Synthesis and biodistribution of 125I labeled bivalent analogs of practolol as potential myocardial imaging agents
Iodinated bivalent ligands 3 and 4 and a monovalent ligand 5 were prepared from the cardioselective β-antagonist, practolol. 125 I-labeled 3, 4 and 5 were prepared by solid phase isotopic exchange reaction with carrier-free Na 125 I and examined in rats as potential receptor-site-directed myocardial...
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| Veröffentlicht in: | International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology Nuclear medicine and biology, 1986, Vol.13 (5), p.551-555 |
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| container_title | International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology |
| container_volume | 13 |
| creator | Kizuka, H. Hanson, R.N. |
| description | Iodinated bivalent ligands
3 and
4 and a monovalent ligand
5 were prepared from the cardioselective β-antagonist, practolol.
125
I-labeled
3, 4 and
5 were prepared by solid phase isotopic exchange reaction with carrier-free Na
125
I and examined in rats as potential receptor-site-directed myocardial imaging agents. Biodistribution of these agents in rats indicated that
125
I-3 and
125
I-4 were localized in the heart similarly to
125
I-5 and the [
125
I]iodobenzoyl practolol (
6) that was previously reported. Localization of
125
I-3 and
125
I-4, was more persistent in the heart than that of
125
I-monovalent ligands
5 and
6. Heart-to-blood ratios of
125
I-3 and
125
I-4 were significantly lower than those of
125
I-5 and
125
I-6, due mainly to slow blood clearance rates of
125
I-3 and
125
I-4. |
| doi_str_mv | 10.1016/0883-2897(86)90137-6 |
| format | Article |
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3 and
4 and a monovalent ligand
5 were prepared from the cardioselective β-antagonist, practolol.
125
I-labeled
3, 4 and
5 were prepared by solid phase isotopic exchange reaction with carrier-free Na
125
I and examined in rats as potential receptor-site-directed myocardial imaging agents. Biodistribution of these agents in rats indicated that
125
I-3 and
125
I-4 were localized in the heart similarly to
125
I-5 and the [
125
I]iodobenzoyl practolol (
6) that was previously reported. Localization of
125
I-3 and
125
I-4, was more persistent in the heart than that of
125
I-monovalent ligands
5 and
6. Heart-to-blood ratios of
125
I-3 and
125
I-4 were significantly lower than those of
125
I-5 and
125
I-6, due mainly to slow blood clearance rates of
125
I-3 and
125
I-4.</description><identifier>ISSN: 0883-2897</identifier><identifier>DOI: 10.1016/0883-2897(86)90137-6</identifier><identifier>PMID: 3818320</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Animals ; Heart - diagnostic imaging ; Indicators and Reagents ; Iodine Radioisotopes ; Kinetics ; Practolol - analogs & derivatives ; Practolol - metabolism ; Radionuclide Imaging ; Rats ; Rats, Inbred Strains ; Tissue Distribution</subject><ispartof>International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology, 1986, Vol.13 (5), p.551-555</ispartof><rights>1986</rights><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c1530-681e5fb50a96b639c70a57cff3359241af1018259854002463f7574293c9c8673</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,4024,27923,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3818320$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kizuka, H.</creatorcontrib><creatorcontrib>Hanson, R.N.</creatorcontrib><title>Synthesis and biodistribution of 125I labeled bivalent analogs of practolol as potential myocardial imaging agents</title><title>International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology</title><addtitle>Int J Rad Appl Instrum B</addtitle><description>Iodinated bivalent ligands
3 and
4 and a monovalent ligand
5 were prepared from the cardioselective β-antagonist, practolol.
