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.

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . The Synthesis and Use of Certain Pyridine Derivatives as Modulators of the G-protein Coupled Receptors mGlu5 and P2Y12

  . Bezard E, et, al. The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model. Mov Disord. 2014 Jul;29(8):1074-9.  [Content Brief]

  . Sciamanna G, et, al. Negative allosteric modulation of mGlu5 receptor rescues striatal D2 dopamine receptor dysfunction in rodent models of DYT1 dystonia. Neuropharmacology. 2014 Oct;85:440-50.  [Content Brief]