Loading…
Autoradiographic Visualization of Corticotropin Releasing Hormone Type 1 Receptors with a Nonpeptide Ligand: Synthesis of [76Br]MJL-1-109-2
A high-affinity, nonpeptide radioligand for the CRHR1 was synthesized and showed distribution in rat brain consistent with CRHR1 using in vitro autoradiography. This is the first nonpeptide radiotracer combining high affinity and appropriate lipophilicity that penetrates the blood−brain barrier and...
Saved in:
| Published in: | Journal of medicinal chemistry 2003-08, Vol.46 (17), p.3559-3562 |
|---|---|
| Main Authors: | , , , , , , , , , , , , |
| Format: | Article |
| Language: | English |
| Subjects: | |
| Citations: | Items that this one cites Items that cite this one |
| Online Access: | Get full text |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| cited_by | cdi_FETCH-LOGICAL-a379t-c96fa7be01b985538c7bc4ed99e77962a2d19d755aacb07d70340bb5882335423 |
|---|---|
| cites | cdi_FETCH-LOGICAL-a379t-c96fa7be01b985538c7bc4ed99e77962a2d19d755aacb07d70340bb5882335423 |
| container_end_page | 3562 |
| container_issue | 17 |
| container_start_page | 3559 |
| container_title | Journal of medicinal chemistry |
| container_volume | 46 |
| creator | Jagoda, Elaine Contoreggi, Carlo Lee, Mei-Jing Kao, Chih-Hao K Szajek, Lawrence P Listwak, Sam Gold, Philip Chrousos, George Greiner, Elisabeth Kim, B. Moon Jacobson, Arthur E Rice, Kenner C Eckelman, William |
| description | A high-affinity, nonpeptide radioligand for the CRHR1 was synthesized and showed distribution in rat brain consistent with CRHR1 using in vitro autoradiography. This is the first nonpeptide radiotracer combining high affinity and appropriate lipophilicity that penetrates the blood−brain barrier and hence has the potential to be used for PET imaging studies. In vivo visualization of changes in the CRH1 receptor or its occupancy would further the understanding of the pathophysiology of stress related diseases. |
| doi_str_mv | 10.1021/jm034077k |
| format | article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_73479902</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>73479902</sourcerecordid><originalsourceid>FETCH-LOGICAL-a379t-c96fa7be01b985538c7bc4ed99e77962a2d19d755aacb07d70340bb5882335423</originalsourceid><addsrcrecordid>eNptkMFu1DAQQCMEokvhwA8gX6jEITC24zjm1q6AglKgdOkFIctxnF1vEzvYiWA5ceXCR_IlZLWr7oXTSDNPT6OXJI8xPMdA8It1BzQDzm_uJDPMCKRZAdndZAZASEpyQo-SBzGuAYBiQu8nR5gIyIAVs-TP6Tj4oGrrl0H1K6vRtY2jau1PNVjvkG_Q3IfBaj8E31uHPpnWqGjdEp370Hln0GLTG4Sngzb95Iroux1WSKH33vXTxtYGlXapXP3y76_f6GrjhpWJNm7VX3h-Fr5evCtTnGIQKXmY3GtUG82j_TxOPr9-tZifp-WHN2_np2WqKBdDqkXeKF4ZwJUoGKOF5pXOTC2E4VzkRJEai5ozppSugNd826eqWFEQSllG6HFysvP2wX8bTRxkZ6M2bauc8WOUnGZcCNiCz3agDj7GYBrZB9upsJEY5Da-vI0_sU_20rHqTH0g97Un4OkeUFGrtgnKaRsPHANaAGQTl-44Gwfz4_auwo3MOeVMLj5eyUsoL_HF2bXMD16lo1z7Mbip3X8e_AfJsKfJ</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>73479902</pqid></control><display><type>article</type><title>Autoradiographic Visualization of Corticotropin Releasing Hormone Type 1 Receptors with a Nonpeptide Ligand: Synthesis of [76Br]MJL-1-109-2</title><source>American Chemical Society:Jisc Collections:American Chemical Society Read & Publish Agreement 2022-2024 (Reading list)</source><creator>Jagoda, Elaine ; Contoreggi, Carlo ; Lee, Mei-Jing ; Kao, Chih-Hao K ; Szajek, Lawrence P ; Listwak, Sam ; Gold, Philip ; Chrousos, George ; Greiner, Elisabeth ; Kim, B. Moon ; Jacobson, Arthur E ; Rice, Kenner C ; Eckelman, William</creator><creatorcontrib>Jagoda, Elaine ; Contoreggi, Carlo ; Lee, Mei-Jing ; Kao, Chih-Hao K ; Szajek, Lawrence P ; Listwak, Sam ; Gold, Philip ; Chrousos, George ; Greiner, Elisabeth ; Kim, B. Moon ; Jacobson, Arthur