Peptide fragment containing amino acids 1-11 of Nociceptin. Potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM); displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Displays analgesic properties in CD-1 mice.

Samidorphan HCl is an orally active and highly potent modulator of the opioid system that binds to μ‐opioid, κ‐opioid, and delta-opioid receptors. Samidorphan HCl is a novel μ-opioid receptor antagonist, a partial agonist for k-opioid and delta-opioid receptors. Samidorphan HCl can be used to prevent and treat schizophrenia.

PF-04455242 是一种有效的选择性 κ-阿片受体 (KOR) 拮抗剂，对于 hKOR/rKOR/mKOR 的 Ki 值分别为 3 nM/21 nM/22 nM。