Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor

Autor:	Robert F. Bruns, Qi Chen, Paloma Vidal, John Mehnert Schaus, Charles R. Yang, Stephen N. Mitchell, Steven Marc Massey, Nuria Diaz, Xushan Wang, David Andrew Coates, Rebecca A. Wright, Beverly A. Heinz, Kevin Matthew Gardinier, Greg Stephenson, James P. Beck, Rajni M. Bhardwaj, Julie F. Falcone, Bruce A. Dressman, Deanna L Maren, Anette M. Johansson, David Michael Remick, Jeff W. Cramer, Cohen Michael Philip, Brian Morgan Watson, Jeffery Richardson, Kjell Svensson, Xin Zhou, Erik James Hembre, Serge Louis Boulet, Reinhard Matthew Robert, Daniel S. Richards, Junliang Hao, David M. Bender, Guy Carter, Christopher David Beadle, Brian G. Getman, Wolfangel Craig Daniel, Diseroad Benjamin Alan, Jason K. Myers, Joseph H. Krushinski, David Edward Tupper
Rok vydání:	2019
Předmět:	0303 health sciences Catechol Allosteric modulator Stereochemistry Subtype selective 01 natural sciences 0104 chemical sciences 010404 medicinal & biomolecular chemistry 03 medical and health sciences chemistry.chemical_compound Dopamine receptor D1 chemistry Dopamine Drug Discovery medicine Molecular Medicine Hydroxymethyl 030304 developmental biology medicine.drug
Zdroj:	Journal of Medicinal Chemistry. 62:8711-8732
ISSN:	1520-4804 0022-2623
Popis:	Clinical development of catechol-based orthosteric agonists of the dopamine D1 receptor has thus far been unsuccessful due to multiple challenges. To address these issues, we identified LY3154207 (...
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::5a353395d3c6f7ca6dfa78c95a347dd4 https://doi.org/10.1021/acs.jmedchem.9b01234 Zobrazit plný text záznamu