E ; Rice, Kenner C ; Eckelman, William</creatorcontrib><description>A high-affinity, nonpeptide radioligand for the CRHR1 was synthesized and showed distribution in rat brain consistent with CRHR1 using in vitro autoradiography. This is the first nonpeptide radiotracer combining high affinity and appropriate lipophilicity that penetrates the blood−brain barrier and hence has the potential to be used for PET imaging studies. In vivo visualization of changes in the CRH1 receptor or its occupancy would further the understanding of the pathophysiology of stress related diseases.</description><identifier>ISSN: 0022-2623</identifier><identifier>EISSN: 1520-4804</identifier><identifier>DOI: 10.1021/jm034077k</identifier><identifier>PMID: 12904058</identifier><identifier>CODEN: JMCMAR</identifier><language>eng</language><publisher>Washington, DC: American Chemical Society</publisher><subject>Animals ; Autoradiography ; Biological and medical sciences ; Blood-Brain Barrier ; Brain - metabolism ; Bromine Radioisotopes ; Contrast media. Radiopharmaceuticals ; In Vitro Techniques ; Ligands ; Medical sciences ; Pharmacology. Drug treatments ; Radiopharmaceuticals - chemical synthesis ; Radiopharmaceuticals - metabolism ; Radiopharmaceuticals - pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Receptors, Corticotropin-Releasing Hormone - metabolism ; Tissue Distribution ; Triazines - chemical synthesis ; Triazines - metabolism ; Triazines - pharmacokinetics</subject><ispartof>Journal of medicinal chemistry, 2003-08, Vol.46 (17), p.3559-3562</ispartof><rights>Copyright © 2003 American Chemical Society</rights><rights>2003 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-a379t-c96fa7be01b985538c7bc4ed99e77962a2d19d755aacb07d70340bb5882335423</citedby><cites>FETCH-LOGICAL-a379t-c96fa7be01b985538c7bc4ed99e77962a2d19d755aacb07d70340bb5882335423</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=15038004$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12904058$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Jagoda, Elaine</creatorcontrib><creatorcontrib>Contoreggi, Carlo</creatorcontrib><creatorcontrib>Lee, Mei-Jing</creatorcontrib><creatorcontrib>Kao, Chih-Hao K</creatorcontrib><creatorcontrib>Szajek, Lawrence P</creatorcontrib><creatorcontrib>Listwak, Sam</creatorcontrib><creatorcontrib>Gold, Philip</creatorcontrib><creatorcontrib>Chrousos, George</creatorcontrib><creatorcontrib>Greiner, Elisabeth</creatorcontrib><creatorcontrib>Kim, B. Moon</creatorcontrib><creatorcontrib>Jacobson, Arthur E</creatorcontrib><creatorcontrib>Rice, Kenner C</creatorcontrib><creatorcontrib>Eckelman, William</creatorcontrib><title>Autoradiographic Visualization of Corticotropin Releasing Hormone Type 1 Receptors with a Nonpeptide Ligand: Synthesis of [76Br]MJL-1-109-2</title><title>Journal of medicinal chemistry</title><addtitle>J. Med. Chem</addtitle><description>A high-affinity, nonpeptide radioligand for the CRHR1 was synthesized and showed distribution in rat brain consistent with CRHR1 using in vitro autoradiography. This is the first nonpeptide radiotracer combining high affinity and appropriate lipophilicity that penetrates the blood−brain barrier and hence has the potential to be used for PET imaging studies. In vivo visualization of changes in the CRH1 receptor or its occupancy would further the understanding of the pathophysiology of stress related diseases.