872363-17-2

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, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

mGluR5: 21 nM (IC₅₀)

[1] The Synthesis and Use of Certain Pyridine Derivatives as Modulators of the G-protein Coupled Receptors mGlu5 and P2Y12
[2] 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. DOI:10.1002/mds.25920
[3] 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. DOI:10.1016/j.neuropharm.2014.06.013