raseglurant (ADX-10059) / Addex - LARVOL DELTA

Design and validation of a low-cost photomodulator for in vivo photoactivation of a mGluR5 inhibitor. (PubMed, Biomed Eng Lett) - "They demonstrate the in vivo capabilities of the photomodulator by photoreleasing raseglurant, an mGluR5 inhibitor, to treat pain in an acute rat model and follow this study by showing how to reconfigure the photomodulator to work wirelessly and interface with other biomedical devices. The online version contains supplementary material available at 10.1007/s13534-023-00334-3."

Journal • Preclinical • Pain

Clinical investigations of compounds targeting metabotropic glutamate receptors. (PubMed, Pharmacol Biochem Behav) - "PET ligands for mGlu5Rs have been studied in a range of patient populations and several mGlu5R antagonists have been tested for potential efficacy in patients including mavoglurant, diploglurant, basimglurant, GET 73, and ADX10059...Fenobam was approved for use as an anxiolytic prior to its recognition as an mGlu5R antagonist. mGlu2/3R agonists (pomaglumated methionil) and mGlu2R agonists (JNJ-40411813, AZD 8529, and LY2979165) have been studied in patients with schizophrenia with promising but mixed results. Antagonists of mGlu2/3Rs (decoglurant and TS-161) have been studied in depression where TS-161 has advanced into a planned Phase 2 study in treatment-resistant depression...The mGlu4R potentiator, foliglurax, did not meet its primary endpoint in patients with Parkinson's disease. Ongoing efforts to develop mGluR-targeted compounds continue to promise these glutamate modulators as medicines for psychiatric and neurological disorders."

Journal • CNS Disorders • Depression • Developmental Disorders • Epilepsy • Fragile X Syndrome • Gastroenterology • Gastroesophageal Reflux Disease • Genetic Disorders • Mental Retardation • Mood Disorders • Movement Disorders • Pain • Parkinson's Disease • Psychiatry • Schizophrenia

The mGlu Receptor Protomer-Mediated Dopamine D Receptor Trans-Inhibition Is Dependent on the Adenosine A Receptor Protomer: Implications for Parkinson's Disease. (PubMed, Mol Neurobiol) - "In agreement, the mGluR-negative allosteric modulator raseglurant significantly reduced the haloperidol-induced catalepsy in mice, and in AR knockout mice, the haloperidol action had almost disappeared, supporting a functional role for mGluR and AR in enhancing DR blockade resulting in catalepsy. The results represent a relevant example of integrative activity within higher-order heteroreceptor complexes."

Journal • CNS Disorders • Movement Disorders • Parkinson's Disease