</description><subject>Animals</subject><subject>Autoradiography</subject><subject>Biological and medical sciences</subject><subject>Blood-Brain Barrier</subject><subject>Brain - metabolism</subject><subject>Bromine Radioisotopes</subject><subject>Contrast media. Radiopharmaceuticals</subject><subject>In Vitro Techniques</subject><subject>Ligands</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Radiopharmaceuticals - chemical synthesis</subject><subject>Radiopharmaceuticals - metabolism</subject><subject>Radiopharmaceuticals - pharmacokinetics</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptors, Corticotropin-Releasing Hormone - metabolism</subject><subject>Tissue Distribution</subject><subject>Triazines - chemical synthesis</subject><subject>Triazines - metabolism</subject><subject>Triazines - pharmacokinetics</subject><issn>0022-2623</issn><issn>1520-4804</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><recordid>eNptkMFu1DAQQCMEokvhwA8gX6jEITC24zjm1q6AglKgdOkFIctxnF1vEzvYiWA5ceXCR_IlZLWr7oXTSDNPT6OXJI8xPMdA8It1BzQDzm_uJDPMCKRZAdndZAZASEpyQo-SBzGuAYBiQu8nR5gIyIAVs-TP6Tj4oGrrl0H1K6vRtY2jau1PNVjvkG_Q3IfBaj8E31uHPpnWqGjdEp370Hln0GLTG4Sngzb95Iroux1WSKH33vXTxtYGlXapXP3y76_f6GrjhpWJNm7VX3h-Fr5evCtTnGIQKXmY3GtUG82j_TxOPr9-tZifp-WHN2_np2WqKBdDqkXeKF4ZwJUoGKOF5pXOTC2E4VzkRJEai5ozppSugNd826eqWFEQSllG6HFysvP2wX8bTRxkZ6M2bauc8WOUnGZcCNiCz3agDj7GYBrZB9upsJEY5Da-vI0_sU_20rHqTH0g97Un4OkeUFGrtgnKaRsPHANaAGQTl-44Gwfz4_auwo3MOeVMLj5eyUsoL_HF2bXMD16lo1z7Mbip3X8e_AfJsKfJ</recordid><startdate>20030814</startdate><enddate>20030814</enddate><creator>Jagoda, Elaine</creator><creator>Contoreggi, Carlo</creator><creator>Lee, Mei-Jing</creator><creator>Kao, Chih-Hao K</creator><creator>Szajek, Lawrence P</creator><creator>Listwak, Sam</creator><creator>Gold, Philip</creator><creator>Chrousos, George</creator><creator>Greiner, Elisabeth</creator><creator>Kim, B. Moon</creator><creator>Jacobson, Arthur E</creator><creator>Rice, Kenner C</creator><creator>Eckelman, William</creator><general>American Chemical Society</general><scope>BSCLL</scope><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>20030814</creationdate><title>Autoradiographic Visualization of Corticotropin Releasing Hormone Type 1 Receptors with a Nonpeptide Ligand: Synthesis of [76Br]MJL-1-109-2</title><author>Jagoda, Elaine ; Contoreggi, Carlo ; Lee, Mei-Jing ; Kao, Chih-Hao K ; Szajek, Lawrence P ; Listwak, Sam ; Gold, Philip ; Chrousos, George ; Greiner, Elisabeth ; Kim, B. Moon ; Jacobson, Arthur E ; Rice, Kenner C ; Eckelman, William</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-a379t-c96fa7be01b985538c7bc4ed99e77962a2d19d755aacb07d70340bb5882335423</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Animals</topic><topic>Autoradiography</topic><topic>Biological and medical sciences</topic><topic>Blood-Brain Barrier</topic><topic>Brain - metabolism</topic><topic>Bromine Radioisotopes</topic><topic>Contrast media. Radiopharmaceuticals</topic><topic>In Vitro Techniques</topic><topic>Ligands</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Radiopharmaceuticals - chemical synthesis</topic><topic>Radiopharmaceuticals - metabolism</topic><topic>Radiopharmaceuticals - pharmacokinetics</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptors, Corticotropin-Releasing Hormone - metabolism</topic><topic>Tissue Distribution</topic><topic>Triazines - chemical synthesis</topic><topic>Triazines - metabolism</topic><topic>Triazines - pharmacokinetics</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Jagoda, Elaine</creatorcontrib><creatorcontrib>Contoreggi, Carlo</creatorcontrib><creatorcontrib>Lee, Mei-Jing</creatorcontrib><creatorcontrib>Kao, Chih-Hao K</creatorcontrib><creatorcontrib>Szajek, Lawrence P</creatorcontrib><creatorcontrib>Listwak, Sam</creatorcontrib><creatorcontrib>Gold, Philip</creatorcontrib><creatorcontrib>Chrousos, George</creatorcontrib><creatorcontrib>Greiner, Elisabeth</creatorcontrib><creatorcontrib>Kim, B. Moon</creatorcontrib><creatorcontrib>Jacobson, Arthur