Nociceptinergic system has become an important target for drug development since the identification of the "orphan", opioid-like-1 receptor and the isolation of its endogenous agonist nociceptin. Involvement of nociceptinergic system has been verified in a wide range of pathophysiological processes. A large number of nociceptinergic agonists and antagonists with peptide and non-peptide structures have been developed. Several non-peptide nociceptinergic antagonists have recently shown effective on different animal models of parkinsonism. Neuropharmacological background for antiparkinsonian effect of nociceptinergic antagonists, experimental models with high predictive value, nociceptinergic antagonists shown to have potential effect in Parkinson's disease are summarized. Medicinal chemistry data (logP and TPSA) of the NOP receptor antagonists which are found to be effective in animal models of Parkinson's disease are provided.