IC87201

IC87201 is an inhibitor of the protein-protein interaction between neuronal nitric oxide synthase (nNOS) and post-synaptic density protein 95 (PSD-95).¹ It inhibits the binding of PSD-95 to nNOS (IC₅₀ = 31 µM). IC87201 inhibits NMDA-induced cGMP production, a marker of PSD-95-dependent NOS activation, in primary rat hippocampal neurons (IC₅₀ = 2.7 µM). IC87201 (10 µM) reduces MPP⁺-induced production of reactive oxygen species (ROS), cytochrome c release, and apoptosis in primary rat cortical neurons.² In vivo, IC87201 decreases thermal hyperalgesia in mice (ED₅₀ = 0.1 mg/kg), as well as mechanical allodynia in a rat model of neuropathic pain induced by chronic constriction injury (CCI). It also reduces immobility time in the forced swim and tail suspension tests in mice when administered at a dose of 1 mg/kg.³

WARNING This product is not for human or veterinary use.

1. Florio, S.K., Loh, C., Huang, S.M., et al. Disruption of nNOS-PSD95 protein-protein interaction inhibits acute thermal hyperalgesia and chronic mechanical allodynia in rodents. Br. J. Pharmacol. 158(2), 494-506 (2009).

2. Hu, W., Guan, L.-S., Dang, X.-B., et al. Small-molecule inhibitors at the PSD-95/nNOS interface attenuate MPP+-induced neuronal injury through Sirt3 mediated inhibition of mitochondrial dysfunction. Neurochem. Int. 79, 57-64 (2014).

3. Doucet, M.V., Levine, H., Dev, K.K., et al. Small-molecule inhibitors at the PSD-95/nNOS interface have antidepressant-like properties in mice. Neuropsychopharmacology 38(8), 1575-1584 (2013).