Synthesis and Evaluation of [ 123I]-Iodo-PK11195 for Mapping Peripheral-Type Benzodiazepine Receptors (ω 3) in Heart
An iodinated analog of PK11195, 1-(2-chlorophenyl)- N-methyl- N-(1-methylpropyl)isoquinoline-3-carboxamide, a specific antagonist of the peripheral-type benzodiazepine receptor (ω 3), has been synthesized in three steps with an overall chemical yield of 40%. Both [ 123I]- and [ 125I]-Iodo-PK11195 ha...
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| Veröffentlicht in: | Nuclear medicine and biology 1996, Vol.23 (1), p.23-28 |
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| creator | Gildersleeve, David L. Van Dort, Marcian E. Johnson, Jon W. Sherman, Phillip S. Wieland, Donald M. |
| description | An iodinated analog of PK11195, 1-(2-chlorophenyl)-
N-methyl-
N-(1-methylpropyl)isoquinoline-3-carboxamide, a specific antagonist of the peripheral-type benzodiazepine receptor (ω
3), has been synthesized in three steps with an overall chemical yield of 40%. Both [
123I]- and [
125I]-Iodo-PK11195 have been synthesized by solid-state isotopic exchange in >60% isolated radiochemical yield and specific activity of 233–348 mCi/mmol. Tissue distribution studies in rats indicate a high uptake of radioactivity in adrenal glands, heart, lung and kidneys, which was blocked 63–87% by preadministration of cold PK11195. Single photon emission computer tomography (SPECT) imaging of the canine heart has been accomplished with [
123I]PK11195. These results suggest that [
123I]PK11195 has potential as a SPECT radiotracer for studying the ω
3 receptor in humans. |
| doi_str_mv | 10.1016/0969-8051(95)02007-1 |
| format | Article |
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N-methyl-
N-(1-methylpropyl)isoquinoline-3-carboxamide, a specific antagonist of the peripheral-type benzodiazepine receptor (ω
3), has been synthesized in three steps with an overall chemical yield of 40%. Both [
123I]- and [
125I]-Iodo-PK11195 have been synthesized by solid-state isotopic exchange in >60% isolated radiochemical yield and specific activity of 233–348 mCi/mmol. Tissue distribution studies in rats indicate a high uptake of radioactivity in adrenal glands, heart, lung and kidneys, which was blocked 63–87% by preadministration of cold PK11195. Single photon emission computer tomography (SPECT) imaging of the canine heart has been accomplished with [
123I]PK11195. These results suggest that [
123I]PK11195 has potential as a SPECT radiotracer for studying the ω
3 receptor in humans.</description><identifier>ISSN: 0969-8051</identifier><identifier>EISSN: 1872-9614</identifier><identifier>DOI: 10.1016/0969-8051(95)02007-1</identifier><identifier>PMID: 9004910</identifier><language>eng</language><publisher>United States: Elsevier Inc</publisher><subject>Animals ; Chromatography, High Pressure Liquid ; Chromatography, Thin Layer ; Dog ; Dogs ; Emission-computed tomography ; Female ; Heart - diagnostic imaging ; In Vitro Techniques ; Iodine Radioisotopes ; Isoquinolines ; Isoquinolines - chemical synthesis ; Isoquinolines - pharmacokinetics ; Isotope Labeling ; Male ; Mitochondrial benzodiazepine receptor ; Myocardium - metabolism ; Rat ; Rats ; Rats, Sprague-Dawley ; Receptors, GABA-A - drug effects ; Tissue Distribution ; Tomography, Emission-Computed, Single-Photon</subject><ispartof>Nuclear medicine and biology, 1996, Vol.23 (1), p.23-28</ispartof><rights>1996</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c357t-6f39ce05721b08c914209f29ec6828a1ccc6c1485f93ebb957d2023de70ecee43</citedby><cites>FETCH-LOGICAL-c357t-6f39ce05721b08c914209f29ec6828a1ccc6c1485f93ebb957d2023de70ecee43</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0969-8051(95)02007-1$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,4024,27923,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9004910$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Gildersleeve, David L.