_volume | 57 |
| creator | Kassiou, M Loc’h, C Dolle, F Musachio, J.L Dolci, L Crouzel, C Dannals, R.F Mazière, B |
| description | Epibatidine analogues have been labelled with I-123 for single photon emission computed tomography and with short half-life positron emitters (C-11 and F-18) for PET. For easier radiopharmacological studies the bromo analogue of epibatidine (norchlorobromoepibatidine or
exo-7-azabicyclo-2-(2-bromo-5-pyridyl)-[2.2.1]heptane) was labelled with Br-76, a longer half-life positron emitter, (
T
1/2=16.2
h). [
76Br]-norchlorobromoepibatidine was prepared by using a Cu
+ assisted bromodeiodination exchange from the iodo analogue in reducing conditions at 190°C. The tracer purified by RP-HPLC was obtained in 70% radiochemical yield with a specific radioactivity of 20
GBq/μmol. Radiochemical and chemical purities measured by radio-TLC and HPLC were >98%. |
| doi_str_mv | 10.1016/S0969-8043(02)00187-2 |
| format | article |
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exo-7-azabicyclo-2-(2-bromo-5-pyridyl)-[2.2.1]heptane) was labelled with Br-76, a longer half-life positron emitter, (
T
1/2=16.2
h). [
76Br]-norchlorobromoepibatidine was prepared by using a Cu
+ assisted bromodeiodination exchange from the iodo analogue in reducing conditions at 190°C. The tracer purified by RP-HPLC was obtained in 70% radiochemical yield with a specific radioactivity of 20
GBq/μmol. Radiochemical and chemical purities measured by radio-TLC and HPLC were >98%.</description><identifier>ISSN: 0969-8043</identifier><identifier>EISSN: 1872-9800</identifier><identifier>DOI: 10.1016/S0969-8043(02)00187-2</identifier><identifier>PMID: 12433046</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Animals ; Bridged Bicyclo Compounds, Heterocyclic - chemical synthesis ; Bridged Bicyclo Compounds, Heterocyclic - chemistry ; Bridged Bicyclo Compounds, Heterocyclic - metabolism ; Bromine Radioisotopes - isolation & purification ; Bromine-76 ; Epibatidine ; In Vitro Techniques ; Ligands ; Nicotinic acetylcholine receptors ; PET ; Pyridines - chemical synthesis ; Pyridines - chemistry ; Pyridines - metabolism ; Radiochemistry ; Radiopharmaceuticals - chemical synthesis ; Radiopharmaceuticals - chemistry ; Radiopharmaceuticals - metabolism ; Receptors, Nicotinic - metabolism ; Tomography, Emission-Computed</subject><ispartof>Applied radiation and isotopes, 2002-11, Vol.57 (5), p.713-717</ispartof><rights>2002 Elsevier Science Ltd</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c361t-25103f402d321e61f744bb93879e54c4fd60d63338b8899857eee4f72c1418833</citedby><cites>FETCH-LOGICAL-c361t-25103f402d321e61f744bb93879e54c4fd60d63338b8899857eee4f72c1418833</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12433046$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kassiou, M</creatorcontrib><creatorcontrib>Loc’h, C</creatorcontrib><creatorcontrib>Dolle, F</creatorcontrib><creatorcontrib>Musachio, J.L</creatorcontrib><creatorcontrib>Dolci, L</creatorcontrib><creatorcontrib>Crouzel, C</creatorcontrib><creatorcontrib>Dannals, R.F</creatorcontrib><creatorcontrib>Mazière, B</creatorcontrib><title>Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studies</title><title>Applied radiation and isotopes</title><addtitle>Appl Radiat Isot</addtitle><description>Epibatidine analogues have been labelled with I-123 for single photon emission computed tomography and with short half-life positron emitters (C-11 and F-18) for PET. For easier radiopharmacological studies the bromo analogue of epibatidine (norchlorobromoepibatidine or
exo-7-azabicyclo-2-(2-bromo-5-pyridyl)-[2.2.1]heptane) was labelled with Br-76, a longer half-life positron emitter, (
T
1/2=16.2
h). [
76Br]-norchlorobromoepibatidine was prepared by using a Cu
+ assisted bromodeiodination exchange from the iodo analogue in reducing conditions at 190°C. The tracer purified by RP-HPLC was obtained in 70% radiochemical yield with a specific radioactivity of 20
GBq/μmol. Radiochemical and chemical purities measured by radio-TLC and HPLC were >98%.</description><subject>Animals</subject><subject>Bridged Bicyclo Compounds, Heterocyclic - chemical synthesis</subject><subject>Bridged Bicyclo Compounds, Heterocyclic - chemistry</subject><subject>Bridged Bicyclo Compounds, Heterocyclic - metabolism</subject><subject>Bromine Radioisotopes - isolation & purification</subject><subject>Bromine-76</subject><subject>Epibatidine</subject><subject>In Vitro Techniques</subject><subject>Ligands</subject><subject>Nicotinic acetylcholine receptors</subject><subject>PET</subject><subject>Pyridines - chemical synthesis</subject><subject>Pyridines - chemistry</subject><subject>Pyridines - metabolism</subject><subject>Radiochemistry</subject><subject>Radiopharmaceuticals - chemical synthesis</subject><subject>Radiopharmaceuticals - chemistry</subject><subject>Radiopharmaceuticals - metabolism</subject><subject>Receptors, Nicotinic - metabolism</subject><subject>Tomography, Emission-Computed</subject><issn>0969-8043</issn><issn>1872-9800</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><recordid>eNqF0M9vFCEUwHFiNHZb_RM0nIwexj5-LANejGmsNmliE_VMGHhTMbPDCIxJ_etluxs99gKXD7y8LyEvGLxlwNT5VzDKdBqkeA38DQDTfccfkU27eWc0wGOy-UdOyGkpPwFAasOfkhPGpRAg1Yb8ucm4uOxqTDNNI3V0yGkXZ-x6RSc34DRhoG52U7pdcS9wiUPjoZl3jS-p4lzpFG_dHOiYMp2jTzW2kzqP9W7yP9LUMM3ocakNlLqGiOUZeTK6qeDz431Gvl9-_Hbxubv-8unq4sN154ViteNbBmKUwIPgDBUbeymHwQjdG9xKL8egICghhB60NkZve0SUY889k0xrIc7Iq8O_S06_VizV7mLxbTE3Y1qL7bkyrShvcHuAPqdSMo52yXHn8p1lYPfR7X10uy9qgdv76Hb_7uVxwDrsMPx_dazcwPsDwLbm74jZFh9x9hhii1JtSPGBEX8BKhiRvQ</recordid><startdate>20021101</startdate><enddate>20021101</enddate><creator>Kassiou, M</creator><creator>Loc’h, C</creator><creator>Dolle, F</creator><creator>Musachio, J.L</creator><creator>Dolci, L</creator><creator>Crouzel, C</creator><creator>Dannals, R.F</creator><creator>Mazière, B</creator><general>Elsevier Ltd</general><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>20021101</creationdate><title>Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studies</title><author>Kassiou, M ; Loc’h, C ; Dolle, F ; Musachio, J.L ; Dolci, L ; Crouzel, C ; Dannals, R.F ; Mazière, B</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c361t-25103f402d321e61f744bb93879e54c4fd60d63338b8899857eee4f72c1418833</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Animals</topic><topic>Bridged Bicyclo Compounds, Heterocyclic - chemical synthesis</topic><topic>Bridged Bicyclo Compounds, Heterocyclic - chemistry</topic><topic>Bridged Bicyclo Compounds, Heterocyclic - metabolism</topic><topic>Bromine Radioisotopes - isolation & purification</topic><topic>Bromine-76</topic><topic>Epibatidine</topic><topic>In Vitro Techniques</topic><topic>Ligands</topic><topic>Nicotinic acetylcholine receptors</topic><topic>PET</topic><topic>Pyridines - chemical synthesis</topic><topic>Pyridines - chemistry</topic><topic>Pyridines - metabolism</topic><topic>Radiochemistry</topic><topic>Radiopharmaceuticals - chemical synthesis</topic><topic>Radiopharmaceuticals - chemistry</topic><topic>Radiopharmaceuticals - metabolism</topic><topic>Receptors, Nicotinic - metabolism</topic><topic>Tomography, Emission-Computed</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kassiou, M</creatorcontrib><creatorcontrib>Loc’h, C</creatorcontrib><creatorcontrib>Dolle, F</creatorcontrib><creatorcontrib>Musachio, J.L</creatorcontrib><creatorcontrib>Dolci, L</creatorcontrib><creatorcontrib>Crouzel, C</creatorcontrib><creatorcontrib>Dannals, R.F</creatorcontrib><creatorcontrib>Mazière, B</creatorcontrib><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>Applied radiation and isotopes</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kassiou, M</au><au>Loc’h, C</au><au>Dolle, F</au><au>Musachio, J.L</au><au>Dolci, L</au><au>Crouzel, C</au><au>Dannals, R.F</au><au>Mazière, B</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studies</atitle><jtitle>Applied radiation and isotopes</jtitle><addtitle>Appl Radiat Isot</addtitle><date>2002-11-01</date><risdate>2002</risdate><volume>57</volume><issue>5</issue><spage>713</spage><epage>717</epage><pages>713-717</pages><issn>0969-8043</issn><eissn>1872-9800</eissn><abstract>Epibatidine analogues have been labelled with I-123 for single photon emission computed tomography and with short half-life positron emitters (C-11 and F-18) for PET. For easier radiopharmacological studies the bromo analogue of epibatidine (norchlorobromoepibatidine or
exo-7-azabicyclo-2-(2-bromo-5-pyridyl)-[2.2.1]heptane) was labelled with Br-76, a longer half-life positron emitter, (
T
1/2=16.2
h). [
76Br]-norchlorobromoepibatidine was prepared by using a Cu
+ assisted bromodeiodination exchange from the iodo analogue in reducing conditions at 190°C. The tracer purified by RP-HPLC was obtained in 70% radiochemical yield with a specific radioactivity of 20
GBq/μmol. Radiochemical and chemical purities measured by radio-TLC and HPLC were >98%.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>12433046</pmid><doi>10.1016/S0969-8043(02)00187-2</doi><tpages>5</tpages></addata></record> |
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| ispartof | Applied radiation and isotopes, 2002-11, Vol.57 (5), p.713-717 |
| issn | 0969-8043 1872-9800 |
| language | eng |
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| source | ScienceDirect Journals |
| subjects | Animals Bridged Bicyclo Compounds, Heterocyclic - chemical synthesis Bridged Bicyclo Compounds, Heterocyclic - chemistry Bridged Bicyclo Compounds, Heterocyclic - metabolism Bromine Radioisotopes - isolation & purification Bromine-76 Epibatidine In Vitro Techniques Ligands Nicotinic acetylcholine receptors PET Pyridines - chemical synthesis Pyridines - chemistry Pyridines - metabolism Radiochemistry Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - chemistry Radiopharmaceuticals - metabolism Receptors, Nicotinic - metabolism Tomography, Emission-Computed |
| title | Preparation of a bromine-76 labelled analogue of epibatidine: a potent ligand for nicotinic acetylcholine receptor studies |
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