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The Neuroscientist, Vol. 9, No. 2, 158-168 (2003)
DOI: 10.1177/1073858403252231
© 2003 SAGE Publications

Nociceptin/Orphanin FQ: Actions within the Brain

Susanne Meis

Institut für Physiologie, Otto-von-Guericke-Universität, D-39120 Magdeburg, Germany

A peptide termed nociceptin/orphanin FQ (N/OFQ) was recently identified as an endogenous agonist for the opioid receptor-like receptor currently specified as NOP receptor. Despite many structural homologies to the opioid system, the NOP receptor shows low-affinity binding to selective opioid agonists or antagonists. Vice versa, N/OFQ selectively activates the NOP receptor but not any opioid receptor subtype. This novel receptor/ligand system is widely expressed in the brain. At the cellular level, the actions of N/OFQ resemble those elicited by opioid peptides. The NOP receptor is coupled to G-proteins, whose activation results in inhibition of adenylate cyclase, modulation of calcium and potassium conductances, and regulation of transmitter systems. At the behavioral level, systemic application of N/OFQ elicits a unique range of responses, including a wide range of effects on pain processing such as hyperalgesia, analgesia, and allodynia, as well as anxiolytic actions, modulation of opioid-mediated processes, and influences on learning and memory. NEUROSCIENTIST 9(2): 158–168, 2003.

Key Words: Nociceptin • Orphanin FQ • Neuropeptide • ORL1 receptor • NOP receptor


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