Nociceptin produces antinociception after spinal administration in amphibians.

Pharmacol Biochem Behav

Department of Pharmacology and Physiology, Oklahoma State University-Center for Health Sciences, College of Osteopathic Medicine, Tulsa, OK 74107-1898, USA.

Published: January 2009

Nociceptin, also known as orphanin FQ, is a opioid-like neuropeptide that mediates its effects at the nociceptin receptor, a member of the G protein-coupled receptor superfamily. In mammals, nociceptin produces analgesia after spinal administration, however the role of nociceptin and nociceptin receptors in the modulation of noxious stimuli in non-mammalian species has not been examined. In an amphibian pain model using the acetic acid test with Rana pipiens, nociceptin and nociceptin1-13 amide produced dose-dependent antinociception (1-100 nmol), blocked by the nociceptin antagonist, [Nphe1]-nociceptin1-13 amide (30 nmol), but not the opioid antagonist, naltrexone (100 nmol/g, s.c.). Conversely, the antinociceptive effects of micro, delta, and kappa opioid receptor agonists were not blocked by the nociceptin antagonist. Nociceptin and nociceptin1-13 amide were the least potent of the opioid agonists tested. These studies demonstrate that spinal nociceptin receptors and not opioid receptors mediate the antinociceptive effect of nociceptin. Considered with previous findings, these behavioral data supports a role for nociceptin inhibition of spinal nociception in amphibians and perhaps all vertebrates.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2662521PMC
http://dx.doi.org/10.1016/j.pbb.2008.08.022DOI Listing

Publication Analysis

Top Keywords

nociceptin
13
nociceptin produces
8
spinal administration
8
role nociceptin
8
nociceptin receptors
8
nociceptin nociceptin1-13
8
nociceptin1-13 amide
8
blocked nociceptin
8
nociceptin antagonist
8
produces antinociception
4

Similar Publications

Recommended Opioid Receptor Tool Compounds: Comparative for Receptor Selectivity Profiles and for Pharmacological Antinociceptive Profiles.

ACS Pharmacol Transl Sci

January 2025

Department of Medicinal Chemistry and Institute for Translational Neuroscience, University of Minnesota, Minneapolis, Minnesota 55455, United States.

Opioid agonist ligands bind opioid receptors and stimulate downstream signaling cascades for various biological processes including pain and reward. Historically, before cloning the receptors, muscle contraction assays using isolated organ tissues were used followed by radiolabel ligand binding assays on native tissues. Upon cloning of the opioid G protein-coupled receptors (GPCRs), cell assays using transfected opioid receptor DNA plasmids became the standard practice including S-GTPγS functional and cAMP based assays.

View Article and Find Full Text PDF

The N/OFQ-NOP receptor is a fascinating peptidergic system with the potential to be exploited for the development of analgesic drugs devoid of side effects associated with classical opioid signalling modulation. To date, up to four X-ray and cryo-EM structures of the NOP receptor in complex with the endogenous peptide agonist N/OFQ and three small molecule antagonists have been solved and released. Despite the available structural information, the details of selective small molecule agonist binding to the NOP receptor in the active state remain elusive.

View Article and Find Full Text PDF

Nuclear Factor-κB Signaling Regulates the Nociceptin Receptor but Not Nociceptin Itself.

Cells

December 2024

Department of Anaesthesiology and Pain Medicine, Inselspital, Bern University Hospital, University of Bern, 3010 Bern, Switzerland.

The nociceptin receptor (NOP) and nociceptin are involved in the pathways of pain and inflammation. The potent role of nuclear factor-κB (NFκB) in the modulation of tumor necrosis factor-α (TNF-α) and interleukin (IL)-1β on the nociceptin system in human THP-1 cells under inflammatory conditions were investigated. Cells were stimulated without/with phorbol-myristate-acetate (PMA), TNF-α, IL-1β, or PMA combined with individual cytokines.

View Article and Find Full Text PDF

Circuit influences on the midbrain dopamine system are crucial to adaptive behavior and cognition. Recent developments in the study of neuropeptide systems have enabled high-resolution investigations of the intersection of neuromodulatory signals with basal ganglia circuitry, identifying the nociceptin/orphanin FQ (N/OFQ) endogenous opioid peptide system as a prospective regulator of striatal dopamine signaling. Using a prepronociceptin-Cre reporter mouse line, we characterized highly selective striosomal patterning of Pnoc mRNA expression in mouse dorsal striatum, reflecting the early developmental expression of Pnoc.

View Article and Find Full Text PDF

The endocannabinoid system (ECS) and nociceptin receptor (NOP) have been implicated in the pathology of inflammatory bowel diseases (IBD) mediating pain and alleviating inflammation. In this study we searched for the possible activation of ECS and NOP system and the correlation between CB1, CB2 and NOP receptors in IBD patients. Patients diagnosed with IBDs who underwent colonic surgical resection or biopsy at colonoscopy and control group (patients without diagnosis of IBD, which colonoscopy for the different medical indications) were recruited into the study.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!