Discovery and Characterization of (R)‑6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1‑c][1,4]oxazin-4(9H)‑one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates - Stepan, Antonia F; Claffey, Michelle M; Reese, Matthew R; Balan, Gayatri; Barreiro, Gabriela; Barricklow, Jason; Bohanon, Michael J; Boscoe, Brian P; Cappon, Gregg D; Chenard, Lois K; Cianfrogna, Julie; Chen, Laigao; et al. (Journal of medicinal chemistry, 2017)
Keywords: Allosteric Regulation - drug effects; Animals; Chemistry, Medicinal; Female; HEK293 Cells; Heterocyclic Compounds, 3-Ring - adverse effects; Heterocyclic Compounds, 3-Ring - chemistry; Heterocyclic Compounds, 3-Ring - pharmacokinetics; Heterocyclic Compounds, 3-Ring - pharmacology; Humans; Life Sciences & Biomedicine; Male; Molecular Docking Simulation; Pharmacology & Pharmacy; Pyridines - adverse effects; Pyridines - chemistry; Pyridines - pharmacokinetics; Pyridines - pharmacology; Rats; Rats, Sprague-Dawley; Receptor, Metabotropic Glutamate 5 - antagonists & inhibitors; Receptor, Metabotropic Glutamate 5 - metabolism; Science & Technology; Structure-Activity Relationship; MEDICINAL CHEMISTRY; ANTAGONIST; CLINICAL DEVELOPMENT; ANXIOLYTIC-LIKE; BASIMGLURANT; MGLU5 RECEPTOR; TOXICITY; BLOCKADE; DRUG TARGETS; PREDICTION