First no‐carrier‐added radioselenation of an adenosine‐A 1 receptor ligand
The precursor synthesis and the no‐carrier‐added (n.c.a.) radiosynthesis of the adenosine‐A 1 receptor ligand 5′‐(methyl[ 75 Se]seleno)‐ N 6 ‐cyclopentyladenosine ([ 75 Se] 1 ) are described in this report. A method was developed starting from elemental n.c.a. selenium‐75, followed by a three‐step p...
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| Veröffentlicht in: | Journal of labelled compounds & radiopharmaceuticals 2004-06, Vol.47 (7), p.415-427 |
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| container_title | Journal of labelled compounds & radiopharmaceuticals |
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| creator | Blum, Till Ermert, Johannes Wutz, Walter Bier, Dirk Coenen, Heinz H. |
| description | The precursor synthesis and the no‐carrier‐added (n.c.a.) radiosynthesis of the adenosine‐A
1
receptor ligand 5′‐(methyl[
75
Se]seleno)‐
N
6
‐cyclopentyladenosine ([
75
Se]
1
) are described in this report. A method was developed starting from elemental n.c.a. selenium‐75, followed by a three‐step polymer‐supported radioselenation and deprotection which gave the radioligand with a radiochemical yield of 30%, a radiochemical purity of > 99% and a specific radioactivity of > 300 GBq/mmol (8 Ci/mmol). Preparation time was 40 min. The nonradioactive compound 5′‐(methylseleno)‐
N
6
‐cyclopentyladenosine (
1
) was pharmacologically evaluated
in vitro
and showed high affinity and selectivity for the adenosine‐A
1
receptor. These preliminary results suggest that this compound could be a useful radioligand for the noninvasive imaging of the brain adenosine‐A
1
receptors using positron emission tomography (PET) when labelled with the positron emitter selenium‐73 (half‐life: 7.1 h). Copyright © 2004 John Wiley & Sons, Ltd. |
| doi_str_mv | 10.1002/jlcr.829 |
| format | Article |
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1
receptor ligand 5′‐(methyl[
75
Se]seleno)‐
N
6
‐cyclopentyladenosine ([
75
Se]
1
) are described in this report. A method was developed starting from elemental n.c.a. selenium‐75, followed by a three‐step polymer‐supported radioselenation and deprotection which gave the radioligand with a radiochemical yield of 30%, a radiochemical purity of > 99% and a specific radioactivity of > 300 GBq/mmol (8 Ci/mmol). Preparation time was 40 min. The nonradioactive compound 5′‐(methylseleno)‐
N
6
‐cyclopentyladenosine (
1
) was pharmacologically evaluated
in vitro
and showed high affinity and selectivity for the adenosine‐A
1
receptor. These preliminary results suggest that this compound could be a useful radioligand for the noninvasive imaging of the brain adenosine‐A
1
receptors using positron emission tomography (PET) when labelled with the positron emitter selenium‐73 (half‐life: 7.1 h). Copyright © 2004 John Wiley & Sons, Ltd.</description><identifier>ISSN: 0362-4803</identifier><identifier>EISSN: 1099-1344</identifier><identifier>DOI: 10.1002/jlcr.829</identifier><language>eng</language><ispartof>Journal of labelled compounds & radiopharmaceuticals, 2004-06, Vol.47 (7), p.415-427</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c729-bf23e518639d7957407a59f502b74e6ffbc9b15f6c94194c405c2ada091b3e03</citedby><cites>FETCH-LOGICAL-c729-bf23e518639d7957407a59f502b74e6ffbc9b15f6c94194c405c2ada091b3e03</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27922,27923</link.rule.ids></links><search><creatorcontrib>Blum, Till</creatorcontrib><creatorcontrib>Ermert, Johannes</creatorcontrib><creatorcontrib>Wutz, Walter</creatorcontrib><creatorcontrib>Bier, Dirk</creatorcontrib><creatorcontrib>Coenen, Heinz H.</creatorcontrib><title>First no‐carrier‐added radioselenation of an adenosine‐A 1 receptor ligand</title><title>Journal of labelled compounds & radiopharmaceuticals</title><description>The precursor synthesis and the no‐carrier‐added (n.c.a.) radiosynthesis of the adenosine‐A
1
receptor ligand 5′‐(methyl[
75
Se]seleno)‐
N
6
‐cyclopentyladenosine ([
75
Se]
1
