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Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity
A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified. A high-throughput screening campaign resulted in the discovery of a...
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| Published in: | Bioorganic & medicinal chemistry 2008-03, Vol.18 (5), p.1725-1729 |
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| Main Authors: | , , , , , , , , , , , , , , , , , |
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| Language: | English |
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| cites | cdi_FETCH-LOGICAL-c415t-6d4ff261e1d3d44f016113babb6e4c8cae1f032773ad7b0001353f94a92f51bd3 |
| container_end_page | 1729 |
| container_issue | 5 |
| container_start_page | 1725 |
| container_title | Bioorganic & medicinal chemistry |
| container_volume | 18 |
| creator | Ermann, Monika Riether, Doris Walker, Edward R. Mushi, Innocent F. Jenkins, James E. Noya-Marino, Beatriz Brewer, Mark L. Taylor, Malcolm G. Amouzegh, Patricia East, Stephen P. Dymock, Brian W. Gemkow, Mark J. Kahrs, Andreas F. Ebneth, Andreas Löbbe, Sabine O’Shea, Kathy Shih, Daw-Tsun Thomson, David |
| description | A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified.
A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified. |
| doi_str_mv | 10.1016/j.bmcl.2008.01.042 |
| format | article |
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A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified.</description><identifier>ISSN: 0960-894X</identifier><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3405</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmcl.2008.01.042</identifier><identifier>PMID: 18255291</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Agonists ; Arylsulfonamide ; Biological and medical sciences ; Cannabinoid receptor ; CB1 ; CB2 ; Medical sciences ; Miscellaneous ; Molecular Structure ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pharmacology. Drug treatments ; Receptor, Cannabinoid, CB1 - agonists ; Receptor, Cannabinoid, CB2 - agonists ; Selectivity ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry, 2008-03, Vol.18 (5), p.1725-1729</ispartof><rights>2008 Elsevier Ltd</rights><rights>2008 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c415t-6d4ff261e1d3d44f016113babb6e4c8cae1f032773ad7b0001353f94a92f51bd3</citedby><cites>FETCH-LOGICAL-c415t-6d4ff261e1d3d44f016113babb6e4c8cae1f032773ad7b0001353f94a92f51bd3</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=20167652$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/18255291$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ermann, Monika</creatorcontrib><creatorcontrib>Riether, Doris</creatorcontrib><creatorcontrib>Walker, Edward R.</creatorcontrib><creatorcontrib>Mushi, Innocent F.</creatorcontrib><creatorcontrib>Jenkins, James E.</creatorcontrib><creatorcontrib>Noya-Marino, Beatriz</creatorcontrib><creatorcontrib>Brewer, Mark L.</creatorcontrib><creatorcontrib>Taylor, Malcolm G.</creatorcontrib><creatorcontrib>Amouzegh, Patricia</creatorcontrib><creatorcontrib>East, Stephen P.</creatorcontrib><creatorcontrib>Dymock, Brian W.</creatorcontrib><creatorcontrib>Gemkow, Mark J.</creatorcontrib><creatorcontrib>Kahrs, Andreas F.</creatorcontrib><creatorcontrib>Ebneth, Andreas</creatorcontrib><creatorcontrib>Löbbe, Sabine</creatorcontrib><creatorcontrib>O’Shea, Kathy</creatorcontrib><creatorcontrib>Shih, Daw-Tsun</creatorcontrib><creatorcontrib>Thomson, David</creatorcontrib><title>Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem Lett</addtitle><description>A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified.
A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified.</description><subject>Agonists</subject><subject>Arylsulfonamide</subject><subject>Biological and medical sciences</subject><subject>Cannabinoid receptor</subject><subject>CB1</subject><subject>CB2</subject><subject>Medical sciences</subject><subject>Miscellaneous</subject><subject>Molecular Structure</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pharmacology. 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Neurotransmission. Receptors</topic><topic>Pharmacology. Drug treatments</topic><topic>Receptor, Cannabinoid, CB1 - agonists</topic><topic>Receptor, Cannabinoid, CB2 - agonists</topic><topic>Selectivity</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ermann, Monika</creatorcontrib><creatorcontrib>Riether, Doris</creatorcontrib><creatorcontrib>Walker, Edward R.</creatorcontrib><creatorcontrib>Mushi, Innocent F.</creatorcontrib><creatorcontrib>Jenkins, James E.</creatorcontrib><creatorcontrib>Noya-Marino, Beatriz</creatorcontrib><creatorcontrib>Brewer, Mark L.</creatorcontrib><creatorcontrib>Taylor, Malcolm G.</creatorcontrib><creatorcontrib>Amouzegh, Patricia</creatorcontrib><creatorcontrib>East, Stephen P.</creatorcontrib><creatorcontrib>Dymock, Brian W.</creatorcontrib><creatorcontrib>Gemkow, Mark J.</creatorcontrib><creatorcontrib>Kahrs, Andreas F.</creatorcontrib><creatorcontrib>Ebneth, Andreas</creatorcontrib><creatorcontrib>Löbbe, Sabine</creatorcontrib><creatorcontrib>O’Shea, Kathy</creatorcontrib><creatorcontrib>Shih, Daw-Tsun</creatorcontrib><creatorcontrib>Thomson, David</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>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ermann, Monika</au><au>Riether, Doris</au><au>Walker, Edward R.</au><au>Mushi, Innocent F.</au><au>Jenkins, James E.</au><au>Noya-Marino, Beatriz</au><au>Brewer, Mark L.</au><au>Taylor, Malcolm G.</au><au>Amouzegh, Patricia</au><au>East, Stephen P.</au><au>Dymock, Brian W.</au><au>Gemkow, Mark J.</au><au>Kahrs, Andreas F.</au><au>Ebneth, Andreas</au><au>Löbbe, Sabine</au><au>O’Shea, Kathy</au><au>Shih, Daw-Tsun</au><au>Thomson, David</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2008-03-01</date><risdate>2008</risdate><volume>18</volume><issue>5</issue><spage>1725</spage><epage>1729</epage><pages>1725-1729</pages><issn>0960-894X</issn><issn>0968-0896</issn><eissn>1464-3405</eissn><eissn>1464-3391</eissn><abstract>A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified.
A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>18255291</pmid><doi>10.1016/j.bmcl.2008.01.042</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry, 2008-03, Vol.18 (5), p.1725-1729 |
| issn | 0960-894X 0968-0896 1464-3405 1464-3391 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_70377469 |
| source | ScienceDirect Freedom Collection |
| subjects | Agonists Arylsulfonamide Biological and medical sciences Cannabinoid receptor CB1 CB2 Medical sciences Miscellaneous Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Receptor, Cannabinoid, CB1 - agonists Receptor, Cannabinoid, CB2 - agonists Selectivity Structure-Activity Relationship |
| title | Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity |
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