Auglurant, formerly known as VU0424238, is a Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. VU0424238 is more than 900-fold selective for mGlu5 versus the other mGlu receptors, and binding studies established a Ki of 4.4 nM at a known allosteric binding site. VU0424238 had a clearance of 19.3 and 15.5 mL/min/kg in rats and cynomolgus monkeys, respectively. Imaging studies using a known mGlu5 PET ligand demonstrated 50% receptor occupancy at an orally bioavailable dose of 0.8 mg/kg in rats and an intravenous dose of 0.06 mg/kg in baboons. References: Felts AS, Rodriguez AL, Blobaum AL, Morrison RD, Bates BS, Thompson Gray A, Rook JM, Tantawy MN, Byers FW, Chang S, Venable DF, Luscombe VB, Tamagnan GD, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide(VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. J Med Chem. 2017 May 31. doi: 10.1021/acs.jmedchem.7b00410. [Epub ahead of print] PubMed PMID: 28530802.

纯度：≥98%

CAS：1396337-04-4