Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor
- Author
- SALOVICH, James M1 3 4 ; VINSON, Paige N1 3 4 ; SCOTT DANIELS, J1 3 4 ; JEFFREY CONN, P1 3 4 ; NISWENDER, Colleen M1 3 4 ; LINDSLEY, Craig W1 2 3 4 ; HOPKINS, CoreyR1 2 3 4 ; SHEFFLER, Douglas J1 3 4 ; LAMSAL, Atin1 3 4 ; UTLEY, Thomas J1 3 4 ; BLOBAUM, Anna L1 3 4 ; BRIDGES, Thomas M1 3 4 ; LE, Uyen1 3 4 ; JONES, Carrie K1 3 4 5 ; WOOD, Michael R1 2 3 4
[1] Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, United States
[2] Department of Chemistry, Vanderbilt University., Nashville, TN 37232, United States
[3] Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States
[4] Vanderbilt Specialized Chemistry Center for Probe Development (MLPCN), Nashville, TN 37232, United States
[5] US Department of Veterans Affairs, Tennessee Valley Healthcare System, Nashville, TN 37232, United States - Source
Bioorganic & medicinal chemistry letters (Print). 2012, Vol 22, Num 15, pp 5084-5088, 5 p
- ISSN
- 0960-894X
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Amsterdam
- Publication country
- Netherlands
- Document type
- Article
- Language
- English
- Author keyword
- CNS penetration M4 ML293 Muscarinic receptor 4 Positive allosteric modulator
- Keyword (fr)
- Barrière hématoencéphalique Dérivé du thiazole Récepteur cholinergique Récepteur muscarinique M4 Récepteur muscarinique Régulation allostérique Sélectivité Pharmacocinétique
- Keyword (en)
- Blood brain barrier Thiazole derivatives Cholinergic receptor M4 muscarinic receptor Muscarinic receptor Allosteric regulation Selectivity Pharmacokinetics
- Keyword (es)
- Barrera hematoencefálica Tiazol derivado Receptor colinérgico Receptor muscarínico M4 Receptor muscarínico Regulación alostérica Selectividad Farmacocinética
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments
- Discipline
- General pharmacology
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 26195346
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
Access to the document
Install on your browser
DOI
10.1016/j.bmcl.2012.05.109 
https://dx.doi.org/10.1016/j.bmcl.2012.05.109
"O:13:\"PanistOpenUrl\":36:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000idc\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2012.05.109\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2012\";s:9:\"\u0000*\u0000volume\";s:2:\"22\";s:8:\"\u0000*\u0000issue\";s:2:\"15\";s:8:\"\u0000*\u0000spage\";s:4:\"5084\";s:8:\"\u0000*\u0000epage\";s:4:\"5088\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:8:\"SALOVICH\";s:10:\"\u0000*\u0000aufirst\";s:7:\"James M\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:14:{i:0;s:15:\"VINSON, Paige N\";i:1;s:16:\"SCOTT DANIELS, J\";i:2;s:15:\"JEFFREY CONN, P\";i:3;s:20:\"NISWENDER, Colleen M\";i:4;s:17:\"LINDSLEY, Craig W\";i:5;s:15:\"HOPKINS, CoreyR\";i:6;s:19:\"SHEFFLER, Douglas J\";i:7;s:12:\"LAMSAL, Atin\";i:8;s:15:\"UTLEY, Thomas J\";i:9;s:15:\"BLOBAUM, Anna L\";i:10;s:17:\"BRIDGES, Thomas M\";i:11;s:8:\"LE, Uyen\";i:12;s:15:\"JONES, Carrie K\";i:13;s:15:\"WOOD, Michael R\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"5\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Panist access
"O:12:\"IstexOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2012.05.109\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2012\";s:9:\"\u0000*\u0000volume\";s:2:\"22\";s:8:\"\u0000*\u0000issue\";s:2:\"15\";s:8:\"\u0000*\u0000spage\";s:4:\"5084\";s:8:\"\u0000*\u0000epage\";s:4:\"5088\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:8:\"SALOVICH\";s:10:\"\u0000*\u0000aufirst\";s:7:\"James M\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:14:{i:0;s:15:\"VINSON, Paige N\";i:1;s:16:\"SCOTT DANIELS, J\";i:2;s:15:\"JEFFREY CONN, P\";i:3;s:20:\"NISWENDER, Colleen M\";i:4;s:17:\"LINDSLEY, Craig W\";i:5;s:15:\"HOPKINS, CoreyR\";i:6;s:19:\"SHEFFLER, Douglas J\";i:7;s:12:\"LAMSAL, Atin\";i:8;s:15:\"UTLEY, Thomas J\";i:9;s:15:\"BLOBAUM, Anna L\";i:10;s:17:\"BRIDGES, Thomas M\";i:11;s:8:\"LE, Uyen\";i:12;s:15:\"JONES, Carrie K\";i:13;s:15:\"WOOD, Michael R\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"5\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Istex access
