IC87201 is a nNOS-PDZ/PSD-95-PDZ inhibitor. IC87201 showed great promise in cellular experiments and animal models of ischemic stroke and pain. IC87201 inhibited the in vitro binding of nNOS with PSD95, without inhibiting nNOS catalytic activity. nNOS-PSD95 interaction is important in maintaining hypersensitivity in acute and chronic pain. Disruption of the nNOS-PSD95 interaction provides a novel approach to obtain selective anti-hyperalgesic compounds.