Ontology highlight
ABSTRACT:
SUBMITTER: Panarese JD
PROVIDER: S-EPMC6421540 | biostudies-literature | 2019 Mar
REPOSITORIES: biostudies-literature
Panarese Joseph D JD Engers Darren W DW Wu Yong-Jin YJ Bronson Joanne J JJ Macor John E JE Chun Aspen A Rodriguez Alice L AL Felts Andrew S AS Engers Julie L JL Loch Matthew T MT Emmitte Kyle A KA Castelhano Arlindo L AL Kates Michael J MJ Nader Michael A MA Jones Carrie K CK Blobaum Anna L AL Conn P Jeffrey PJ Niswender Colleen M CM Hopkins Corey R CR Lindsley Craig W CW
ACS medicinal chemistry letters 20181016 3
Herein, we report the discovery of a novel potent, selective, CNS penetrant, and orally bioavailable mGlu<sub>4</sub> PAM, VU0652957 (VU2957, Valiglurax). VU2957 possessed attractive <i>in vitro</i> and <i>in vivo</i> pharmacological and DMPK properties across species. To advance toward the clinic, a spray-dried dispersion (SDD) formulation of VU2957 was developed to support IND-enabling toxicology studies. Based on its overall profile, VU2957 was evaluated as a preclinical development candidate ...[more]