"O:16:\"UnpaywallOpenUrl\":35:{s:8:\"\u0000*\u0000email\";s:27:\"assistance-portail@inist.fr\";s:6:\"\u0000*\u0000fmt\";N;s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2012.05.109\";s:6:\"\u0000*\u0000pii\";N;s:7:\"\u0000*\u0000pmid\";N;s:9:\"\u0000*\u0000atitle\";N;s:9:\"\u0000*\u0000jtitle\";N;s:9:\"\u0000*\u0000stitle\";N;s:7:\"\u0000*\u0000date\";N;s:9:\"\u0000*\u0000volume\";N;s:8:\"\u0000*\u0000issue\";N;s:8:\"\u0000*\u0000spage\";N;s:8:\"\u0000*\u0000epage\";N;s:8:\"\u0000*\u0000pages\";N;s:7:\"\u0000*\u0000issn\";N;s:8:\"\u0000*\u0000eissn\";N;s:9:\"\u0000*\u0000aulast\";N;s:10:\"\u0000*\u0000aufirst\";N;s:9:\"\u0000*\u0000auinit\";N;s:10:\"\u0000*\u0000auinitm\";N;s:5:\"\u0000*\u0000au\";N;s:9:\"\u0000*\u0000aucorp\";N;s:7:\"\u0000*\u0000isbn\";N;s:8:\"\u0000*\u0000coden\";N;s:8:\"\u0000*\u0000genre\";N;s:7:\"\u0000*\u0000part\";N;s:9:\"\u0000*\u0000btitle\";N;s:8:\"\u0000*\u0000title\";N;s:8:\"\u0000*\u0000place\";N;s:6:\"\u0000*\u0000pub\";N;s:10:\"\u0000*\u0000edition\";N;s:9:\"\u0000*\u0000tpages\";N;s:9:\"\u0000*\u0000series\";N;s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";N;}"
Unpaywall access
"O:16:\"EuropePMCOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2012.05.109\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2012\";s:9:\"\u0000*\u0000volume\";s:2:\"22\";s:8:\"\u0000*\u0000issue\";s:2:\"15\";s:8:\"\u0000*\u0000spage\";s:4:\"5084\";s:8:\"\u0000*\u0000epage\";s:4:\"5088\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:8:\"SALOVICH\";s:10:\"\u0000*\u0000aufirst\";s:7:\"James M\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:14:{i:0;s:15:\"VINSON, Paige N\";i:1;s:16:\"SCOTT DANIELS, J\";i:2;s:15:\"JEFFREY CONN, P\";i:3;s:20:\"NISWENDER, Colleen M\";i:4;s:17:\"LINDSLEY, Craig W\";i:5;s:15:\"HOPKINS, CoreyR\";i:6;s:19:\"SHEFFLER, Douglas J\";i:7;s:12:\"LAMSAL, Atin\";i:8;s:15:\"UTLEY, Thomas J\";i:9;s:15:\"BLOBAUM, Anna L\";i:10;s:17:\"BRIDGES, Thomas M\";i:11;s:8:\"LE, Uyen\";i:12;s:15:\"JONES, Carrie K\";i:13;s:15:\"WOOD, Michael R\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"5\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Europe PubMed Central access
"O:11:\"BaseOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2012.05.109\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2012\";s:9:\"\u0000*\u0000volume\";s:2:\"22\";s:8:\"\u0000*\u0000issue\";s:2:\"15\";s:8:\"\u0000*\u0000spage\";s:4:\"5084\";s:8:\"\u0000*\u0000epage\";s:4:\"5088\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:8:\"SALOVICH\";s:10:\"\u0000*\u0000aufirst\";s:7:\"James M\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:14:{i:0;s:15:\"VINSON, Paige N\";i:1;s:16:\"SCOTT DANIELS, J\";i:2;s:15:\"JEFFREY CONN, P\";i:3;s:20:\"NISWENDER, Colleen M\";i:4;s:17:\"LINDSLEY, Craig W\";i:5;s:15:\"HOPKINS, CoreyR\";i:6;s:19:\"SHEFFLER, Douglas J\";i:7;s:12:\"LAMSAL, Atin\";i:8;s:15:\"UTLEY, Thomas J\";i:9;s:15:\"BLOBAUM, Anna L\";i:10;s:17:\"BRIDGES, Thomas M\";i:11;s:8:\"LE, Uyen\";i:12;s:15:\"JONES, Carrie K\";i:13;s:15:\"WOOD, Michael R\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"5\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Base Search access
"O:12:\"ArXivOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2012.05.109\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2012\";s:9:\"\u0000*\u0000volume\";s:2:\"22\";s:8:\"\u0000*\u0000issue\";s:2:\"15\";s:8:\"\u0000*\u0000spage\";s:4:\"5084\";s:8:\"\u0000*\u0000epage\";s:4:\"5088\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:8:\"SALOVICH\";s:10:\"\u0000*\u0000aufirst\";s:7:\"James M\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:14:{i:0;s:15:\"VINSON, Paige N\";i:1;s:16:\"SCOTT DANIELS, J\";i:2;s:15:\"JEFFREY CONN, P\";i:3;s:20:\"NISWENDER, Colleen M\";i:4;s:17:\"LINDSLEY, Craig W\";i:5;s:15:\"HOPKINS, CoreyR\";i:6;s:19:\"SHEFFLER, Douglas J\";i:7;s:12:\"LAMSAL, Atin\";i:8;s:15:\"UTLEY, Thomas J\";i:9;s:15:\"BLOBAUM, Anna L\";i:10;s:17:\"BRIDGES, Thomas M\";i:11;s:8:\"LE, Uyen\";i:12;s:15:\"JONES, Carrie K\";i:13;s:15:\"WOOD, Michael R\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:184:\"Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"5\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
arXiv access
