Winters Bryony L, Christie Macdonald J, Vaughan Christopher W
Pain Management Research Institute, Kolling Institute of Medical Research, Northern Clinical School, Faculty of Medicine and Health, The University of Sydney and Royal North Shore Hospital, St Leonards, NSW, Australia.
Discipline of Pharmacology, Faculty of Medicine and Health, The University of Sydney, Camperdown, NSW, Australia.
Handb Exp Pharmacol. 2019;254:91-130. doi: 10.1007/164_2019_205.
Whilst the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) has similar intracellular coupling mechanisms to opioid receptors, it has distinct modulatory effects on physiological functions such as pain. These actions range from agonistic to antagonistic interactions with classical opioids within the spinal cord and brain, respectively. Understanding the electrophysiological actions of N/OFQ has been crucial in ascertaining the mechanisms by which these agonistic and antagonistic interactions occur. These similarities and differences between N/OFQ and opioids are due to the relative location of NOP versus opioid receptors on specific neuronal elements within these CNS regions. These mechanisms result in varied cellular actions including postsynaptic modulation of ion channels and presynaptic regulation of neurotransmitter release.
虽然痛敏肽/孤啡肽FQ(N/OFQ)受体(NOP)与阿片受体具有相似的细胞内偶联机制,但它对疼痛等生理功能具有独特的调节作用。这些作用分别在脊髓和脑内与经典阿片类药物产生从激动到拮抗的相互作用。了解N/OFQ的电生理作用对于确定这些激动和拮抗相互作用发生的机制至关重要。N/OFQ与阿片类药物之间的这些异同是由于NOP与阿片受体在这些中枢神经系统区域特定神经元成分上的相对位置。这些机制导致多种细胞作用,包括离子通道的突触后调制和神经递质释放的突触前调节。