Identification and characterization of m4 selective muscarinic antagonists
Our interest in the area of m4 muscarinic antagonists has led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC 50 value of 90.7nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) mo...
Gespeichert in:
| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 1998-08, Vol.8 (15), p.1991-1996 |
|---|---|
| Hauptverfasser: | , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 1996 |
|---|---|
| container_issue | 15 |
| container_start_page | 1991 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 8 |
| creator | Augelli-Szafran, Corinne E Jaen, Juan C Moreland, David W Nelson, Carrie B Penvose-Yi, Jan R Schwarz, Roy D |
| description | Our interest in the area of m4 muscarinic antagonists has led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example
1 with an IC
50 value of 90.7nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of
1 are reported.
The study of a series of benzoxazine isoquinolines, which led to the identification of a potent and selective m4 muscarinic antagonist
1 is reported. [For
1 at the m4 receptor, the IC
50 = 90.7 nM; however,
1 is 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective when compared to the other receptors.] |
| doi_str_mv | 10.1016/S0960-894X(98)00351-5 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_69113623</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0960894X98003515</els_id><sourcerecordid>69113623</sourcerecordid><originalsourceid>FETCH-LOGICAL-c507t-8bd238ccaa1861a173687aab9fd37d04199c95df50e511a6f0bae3e164b2e7b43</originalsourceid><addsrcrecordid>eNqFkE1r3DAQhkVoSTab_oSAD6U0B6ca68PWqYSl-WKhhzTQmxhL40TFH6lkLzS_vt7sstecBmaed2Z4GDsHfgkc9LcHbjTPKyN_fzXVBedCQa6O2AKklrmQXH1giwNywk5T-sM5SC7lMTs2VSlkWSzY_Z2nfgxNcDiGoc-w95l7xohupBhed82hyTqZJWrJjWFDWTclhzH0wc38iE9DH9KYztjHBttEn_Z1yR6vf_xa3ebrnzd3q6t17hQvx7yqfSEq5xCh0oBQCl2ViLVpvCg9l2CMM8o3ipMCQN3wGkkQaFkXVNZSLNmX3d6XOPydKI22C8lR22JPw5SsNgBCF2IG1Q50cUgpUmNfYugw_rPA7dahfXNot4KsqeybQ6vm3Pn-wFR35A-pvbR5_nk_x9lD20TsXUgHrBBKgS5n7PsOo1nGJlC0yQXqHfkQZ5HWD-GdR_4D-K2PDg</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>69113623</pqid></control><display><type>article</type><title>Identification and characterization of m4 selective muscarinic antagonists</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals</source><creator>Augelli-Szafran, Corinne E ; Jaen, Juan C ; Moreland, David W ; Nelson, Carrie B ; Penvose-Yi, Jan R ; Schwarz, Roy D</creator><creatorcontrib>Augelli-Szafran, Corinne E ; Jaen, Juan C ; Moreland, David W ; Nelson, Carrie B ; Penvose-Yi, Jan R ; Schwarz, Roy D</creatorcontrib><description>Our interest in the area of m4 muscarinic antagonists has led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example
1 with an IC
50 value of 90.7nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of
1 are reported.
The study of a series of benzoxazine isoquinolines, which led to the identification of a potent and selective m4 muscarinic antagonist
1 is reported. [For
1 at the m4 receptor, the IC
50 = 90.7 nM; however,
1 is 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective when compared to the other receptors.]</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/S0960-894X(98)00351-5</identifier><identifier>PMID: 9873472</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Biological and medical sciences ; Cholinergic system ; Isoquinolines - chemistry ; Isoquinolines - metabolism ; Isoquinolines - pharmacology ; Medical sciences ; Muscarinic Antagonists - chemistry ; Muscarinic Antagonists - metabolism ; Muscarinic Antagonists - pharmacology ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pharmacology. Drug treatments ; Protein Binding ; Receptor, Muscarinic M4 ; Receptors, Muscarinic - drug effects ; Receptors, Muscarinic - metabolism</subject><ispartof>Bioorganic & medicinal chemistry letters, 1998-08, Vol.8 (15), p.1991-1996</ispartof><rights>1998</rights><rights>1998 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c507t-8bd238ccaa1861a173687aab9fd37d04199c95df50e511a6f0bae3e164b2e7b43</citedby><cites>FETCH-LOGICAL-c507t-8bd238ccaa1861a173687aab9fd37d04199c95df50e511a6f0bae3e164b2e7b43</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0960-894X(98)00351-5$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,45974</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2355167$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9873472$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Augelli-Szafran, Corinne E</creatorcontrib><creatorcontrib>Jaen, Juan C</creatorcontrib><creatorcontrib>Moreland, David W</creatorcontrib><creatorcontrib>Nelson, Carrie B</creatorcontrib><creatorcontrib>Penvose-Yi, Jan R</creatorcontrib><creatorcontrib>Schwarz, Roy D</creatorcontrib><title>Identification and characterization of m4 selective muscarinic antagonists</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Our interest in the area of m4 muscarinic antagonists has led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example
1 with an IC
50 value of 90.7nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of
1 are reported.
