Department of Pharmacodynamics, H-1089 Nagyvarad ter 4, Budapest, Hungary.
Mini Rev Med Chem. 2013 Aug;13(10):1389-97. doi: 10.2174/13895575113139990006.
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.
痛觉感受系统已成为药物研发的一个重要靶点，因为“孤儿”阿片样物质-1 受体的鉴定和其内源性激动剂孤啡肽的分离。痛觉感受系统的参与已在广泛的病理生理过程中得到证实。已经开发出大量具有肽和非肽结构的痛觉感受系统激动剂和拮抗剂。最近，一些非肽类的痛觉感受系统拮抗剂在不同的帕金森病动物模型中显示出有效。总结了痛觉感受系统拮抗剂抗帕金森作用的神经药理学背景、具有高预测价值的实验模型，以及痛觉感受系统拮抗剂在帕金森病中显示出的潜在作用。提供了在帕金森病动物模型中有效的 NOP 受体拮抗剂的药物化学数据（logP 和 TPSA）。
