BioCentury
ARTICLE | Distillery Therapeutics

Neurology

October 3, 2018 11:28 PM UTC

Cell culture and rat studies identified a positive allosteric modulator (PAM) of mGluR4 that could help treat catalepsy in PD. Optimization and testing in human mGluR4-expressing CHO cells of a previously reported class of pyrazolopyridine-based PAMs yielded a compound that potentiated mGluR4-glutamate with an EC50 of 50.1 nM. In a rat model of haloperidol-induced PD-associated catalepsy, the compound decreased catalepsy compared with vehicle. Next steps could include testing the compound in additional animal models of PD-associated catalepsy.

Domain Therapeutics S.A. and Prexton Therapeutics S.A. have foliglurax, a small molecule mGluR4 PAM, in Phase II testing for PD...