An NMDA receptor antagonist
Radiprodil is an antagonist of NR2B subunit-containing NMDA receptors (IC50 = 8 nM).1 It is selective for NR2B subunit-containing NMDA receptors over NR1 and NR2A subunit-containing NMDA receptors at 15 ?M. Radiprodil (10 nM) reduces amyloid β (1-42) (Aβ42) and Aβ40-induced decreases in dendritic spine density in mouse hippocampal CA1 pyramidal neurons.2 Radiprodil (2 mg/kg) restores novel object-stimulated locomotion in a marmoset model of MPTP-induced Parkinson's disease.3
1.Barta-Szalai, G., Borza, I., Bozó, E., et al.Oxamides as novel NR2B selective NMDA receptor antagonistsBioorg. Med. Chem. Lett.14(15)3953-3956(2004) 2.Rammes, G., Seeser, F., Mattusch, K., et al.The NMDA receptor antagonist radiprodil reverses the synaptotoxic effects of different amyloid-beta (Ab) species on long-term potentiation (LTP)Neuropharmacology140(10)184-192(2018) 3.Michel, A., Nicolas, J.M., Rose, S., et al.Antiparkinsonian effects of the "Radiprodil and Tozadenant" combination in MPTP-treated marmosetsPLoS One12(8)e0182887(2017)
动态评分
0.0