NMDA-IN-1 (dihydrochloride)

NMDA-IN-1 dihydrochloride is a selective NMDA NR2B antagonist with a Ki of 0.85 nM; NR2B Ca₂₊ influx IC₅₀ is 9.7 nM. NMDA-IN-1 dihydrochloride inhibits Glu/Gly stimulated Ca₂₊ flux in Ltk- cells expressing the hNR1a/NR2B with a IC₅₀ of 9.7 nM. NMDA-IN-1 dihydrochloride has no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor. NMDA-IN-1 dihydrochloride shows excellent activity in the mechanical hyperalgesia assay in rats. NMDA-IN-1 dihydrochloride can be used for the studies of stroke, parkinson, and neuropathic pain^[1]. In Vivo:NMDA-IN-1 dihydrochloride (Compound 37a) (1, 3 and 10 mg/kg, i.v., single dose) shows good activity with an ED₅₀ of <3 mg/kg in carrageenan-induced mechanical hyperalgesia model in rats^[1].
NMDA-IN-1 dihydrochloride (30 mg/kg for rats and 3 mg/kg for dogs, p.o., single dose) shows poor oral bioavailability in rat but, in contrast, demonstrated good pharmacokinetic profiles in dog^[1].