Drug intelligence / Profile preview

IC87201

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

**IC87201** is a small molecule inhibitor that selectively disrupts the interaction between postsynaptic density protein 95 (PSD-95) and neuronal nitric oxide synthase (nNOS), key components of the intracellular signaling pathway downstream of NMDA (N-methyl-D-aspartate) receptors[1][2][3][4][5][7]. Unlike NMDA antagonists, IC87201 does not affect NMDA postsynaptic currents but instead reduces NMDA-dependent production of nitric oxide and cGMP, minimizing excitotoxic neuronal injury and reducing nitrogenic stress[1][2][4][5][7]. It exhibits protective effects in models of cerebral ischemia/stroke and pain, effectively reducing infarct volume, improving neurobehavioral outcomes, and ameliorating cardiac dysfunction post-stroke in animal studies[3][4][7]. Initially discovered via high-throughput screening as a PSD95-nNOS interaction inhibitor, IC87201 acts primarily by binding to the β-finger of nNOS-PDZ and allosterically blocking the protein-protein interaction required for toxic downstream NO signaling[1][2][5].

Other names
IC87201IC-87201IC 87201
02

Targets

Postsynaptic density protein 95/Neuronal nitric oxide synthase complexNOS1 (nNOS)

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