Evaluation of [ 125I]7α-O-iodoallyl diprenophine as a new potential spect opioid receptor imaging agent
A new iodinated diprenorphine analog, [ 125I]7α-O-iodoallyl diprenorphine ([ 125I]7α-O-IA-DPN), was prepared by iododestannylation and characterized. As an opioid antagonist, this agent showed very high affinity (K i = 0.4 ± 0.2 nM) and 63% of specific binding by in vitro and in vivo binding studies...
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| Veröffentlicht in: | Nuclear medicine and biology 1997-08, Vol.24 (6), p.553-558 |
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| container_title | Nuclear medicine and biology |
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| creator | Wang, R.F. Tafani, J.A.M. Francés, B. Bergon, M. Coulais, Y. Zajac, J.M. Guiraud, R. |
| description | A new iodinated diprenorphine analog, [
125I]7α-O-iodoallyl diprenorphine ([
125I]7α-O-IA-DPN), was prepared by iododestannylation and characterized. As an opioid antagonist, this agent showed very high affinity (K
i = 0.4 ± 0.2 nM) and 63% of specific binding by
in vitro and
in vivo binding studies. Inhibition curves indicated that this tracer labeled with the same affinities to three opioid receptors (μ = δ = κ). The findings demonstrate that this proposed compound appears to be a potential radioprobe for future study of opioid receptors by
in vivo SPECT. |
| doi_str_mv | 10.1016/S0969-8051(97)00068-1 |
| format | Article |
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125I]7α-O-iodoallyl diprenorphine ([
125I]7α-O-IA-DPN), was prepared by iododestannylation and characterized. As an opioid antagonist, this agent showed very high affinity (K
i = 0.4 ± 0.2 nM) and 63% of specific binding by
in vitro and
in vivo binding studies. Inhibition curves indicated that this tracer labeled with the same affinities to three opioid receptors (μ = δ = κ). The findings demonstrate that this proposed compound appears to be a potential radioprobe for future study of opioid receptors by
in vivo SPECT.</description><identifier>ISSN: 0969-8051</identifier><identifier>EISSN: 1872-9614</identifier><identifier>DOI: 10.1016/S0969-8051(97)00068-1</identifier><identifier>PMID: 9316084</identifier><language>eng</language><publisher>Amsterdam: Elsevier Inc</publisher><subject>7α-O-IA-DPN ; Animals ; Binding assay ; Biological and medical sciences ; Brain - metabolism ; Contrast media. Radiopharmaceuticals ; Diprenorphine ; Diprenorphine - analogs & derivatives ; Imaging agent ; Iodine Radioisotopes ; Male ; Medical sciences ; Mice ; Multiple opioid receptors ; Narcotic Antagonists ; Pharmacology. Drug treatments ; Rats ; Rats, Wistar ; Receptors, Opioid - analysis ; SPECT ; Tissue Distribution ; Tomography, Emission-Computed, Single-Photon</subject><ispartof>Nuclear medicine and biology, 1997-08, Vol.24 (6), p.553-558</ispartof><rights>1997</rights><rights>1997 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c389t-506ebf761248a17a4b87566934351b3187aa564aef5e22b26604a8610d4a0f383</citedby><cites>FETCH-LOGICAL-c389t-506ebf761248a17a4b87566934351b3187aa564aef5e22b26604a8610d4a0f383</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(97)00068-1$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,27923,27924,45994</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2810212$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9316084$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Wang, R.F.</creatorcontrib><creatorcontrib>Tafani, J.A.M.</creatorcontrib><creatorcontrib>Francés, B.</creatorcontrib><creatorcontrib>Bergon, M.</creatorcontrib><creatorcontrib>Coulais, Y.</creatorcontrib><creatorcontrib>Zajac, J.M.</creatorcontrib><creatorcontrib>Guiraud, R.</creatorcontrib><title>Evaluation of [ 125I]7α-O-iodoallyl diprenophine as a new potential spect opioid receptor imaging agent</title><title>Nuclear medicine and biology</title><addtitle>Nucl Med Biol</addtitle><description>A new iodinated diprenorphine analog, [
125I]7α-O-iodoallyl diprenorphine ([
125I]7α-O-IA-DPN), was prepared by iododestannylation and characterized. As an opioid antagonist, this agent showed very high affinity (K
i = 0.4 ± 0.2 nM) and 63% of specific binding by
in vitro and
in vivo binding studies. Inhibition curves indicated that this tracer labeled with the same affinities to three opioid receptors (μ = δ = κ). The findings demonstrate that this proposed compound appears to be a potential radioprobe for future study of opioid receptors by
