Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrantmGluR5negative allosteric modulator (NAM), with anIC₅₀of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo^[1][2].

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].

Dipraglurant (3-30 mg/kg; a single p.o.) reduces L-dopa-induced chorea and dystonia and does not interfere with the efficacy 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].

265.29

Solid

C₁₆H₁₂FN₃

872363-17-2

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 40 mg/mL(150.78 mM)

*"≥" means soluble, but saturation unknown.

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