The study of a series of benzoxazine isoquinolines, which led to the identification of a potent and selective m4 muscarinic antagonist
1 is reported. [For
1 at the m4 receptor, the IC
50 = 90.7 nM; however,
1 is 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective when compared to the other receptors.]</description><subject>Biological and medical sciences</subject><subject>Cholinergic system</subject><subject>Isoquinolines - chemistry</subject><subject>Isoquinolines - metabolism</subject><subject>Isoquinolines - pharmacology</subject><subject>Medical sciences</subject><subject>Muscarinic Antagonists - chemistry</subject><subject>Muscarinic Antagonists - metabolism</subject><subject>Muscarinic Antagonists - pharmacology</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Binding</subject><subject>Receptor, Muscarinic M4</subject><subject>Receptors, Muscarinic - drug effects</subject><subject>Receptors, Muscarinic - metabolism</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1r3DAQhkVoSTab_oSAD6U0B6ca68PWqYSl-WKhhzTQmxhL40TFH6lkLzS_vt7sstecBmaed2Z4GDsHfgkc9LcHbjTPKyN_fzXVBedCQa6O2AKklrmQXH1giwNywk5T-sM5SC7lMTs2VSlkWSzY_Z2nfgxNcDiGoc-w95l7xohupBhed82hyTqZJWrJjWFDWTclhzH0wc38iE9DH9KYztjHBttEn_Z1yR6vf_xa3ebrnzd3q6t17hQvx7yqfSEq5xCh0oBQCl2ViLVpvCg9l2CMM8o3ipMCQN3wGkkQaFkXVNZSLNmX3d6XOPydKI22C8lR22JPw5SsNgBCF2IG1Q50cUgpUmNfYugw_rPA7dahfXNot4KsqeybQ6vm3Pn-wFR35A-pvbR5_nk_x9lD20TsXUgHrBBKgS5n7PsOo1nGJlC0yQXqHfkQZ5HWD-GdR_4D-K2PDg</recordid><startdate>19980804</startdate><enddate>19980804</enddate><creator>Augelli-Szafran, Corinne E</creator><creator>Jaen, Juan C</creator><creator>Moreland, David W</creator><creator>Nelson, Carrie B</creator><creator>Penvose-Yi, Jan R</creator><creator>Schwarz, Roy D</creator><general>Elsevier Ltd</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>19980804</creationdate><title>Identification and characterization of m4 selective muscarinic antagonists</title><author>Augelli-Szafran, Corinne E ; Jaen, Juan C ; Moreland, David W ; Nelson, Carrie B ; Penvose-Yi, Jan R ; Schwarz, Roy D</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c507t-8bd238ccaa1861a173687aab9fd37d04199c95df50e511a6f0bae3e164b2e7b43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Biological and medical sciences</topic><topic>Cholinergic system</topic><topic>Isoquinolines - chemistry</topic><topic>Isoquinolines - metabolism</topic><topic>Isoquinolines - pharmacology</topic><topic>Medical sciences</topic><topic>Muscarinic Antagonists - chemistry</topic><topic>Muscarinic Antagonists - metabolism</topic><topic>Muscarinic Antagonists - pharmacology</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pharmacology. Drug treatments</topic><topic>Protein Binding</topic><topic>Receptor, Muscarinic M4</topic><topic>Receptors, Muscarinic - drug effects</topic><topic>Receptors, Muscarinic - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Augelli-Szafran, Corinne E</creatorcontrib><creatorcontrib>Jaen, Juan C</creatorcontrib><creatorcontrib>Moreland, David W</creatorcontrib><creatorcontrib>Nelson, Carrie B</creatorcontrib><creatorcontrib>Penvose-Yi, Jan R</creatorcontrib><creatorcontrib>Schwarz, Roy D</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>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Augelli-Szafran, Corinne E</au><au>Jaen, Juan C</au><au>Moreland, David W</au><au>Nelson, Carrie B</au><au>Penvose-Yi, Jan R</au><au>Schwarz, Roy D</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Identification and characterization of m4 selective muscarinic antagonists</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>1998-08-04</date><risdate>1998</risdate><volume>8</volume><issue>15</issue><spage>1991</spage><epage>1996</epage><pages>1991-1996</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Our interest in the area of m4 muscarinic antagonists has led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example
1 with an IC
50 value of 90.7nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of
1 are reported.
The study of a series of benzoxazine isoquinolines, which led to the identification of a potent and selective m4 muscarinic antagonist
1 is reported. [For
1 at the m4 receptor, the IC
50 = 90.7 nM; however,
1 is 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective when compared to the other receptors.]</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>9873472</pmid><doi>10.1016/S0960-894X(98)00351-5</doi><tpages>6</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 1998-08, Vol.8 (15), p.1991-1996 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_69113623 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Biological and medical sciences Cholinergic system Isoquinolines - chemistry Isoquinolines - metabolism Isoquinolines - pharmacology Medical sciences Muscarinic Antagonists - chemistry Muscarinic Antagonists - metabolism Muscarinic Antagonists - pharmacology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Protein Binding Receptor, Muscarinic M4 Receptors, Muscarinic - drug effects Receptors, Muscarinic - metabolism |
| title | Identification and characterization of m4 selective muscarinic antagonists |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-22T05%3A19%3A03IST&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=Identification%20and%20characterization%20of%20m4%20selective%20muscarinic%20antagonists&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry%20letters&rft.au=Augelli-Szafran,%20Corinne%20E&rft.date=1998-08-04&rft.volume=8&rft.issue=15&rft.spage=1991&rft.epage=1996&rft.pages=1991-1996&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/S0960-894X(98)00351-5&rft_dat=%3Cproquest_cross%3E69113623%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=69113623&rft_id=info:pmid/9873472&rft_els_id=S0960894X98003515&rfr_iscdi=true |