On September 14, 2017, Bollinger, Katrina A.; Felts, Andrew S.; Brassard, Christopher J.; Engers, Julie L.; Rodriguez, Alice L.; Weiner, Rebecca L.; Cho, Hyekyung P.; Chang, Sichen; Bubser, Michael; Jones, Carrie K.; Blobaum, Anna L.; Niswender, Colleen M.; Conn, P. Jeffrey; Emmitte, Kyle A.; Lindsley, Craig W. published an article.Related Products of 386704-04-7 The title of the article was Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core. And the article contained the following:
Herein, the authors detail the optimization of the mGlu2 neg. allosteric modulator (NAM), 4-(4-fluorophenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide (VU6001192), by a reductionist approach to afford a novel, simplified mGlu2 NAM scaffold. This new chemotype not only affords potent and selective mGlu2 inhibition, as exemplified by VU6001966 (mGlu2 IC50 = 78 nM, mGlu3 IC50 > 30 μM), but also excellent central nervous system (CNS) penetration (Kp = 1.9, Kp,uu = 0.78), a feature devoid in all previously disclosed mGlu2 NAMs (Kps ≈ 0.3, Kp,uus ≈ 0.1). Moreover, this series, based on overall properties, represents an exciting lead series for potential mGlu2 PET tracer development. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Related Products of 386704-04-7
The Article related to mglu2 central nervous system penetration picolinamide pharmacokinetics, cns penetration, negative allosteric modulator (nam), vu6001966, depression, metabotropic glutamate receptor 2 (mglu2) and other aspects.Related Products of 386704-04-7
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