</creatorcontrib><creatorcontrib>Van Dort, Marcian E.</creatorcontrib><creatorcontrib>Johnson, Jon W.</creatorcontrib><creatorcontrib>Sherman, Phillip S.</creatorcontrib><creatorcontrib>Wieland, Donald M.</creatorcontrib><title>Synthesis and Evaluation of [ 123I]-Iodo-PK11195 for Mapping Peripheral-Type Benzodiazepine Receptors (ω 3) in Heart</title><title>Nuclear medicine and biology</title><addtitle>Nucl Med Biol</addtitle><description>An iodinated analog of PK11195, 1-(2-chlorophenyl)-
N-methyl-
N-(1-methylpropyl)isoquinoline-3-carboxamide, a specific antagonist of the peripheral-type benzodiazepine receptor (ω
3), has been synthesized in three steps with an overall chemical yield of 40%. Both [
123I]- and [
125I]-Iodo-PK11195 have been synthesized by solid-state isotopic exchange in >60% isolated radiochemical yield and specific activity of 233–348 mCi/mmol. Tissue distribution studies in rats indicate a high uptake of radioactivity in adrenal glands, heart, lung and kidneys, which was blocked 63–87% by preadministration of cold PK11195. Single photon emission computer tomography (SPECT) imaging of the canine heart has been accomplished with [
123I]PK11195. These results suggest that [
123I]PK11195 has potential as a SPECT radiotracer for studying the ω
3 receptor in humans.</description><subject>Animals</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Chromatography, Thin Layer</subject><subject>Dog</subject><subject>Dogs</subject><subject>Emission-computed tomography</subject><subject>Female</subject><subject>Heart - diagnostic imaging</subject><subject>In Vitro Techniques</subject><subject>Iodine Radioisotopes</subject><subject>Isoquinolines</subject><subject>Isoquinolines - chemical synthesis</subject><subject>Isoquinolines - pharmacokinetics</subject><subject>Isotope Labeling</subject><subject>Male</subject><subject>Mitochondrial benzodiazepine receptor</subject><subject>Myocardium - metabolism</subject><subject>Rat</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptors, GABA-A - drug effects</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>1996</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kM1O3DAQxy1ERbe0b0Aln9BycDvjfPqCBIjCqlRFLZwQsrzOBIyycbATpOUNeLq-UrPsiiOnOfy_ND_G9hC-IWD-HVSuRAkZTlV2ABKgELjFJlgWUqgc0202ebN8ZJ9ifIAxliLssB0FkCqECRv-Ltv-nqKL3LQVP30yzWB651vua37DUSazWzHzlReXPxFRZbz2gf8yXefaO35JwXX3FEwjrpYd8WNqn33lzDONMvE_ZKnrfYh8-u-FJwfctfycTOg_sw-1aSJ92dxddv3j9OrkXFz8PpudHF0Im2RFL_I6UZYgKyTOobQKUwmqlopsXsrSoLU2t5iWWa0Sms9VVlQSZFJRAeMypcku21_3dsE_DhR7vXDRUtOYlvwQdVFCmo8sRmO6NtrgYwxU6y64hQlLjaBXtPUKpV6h1CrTr7Q1jrGvm_5hvqDqLbTBO-qHa53GJ58cBR2to9ZS5QLZXlfevT_wH20djPk</recordid><startdate>1996</startdate><enddate>1996</enddate><creator>Gildersleeve, David L.</creator><creator>Van Dort, Marcian E.</creator><creator>Johnson, Jon W.</creator><creator>Sherman, Phillip S.</creator><creator>Wieland, Donald M.