SHA-68 is an antagonist of the neuropeptide S receptor (NPSR; IC50s = 22 and 23.8 nM for the NPSR Asn107 and NPSR Ile107 isoforms, respectively). It is selective for NPSR over a panel of 14 G protein-coupled receptors exhibiting no activity at a concentration of 10 μM. SHA-68 (50 mg/kg) reduces NPS-induced horizontal activity and vertical rearing and climbing in mice. SHA-68 also reduces conditioned reinstatement of cocaine seeking in rats.
