NMDA-IN-1 dihydrochloride is a selective antagonist of the NMDA NR2B receptor, exhibiting a Ki of 0.85 nM and an IC50 of 9.7 nM for NR2B-mediated Ca2+ influx. This compound effectively inhibits Glu/Gly-stimulated Ca2+ flux in Ltk- cells expressing hNR1a/NR2B, demonstrating specificity as it does not interact with NR2A, NR2C, NR2D, hERG channels, or α1-adrenergic receptors. NMDA-IN-1 dihydrochloride displays significant efficacy in mechanical hyperalgesia models in rats and is relevant for investigations into stroke, Parkinson's disease, and neuropathic pain.
NMDA-IN-1 dihydrochloride is a selective antagonist of the NMDA NR2B receptor, exhibiting a Ki of 0.85 nM and an IC50 of 9.7 nM for NR2B-mediated Ca2+ influx. This compound effectively inhibits Glu/Gly-stimulated Ca2+ flux in Ltk- cells expressing hNR1a/NR2B, demonstrating specificity as it does not interact with NR2A, NR2C, NR2D, hERG channels, or α1-adrenergic receptors. NMDA-IN-1 dihydrochloride displays significant efficacy in mechanical hyperalgesia models in rats and is relevant for investigations into stroke, Parkinson's disease, and neuropathic pain.
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