in vivo SPECT.</description><subject>7α-O-IA-DPN</subject><subject>Animals</subject><subject>Binding assay</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Contrast media. Radiopharmaceuticals</subject><subject>Diprenorphine</subject><subject>Diprenorphine - analogs & derivatives</subject><subject>Imaging agent</subject><subject>Iodine Radioisotopes</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Multiple opioid receptors</subject><subject>Narcotic Antagonists</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, Opioid - analysis</subject><subject>SPECT</subject><subject>Tissue Distribution</subject><subject>Tomography, Emission-Computed, Single-Photon</subject><issn>0969-8051</issn><issn>1872-9614</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1997</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkM9u1DAQhy0EKtvCI1TyASF6CNiO7dgnhKoClSr1AJwQsibOZGvktYOdLepj8SI8E9nuaq-c5jDfb_58hJxz9pYzrt99YVbbxjDF39jugjGmTcOfkBU3nWis5vIpWR2R5-S01p9syUnOTsiJbblmRq7I3dU9xC3MISeaR_qdcqGuf3R__zS3TchDhhgfIh3CVDDl6S4kpFAp0IS_6ZRnTHOASOuEfqZ5CjkMtKDHac6Fhg2sQ1pTWC_YC_JshFjx5aGekW8fr75efm5ubj9dX364aXxr7NwoprEfO82FNMA7kL3plNa2la3ifbs8B6C0BBwVCtELrZkEozkbJLCxNe0Zeb2fO5X8a4t1dptQPcYICfO2us62QikpFlDtQV9yrQVHN5Xl4vLgOHM7w-7RsNvpc7Zzj4YdX3LnhwXbfoPDMXVQuvRfHfpQPcSxQPKhHjFhOBN8t_79HsNFxn3A4qoPmDwOYRE4uyGH_xzyD666lyc</recordid><startdate>19970801</startdate><enddate>19970801</enddate><creator>Wang, R.F.</creator><creator>Tafani, J.A.M.</creator><creator>Francés, B.</creator><creator>Bergon, M.</creator><creator>Coulais, Y.</creator><creator>Zajac, J.M.</creator><creator>Guiraud, R.</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>19970801</creationdate><title>Evaluation of [ 125I]7α-O-iodoallyl diprenophine as a new potential spect opioid receptor imaging agent</title><author>Wang, R.F. ; Tafani, J.A.M. ; Francés, B. ; Bergon, M. ; Coulais, Y. ; Zajac, J.M. ; Guiraud, R.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c389t-506ebf761248a17a4b87566934351b3187aa564aef5e22b26604a8610d4a0f383</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1997</creationdate><topic>7α-O-IA-DPN</topic><topic>Animals</topic><topic>Binding assay</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Contrast media. Radiopharmaceuticals</topic><topic>Diprenorphine</topic><topic>Diprenorphine - analogs & derivatives</topic><topic>Imaging agent</topic><topic>Iodine Radioisotopes</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Multiple opioid receptors</topic><topic>Narcotic Antagonists</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Receptors, Opioid - analysis</topic><topic>SPECT</topic><topic>Tissue Distribution</topic><topic>Tomography, Emission-Computed, Single-Photon</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Wang, R.F.</creatorcontrib><creatorcontrib>Tafani, J.A.M.</creatorcontrib><creatorcontrib>Francés, B.</creatorcontrib><creatorcontrib>Bergon, M.</creatorcontrib><creatorcontrib>Coulais, Y.</creatorcontrib><creatorcontrib>Zajac, J.M.</creatorcontrib><creatorcontrib>Guiraud, R.</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>Wang, R.F.</au><au>Tafani, J.A.M.</au><au>Francés, B.</au><au>Bergon, M.</au><au>Coulais, Y.</au><au>Zajac, J.M.</au><au>Guiraud, R.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evaluation of [ 125I]7α-O-iodoallyl diprenophine as a new potential spect opioid receptor imaging agent</atitle><jtitle>Nuclear medicine and biology</jtitle><addtitle>Nucl Med Biol</addtitle><date>1997-08-01</date><risdate>1997</risdate><volume>24</volume><issue>6</issue><spage>553</spage><epage>558</epage><pages>553-558</pages><issn>0969-8051</issn><eissn>1872-9614</eissn><abstract>A new iodinated diprenorphine analog, [
125I]7α-O-iodoallyl diprenorphine ([
125I]7α-O-IA-DPN), was prepared by iododestannylation and characterized. As an opioid antagonist, this agent showed very high affinity (K
i = 0.4 ± 0.2 nM) and 63% of specific binding by
in vitro and
in vivo binding studies. Inhibition curves indicated that this tracer labeled with the same affinities to three opioid receptors (μ = δ = κ). The findings demonstrate that this proposed compound appears to be a potential radioprobe for future study of opioid receptors by
in vivo SPECT.</abstract><cop>Amsterdam</cop><pub>Elsevier Inc</pub><pmid>9316084</pmid><doi>10.1016/S0969-8051(97)00068-1</doi><tpages>6</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0969-8051 |
| ispartof | Nuclear medicine and biology, 1997-08, Vol.24 (6), p.553-558 |
| issn | 0969-8051 1872-9614 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_79325542 |
| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | 7α-O-IA-DPN Animals Binding assay Biological and medical sciences Brain - metabolism Contrast media. Radiopharmaceuticals Diprenorphine Diprenorphine - analogs & derivatives Imaging agent Iodine Radioisotopes Male Medical sciences Mice Multiple opioid receptors Narcotic Antagonists Pharmacology. Drug treatments Rats Rats, Wistar Receptors, Opioid - analysis SPECT Tissue Distribution Tomography, Emission-Computed, Single-Photon |
| title | Evaluation of [ 125I]7α-O-iodoallyl diprenophine as a new potential spect opioid receptor imaging agent |
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