Ro 64-6198 hydrochloride is a nonpeptidic, selective, brain-penetrant agonist of nociceptin/orphanin FQ receptor (NOP receptor/ORL1) with pKi of 9.41.
Ro 64-6198 displays >100-fold selectivity for ORL1 over other members of opioid receptor family.
Ro 64-6198 elicits dose-dependent anxiolytic-like effects in models of distinct types of anxiety states in rata, with no efficient anti-panic-like activity, absence of anticonvulsant properties, and lack of effects on motor performance and cognitive function at anxiolytic doses (0.3 to 3 mg/kg i.p.).