125
I-labeled
3, 4 and
5 were prepared by solid phase isotopic exchange reaction with carrier-free Na
125
I and examined in rats as potential receptor-site-directed myocardial imaging agents. Biodistribution of these agents in rats indicated that
125
I-3 and
125
I-4 were localized in the heart similarly to
125
I-5 and the [
125
I]iodobenzoyl practolol (
6) that was previously reported. Localization of
125
I-3 and
125
I-4, was more persistent in the heart than that of
125
I-monovalent ligands
5 and
6. Heart-to-blood ratios of
125
I-3 and
125
I-4 were significantly lower than those of
125
I-5 and
125
I-6, due mainly to slow blood clearance rates of
125
I-3 and
125
I-4.</description><subject>Animals</subject><subject>Heart - diagnostic imaging</subject><subject>Indicators and Reagents</subject><subject>Iodine Radioisotopes</subject><subject>Kinetics</subject><subject>Practolol - analogs & derivatives</subject><subject>Practolol - metabolism</subject><subject>Radionuclide Imaging</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Tissue Distribution</subject><issn>0883-2897</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1986</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMtOwzAQRb0AlVL4A5C8QrAI2HH82iChikelSiyAteU4TjBy42Knlfr3OLRiyWqsuXdmfA8AFxjdYoTZHRKCFKWQ_FqwG4kw4QU7AtO_9gk4TekLoVJUlE_AhAgsSImmIL7t-uHTJpeg7htYu9C4NERXbwYXehhaiEu6gF7X1ttR32pv-yGbtQ9dGg3rqM0QfPBQJ7gOQ5ad9nC1C0bHZny6le5c30HdZS2dgeNW-2TPD3UGPp4e3-cvxfL1eTF_WBYGU4IKJrClbU2RlqxmRBqONOWmbQmhsqywbnNyUVIpaJWDVYy0nPKqlMRIIxgnM3C137uO4Xtj06BWLhnrve5t2CTFecmJzBxmoNobTQwpRduqdcxfjjuFkRrxqpGjGjkqwdQvXsXy2OVh_6Ze2eZv6MA26_d73eaQW2ejSsbZ3tjGRWsG1QT3_4EfxuWLaw</recordid><startdate>1986</startdate><enddate>1986</enddate><creator>Kizuka, H.</creator><creator>Hanson, R.N.</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>1986</creationdate><title>Synthesis and biodistribution of 125I labeled bivalent analogs of practolol as potential myocardial imaging agents</title><author>Kizuka, H. ; Hanson, R.N.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c1530-681e5fb50a96b639c70a57cff3359241af1018259854002463f7574293c9c8673</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1986</creationdate><topic>Animals</topic><topic>Heart - diagnostic imaging</topic><topic>Indicators and Reagents</topic><topic>Iodine Radioisotopes</topic><topic>Kinetics</topic><topic>Practolol - analogs & derivatives</topic><topic>Practolol - metabolism</topic><topic>Radionuclide Imaging</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Tissue Distribution</topic><toplevel>online_resources</toplevel><creatorcontrib>Kizuka, H.</creatorcontrib><creatorcontrib>Hanson, R.N.</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>International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kizuka, H.</au><au>Hanson, R.N.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and biodistribution of 125I labeled bivalent analogs of practolol as potential myocardial imaging agents</atitle><jtitle>International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology</jtitle><addtitle>Int J Rad Appl Instrum B</addtitle><date>1986</date><risdate>1986</risdate><volume>13</volume><issue>5</issue><spage>551</spage><epage>555</epage><pages>551-555</pages><issn>0883-2897</issn><abstract>Iodinated bivalent ligands
3 and
4 and a monovalent ligand
5 were prepared from the cardioselective β-antagonist, practolol.
125
I-labeled
3, 4 and
5 were prepared by solid phase isotopic exchange reaction with carrier-free Na
125
I and examined in rats as potential receptor-site-directed myocardial imaging agents. Biodistribution of these agents in rats indicated that
125
I-3 and
125
I-4 were localized in the heart similarly to
125
I-5 and the [
125
I]iodobenzoyl practolol (
6) that was previously reported. Localization of
125
I-3 and
125
I-4, was more persistent in the heart than that of
125
I-monovalent ligands
5 and
6. Heart-to-blood ratios of
125
I-3 and
125
I-4 were significantly lower than those of
125
I-5 and
125
I-6, due mainly to slow blood clearance rates of
125
I-3 and
125
I-4.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>3818320</pmid><doi>10.1016/0883-2897(86)90137-6</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0883-2897 |
| ispartof | International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology, 1986, Vol.13 (5), p.551-555 |
| issn | 0883-2897 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_77273918 |
| source | MEDLINE; Alma/SFX Local Collection |
| subjects | Animals Heart - diagnostic imaging Indicators and Reagents Iodine Radioisotopes Kinetics Practolol - analogs & derivatives Practolol - metabolism Radionuclide Imaging Rats Rats, Inbred Strains Tissue Distribution |
| title | Synthesis and biodistribution of 125I labeled bivalent analogs of practolol as potential myocardial imaging agents |
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