Nociceptin/orphanin FQ binding increases in superficial laminae of the rat spinal cord during persistent peripheral inflammation
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Acknowledgements
These studies were supported by a grant from NINDS (NS17702). D.R.L. was supported by a grant from NIDA (T32DA07234).
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Nociceptin/orphanin FQ opioid peptide (NOP) receptor and µ-opioid peptide (MOP) receptors both contribute to the anti-hypersensitive effect of cebranopadol in a rat model of arthritic pain
2018, European Journal of PharmacologyCitation Excerpt :Functional NOP and MOP receptors are expressed at peripheral, spinal and supraspinal sites of descending and ascending pain pathways (Schröder et al., 2014) and cebranopadol may target both receptor systems to provide an anti-hypersensitive effect following systemic administration. The involvement of the NOP system in modulating inflammatory nociception is also supported by observations in rat models of up-regulation of spinal NOP receptors 4 days after CFA-induced inflammation (Jia et al., 1998) and up-regulation of NOP receptors and nociceptin/orphanin FQ peptide in dorsal root ganglion neurons 7 days after CFA-induced inflammation (Chen and Sommer, 2006). Assessment of the anti-hypersensitive effect of cebranopadol on day 5 after CFA injection in the present study falls within both the period of pronounced changes in weight bearing and the previously reported period of up-regulation of the NOP system.
Central N/OFQ-NOP Receptor System in Pain Modulation
2016, Advances in PharmacologyCitation Excerpt :These NOP receptor agonist-induced antihyperalgesic and antiallodynic effects might be at least in part explained by an upregulation of the NOP receptors in the spinal cord under these painful conditions. In fact, expression of N/OFQ and the NOP receptor were upregulated in the dorsal horn of rats under carrageenan- and CFA-induced inflammation, respectively (Jia, Linden, Serie, & Seybold, 1998; Rosen, Lundeberg, Bytner, & Nylander, 2000). Importantly, the NOP receptor was also upregulated in the dorsal horn of rats with CCI (Briscini, Corradini, Ongini, & Bertorelli, 2002) and the inhibitory effect of N/OFQ on spinal wide dynamic range neurons was enhanced in rats under neuropathic pain (Sotgiu, Bellomi, & Biella, 2004).
Intrathecal administration of nociceptin/orphanin FQ receptor agonists in rats: A strategy to relieve chemotherapy-induced neuropathic hypersensitivity
2015, European Journal of PharmacologyCitation Excerpt :N/OFQ and the NOP receptor exhibit sequence homology with members of the opioid receptor family although N/OFQ displays low affinity for classical opioid receptors as demonstrated by in vitro and in vivo studies (Lambert, 2008). In rodent, the NOP system is upregulated in brain and spinal cord under both neuropathic and inflammatory pain conditions (Briscini et al., 2002; Jia et al., 1998). The activation of the NOP receptors after N/OFQ administration is able to modulate nociception in acute, neuropathic and inflammatory pain (Hao et al., 1997; Obara et al., 2005; Tian et al., 1997) highlighting the NOP system as exploitable target for neuropathic pain treatment.
The role of nociceptin and dynorphin in chronic pain: Implications of neuro-glial interaction
2011, NeuropeptidesCitation Excerpt :This presence may be important for the role of the NOC system in pain conditions, especially in inflammation, and may influence the level of detectable NOP receptor mRNA in these conditions. Furthermore, Jia et al. (1998) showed an increase in NOC binding sites in the DRG 4 days after an injection of complete Freund’s adjuvant. Considering that NOC has both pronociceptive and antinociceptive properties (Calo et al., 1998, 2000b; Mogil and Pasternak, 2001), it remains to be determined whether the activation of the NOC system in the DRG after peripheral nerve injury is associated with hyperalgesia or with the suppression of nociceptive hypersensitivity.
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H- benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: Design, synthesis, and structure-activity relationships
2010, Bioorganic and Medicinal ChemistryRole of opioid receptors in the reduction of formalin-induced secondary allodynia and hyperalgesia in rats
2009, European Journal of Pharmacology