On February 1, 2015, Kurata, Haruto; Gentry, Patrick R.; Kokubo, Masaya; Cho, Hyekyung P.; Bridges, Thomas M.; Niswender, Colleen M.; Byers, Frank W.; Wood, Michael R.; Daniels, J. Scott; Conn, P. Jeffrey; Lindsley, Craig W. published an article.Quality Control of 1-Fluoro-2-methoxybenzene The title of the article was Further optimization of the M5 NAM MLPCN probe ML375: Tactics and challenges. And the article contained the following:
This Letter describes the continued optimization of the MLPCN probe ML375, a highly selective M5 neg. allosteric modulator (NAM), through a combination of matrix libraries and iterative parallel synthesis. True to certain allosteric ligands, SAR was shallow, and the matrix library approach highlighted the challenges with M5 NAM SAR within in this chemotype. Once again, enantiospecific activity was noted, and potency at rat and human M5 were improved over ML375, along with slight enhancement in physiochem. properties, certain in vitro DMPK parameters and CNS distribution. Attempts to further enhance pharmacokinetics with deuterium incorporation afforded mixed results, but pretreatment with a pan-P 450 inhibitor (1-aminobenzotriazole; ABT) provided increased plasma exposure. The experimental process involved the reaction of 1-Fluoro-2-methoxybenzene(cas: 321-28-8).Quality Control of 1-Fluoro-2-methoxybenzene
The Article related to enantiospecific activity, m(5), matrix library, muscarinic receptor, negative allosteric modulator, pharmacokinetics, Pharmacology: Structure-Activity and other aspects.Quality Control of 1-Fluoro-2-methoxybenzene
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Ether | (C2H5)2O – PubChem