A selective nociceptin/orphanin FQ receptor antagonist, 7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-olhydrochloride can act as a potentially useful adjunct to chronic pain therapy with opioids and can be used to treat conditions in which thermal hyperalgesia is a significant component of the pain response.
SB-612111 is a potent antagonist of the nociceptin receptor ORL-1. SB-612111 binds to ORL-1 with high affinity (Ki = 0.33 nM) but has very low affinity for classic opioid receptors. The compound SB-612111 antagonizes the anti-morphine effects of nociceptin and blocks nociceptin-induced thermal hyperalgesia.