</creator><general>Elsevier Inc</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>1996</creationdate><title>Synthesis and Evaluation of [ 123I]-Iodo-PK11195 for Mapping Peripheral-Type Benzodiazepine Receptors (ω 3) in Heart</title><author>Gildersleeve, David L. ; Van Dort, Marcian E. ; Johnson, Jon W. ; Sherman, Phillip S. ; Wieland, Donald M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c357t-6f39ce05721b08c914209f29ec6828a1ccc6c1485f93ebb957d2023de70ecee43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1996</creationdate><topic>Animals</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Chromatography, Thin Layer</topic><topic>Dog</topic><topic>Dogs</topic><topic>Emission-computed tomography</topic><topic>Female</topic><topic>Heart - diagnostic imaging</topic><topic>In Vitro Techniques</topic><topic>Iodine Radioisotopes</topic><topic>Isoquinolines</topic><topic>Isoquinolines - chemical synthesis</topic><topic>Isoquinolines - pharmacokinetics</topic><topic>Isotope Labeling</topic><topic>Male</topic><topic>Mitochondrial benzodiazepine receptor</topic><topic>Myocardium - metabolism</topic><topic>Rat</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptors, GABA-A - drug effects</topic><topic>Tissue Distribution</topic><topic>Tomography, Emission-Computed, Single-Photon</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Gildersleeve, David L.</creatorcontrib><creatorcontrib>Van Dort, Marcian E.</creatorcontrib><creatorcontrib>Johnson, Jon W.</creatorcontrib><creatorcontrib>Sherman, Phillip S.</creatorcontrib><creatorcontrib>Wieland, Donald M.</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>Nuclear medicine and biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Gildersleeve, David L.</au><au>Van Dort, Marcian E.</au><au>Johnson, Jon W.</au><au>Sherman, Phillip S.</au><au>Wieland, Donald M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and Evaluation of [ 123I]-Iodo-PK11195 for Mapping Peripheral-Type Benzodiazepine Receptors (ω 3) in Heart</atitle><jtitle>Nuclear medicine and biology</jtitle><addtitle>Nucl Med Biol</addtitle><date>1996</date><risdate>1996</risdate><volume>23</volume><issue>1</issue><spage>23</spage><epage>28</epage><pages>23-28</pages><issn>0969-8051</issn><eissn>1872-9614</eissn><abstract>An iodinated analog of PK11195, 1-(2-chlorophenyl)-
N-methyl-
N-(1-methylpropyl)isoquinoline-3-carboxamide, a specific antagonist of the peripheral-type benzodiazepine receptor (ω
3), has been synthesized in three steps with an overall chemical yield of 40%. Both [
123I]- and [
125I]-Iodo-PK11195 have been synthesized by solid-state isotopic exchange in >60% isolated radiochemical yield and specific activity of 233–348 mCi/mmol. Tissue distribution studies in rats indicate a high uptake of radioactivity in adrenal glands, heart, lung and kidneys, which was blocked 63–87% by preadministration of cold PK11195. Single photon emission computer tomography (SPECT) imaging of the canine heart has been accomplished with [
123I]PK11195. These results suggest that [
123I]PK11195 has potential as a SPECT radiotracer for studying the ω
3 receptor in humans.</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>9004910</pmid><doi>10.1016/0969-8051(95)02007-1</doi><tpages>6</tpages></addata></record> |
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| ispartof | Nuclear medicine and biology, 1996, Vol.23 (1), p.23-28 |
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| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Animals Chromatography, High Pressure Liquid Chromatography, Thin Layer Dog Dogs Emission-computed tomography Female Heart - diagnostic imaging In Vitro Techniques Iodine Radioisotopes Isoquinolines Isoquinolines - chemical synthesis Isoquinolines - pharmacokinetics Isotope Labeling Male Mitochondrial benzodiazepine receptor Myocardium - metabolism Rat Rats Rats, Sprague-Dawley Receptors, GABA-A - drug effects Tissue Distribution Tomography, Emission-Computed, Single-Photon |
| title | Synthesis and Evaluation of [ 123I]-Iodo-PK11195 for Mapping Peripheral-Type Benzodiazepine Receptors (ω 3) in Heart |
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