E</creatorcontrib><creatorcontrib>Rice, Kenner C</creatorcontrib><creatorcontrib>Eckelman, William</creatorcontrib><collection>Istex</collection><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>Journal of medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Jagoda, Elaine</au><au>Contoreggi, Carlo</au><au>Lee, Mei-Jing</au><au>Kao, Chih-Hao K</au><au>Szajek, Lawrence P</au><au>Listwak, Sam</au><au>Gold, Philip</au><au>Chrousos, George</au><au>Greiner, Elisabeth</au><au>Kim, B. Moon</au><au>Jacobson, Arthur E</au><au>Rice, Kenner C</au><au>Eckelman, William</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Autoradiographic Visualization of Corticotropin Releasing Hormone Type 1 Receptors with a Nonpeptide Ligand: Synthesis of [76Br]MJL-1-109-2</atitle><jtitle>Journal of medicinal chemistry</jtitle><addtitle>J. Med. Chem</addtitle><date>2003-08-14</date><risdate>2003</risdate><volume>46</volume><issue>17</issue><spage>3559</spage><epage>3562</epage><pages>3559-3562</pages><issn>0022-2623</issn><eissn>1520-4804</eissn><coden>JMCMAR</coden><abstract>A high-affinity, nonpeptide radioligand for the CRHR1 was synthesized and showed distribution in rat brain consistent with CRHR1 using in vitro autoradiography. This is the first nonpeptide radiotracer combining high affinity and appropriate lipophilicity that penetrates the blood−brain barrier and hence has the potential to be used for PET imaging studies. In vivo visualization of changes in the CRH1 receptor or its occupancy would further the understanding of the pathophysiology of stress related diseases.</abstract><cop>Washington, DC</cop><pub>American Chemical Society</pub><pmid>12904058</pmid><doi>10.1021/jm034077k</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0022-2623 |
| ispartof | Journal of medicinal chemistry, 2003-08, Vol.46 (17), p.3559-3562 |
| issn | 0022-2623 1520-4804 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_73479902 |
| source | American Chemical Society:Jisc Collections:American Chemical Society Read & Publish Agreement 2022-2024 (Reading list) |
| subjects | Animals Autoradiography Biological and medical sciences Blood-Brain Barrier Brain - metabolism Bromine Radioisotopes Contrast media. Radiopharmaceuticals In Vitro Techniques Ligands Medical sciences Pharmacology. Drug treatments Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - metabolism Radiopharmaceuticals - pharmacokinetics Rats Rats, Sprague-Dawley Receptors, Corticotropin-Releasing Hormone - metabolism Tissue Distribution Triazines - chemical synthesis Triazines - metabolism Triazines - pharmacokinetics |
| title | Autoradiographic Visualization of Corticotropin Releasing Hormone Type 1 Receptors with a Nonpeptide Ligand: Synthesis of [76Br]MJL-1-109-2 |
| url | http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-26T08%3A11%3A54IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Autoradiographic%20Visualization%20of%20Corticotropin%20Releasing%20Hormone%20Type%201%20Receptors%20with%20a%20Nonpeptide%20Ligand:%E2%80%89%20Synthesis%20of%20%5B76Br%5DMJL-1-109-2&rft.jtitle=Journal%20of%20medicinal%20chemistry&rft.au=Jagoda,%20Elaine&rft.date=2003-08-14&rft.volume=46&rft.issue=17&rft.spage=3559&rft.epage=3562&rft.pages=3559-3562&rft.issn=0022-2623&rft.eissn=1520-4804&rft.coden=JMCMAR&rft_id=info:doi/10.1021/jm034077k&rft_dat=%3Cproquest_cross%3E73479902%3C/proquest_cross%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-a379t-c96fa7be01b985538c7bc4ed99e77962a2d19d755aacb07d70340bb5882335423%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_pqid=73479902&rft_id=info:pmid/12904058&rfr_iscdi=true |