Dipraglurant

Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC₅₀ of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo^[1][2]. Dipraglurant is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. In Vitro: Dipraglurant (1-10 μM; 15 min) counteracts the abnormal membrane responses and calcium rise induced either by the D2R agonist quinpirole or by caged dopamine (NPEC-Dopamine)^[3]. In Vivo: Dipraglurant (3-30 mg/kg; a single p.o.) reduces L-dopa-induced chorea and dystonia and does not interfere with the ef cacy of L-dopa in treating parkinsonian disability macaque^[1].
Dipraglurant exhibits C_max (1.040, 1.380, 5.310 ng/mL) T_max (1.0, 0.5, 1.0 h) and AUC_inf (2.230, 2.860, 15.700) following p.o. administration (3, 10, 30 mg/kg) in macaque^[1].