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 study of stroke, Parkinson, and neuropathic pain^[1].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

412.33

C₂₀H₂₄Cl₂FN₃O

1784252-90-9

OC1=CC=C2N=C(CN3CCC(CC4=CC=CC=C4F)CC3)NC2=C1.Cl.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. McCauley JA,et al. NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. J Med Chem. 2004 Apr 8;47(8):2089-96.  [Content Brief]