Discovery of VU2957 (Valiglurax): An mGlu Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease.

Joseph D Panarese,Darren W Engers,Yong-Jin Wu,Joanne J Bronson,John E Macor,Aspen Chun,Alice L Rodriguez,Andrew S Felts,Julie L Engers,Matthew T Loch,Kyle A Emmitte,Arlindo L Castelhano, Michael J Kates,Michael A Nader,Carrie K Jones,Anna L Blobaum,P Jeffrey Conn,Colleen M Niswender,Corey R Hopkins,Craig W Lindsley

ACS MEDICINAL CHEMISTRY LETTERS（2019）

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摘要

Herein, we report the discovery of a novel potent, selective, CNS penetrant, and orally bioavailable mGlu PAM, VU0652957 (VU2957, Valiglurax). VU2957 possessed attractive and 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 for the treatment of Parkinson's disease.

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关键词

Positive allosteric modulator (PAM),metabotropic glutamate receptor 4 (mGlu(4)),VU2957,Parkinson's disease

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