) are described in this report. A method was developed starting from elemental n.c.a. selenium‐75, followed by a three‐step polymer‐supported radioselenation and deprotection which gave the radioligand with a radiochemical yield of 30%, a radiochemical purity of > 99% and a specific radioactivity of > 300 GBq/mmol (8 Ci/mmol). Preparation time was 40 min. The nonradioactive compound 5′‐(methylseleno)‐
N
6
‐cyclopentyladenosine (
1
) was pharmacologically evaluated
in vitro
and showed high affinity and selectivity for the adenosine‐A
1
receptor. These preliminary results suggest that this compound could be a useful radioligand for the noninvasive imaging of the brain adenosine‐A
1
receptors using positron emission tomography (PET) when labelled with the positron emitter selenium‐73 (half‐life: 7.1 h). Copyright © 2004 John Wiley & Sons, Ltd.</description><issn>0362-4803</issn><issn>1099-1344</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><recordid>eNotkM1KAzEUhYMoWKvgI2TpZurNz_xkWYq1QkFB90MmuZGUMSk3s3HnI_iMPolTdHUOnI-z-Bi7FbASAPL-MDpaddKcsYUAYyqhtD5nC1CNrHQH6pJdlXIAmDetF-xlG6lMPOWfr29niSLS3Kz36DlZH3PBEZOdYk48B24Ttx5TLjHhzK254IQOj1MmPsZ3m_w1uwh2LHjzn0v2un142-yq_fPj02a9r1wrTTUEqbAWXaOMb03damhtbUINcmg1NiEMzgyiDo0zWhjtNNROWm_BiEEhqCW7-3t1lEshDP2R4oelz15Af_LQnzz0swf1C2UvU7s</recordid><startdate>200406</startdate><enddate>200406</enddate><creator>Blum, Till</creator><creator>Ermert, Johannes</creator><creator>Wutz, Walter</creator><creator>Bier, Dirk</creator><creator>Coenen, Heinz H.</creator><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>200406</creationdate><title>First no‐carrier‐added radioselenation of an adenosine‐A 1 receptor ligand</title><author>Blum, Till ; Ermert, Johannes ; Wutz, Walter ; Bier, Dirk ; Coenen, Heinz H.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c729-bf23e518639d7957407a59f502b74e6ffbc9b15f6c94194c405c2ada091b3e03</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Blum, Till</creatorcontrib><creatorcontrib>Ermert, Johannes</creatorcontrib><creatorcontrib>Wutz, Walter</creatorcontrib><creatorcontrib>Bier, Dirk</creatorcontrib><creatorcontrib>Coenen, Heinz H.</creatorcontrib><collection>CrossRef</collection><jtitle>Journal of labelled compounds & radiopharmaceuticals</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Blum, Till</au><au>Ermert, Johannes</au><au>Wutz, Walter</au><au>Bier, Dirk</au><au>Coenen, Heinz H.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>First no‐carrier‐added radioselenation of an adenosine‐A 1 receptor ligand</atitle><jtitle>Journal of labelled compounds & radiopharmaceuticals</jtitle><date>2004-06</date><risdate>2004</risdate><volume>47</volume><issue>7</issue><spage>415</spage><epage>427</epage><pages>415-427</pages><issn>0362-4803</issn><eissn>1099-1344</eissn><abstract>The precursor synthesis and the no‐carrier‐added (n.c.a.) radiosynthesis of the adenosine‐A
1
receptor ligand 5′‐(methyl[
75
Se]seleno)‐
N
6
‐cyclopentyladenosine ([
75
Se]
1
) are described in this report. A method was developed starting from elemental n.c.a. selenium‐75, followed by a three‐step polymer‐supported radioselenation and deprotection which gave the radioligand with a radiochemical yield of 30%, a radiochemical purity of > 99% and a specific radioactivity of > 300 GBq/mmol (8 Ci/mmol). Preparation time was 40 min. The nonradioactive compound 5′‐(methylseleno)‐
N
6
‐cyclopentyladenosine (
1
) was pharmacologically evaluated
in vitro
and showed high affinity and selectivity for the adenosine‐A
1
receptor. These preliminary results suggest that this compound could be a useful radioligand for the noninvasive imaging of the brain adenosine‐A
1
receptors using positron emission tomography (PET) when labelled with the positron emitter selenium‐73 (half‐life: 7.1 h). Copyright © 2004 John Wiley & Sons, Ltd.</abstract><doi>10.1002/jlcr.829</doi><tpages>13</tpages></addata></record> |
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| identifier | ISSN: 0362-4803 |
| ispartof | Journal of labelled compounds & radiopharmaceuticals, 2004-06, Vol.47 (7), p.415-427 |
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| language | eng |
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| source | Wiley Online Library Journals Frontfile Complete |
| title | First no‐carrier‐added radioselenation of an adenosine‐A 1 receptor ligand |
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