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Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor
Abstract
A heptadecapeptide was identified and purified from porcine brain tissue as a ligand for an orphan heterotrimeric GTP- binding protein (G protein)- coupled receptor (LC132) that is similar in sequence to opioid receptors. This peptide, orphanin FQ, has a primary structure reminiscent of that of opioid peptides. Nanomolar concentrations of orphanin FQ inhibited forskolin-stimulated adenylyl cyclase activity in cells transfected with LC132. This inhibitory activity was not affected by the addition of opioid ligands, nor did the peptide activate opioid receptors. Orphanin FQ bound to its receptor in a saturable manner and with high affinity. When injected intracerebroventricularly into mice, orphanin FQ caused a decrease in locomotor activity but did not induce analgesia in the hot-plate test. However, the peptide produced hyperalgesia in the tail-flick assay. Thus, orphanin FQ may act as a transmitter in the brain by modulating nociceptive and locomotor behavior.
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Cited by
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Kojima, M., Hosoda, H., Date, Y., Nakazato, M., Matsuo, H., & Kangawa, K. (1999) · Nature · doi:10.1038/45230 · Cited by 8,479
Ghrelin: Structure and Function
Kojima, M., & Kangawa, K. (2005) · Physiological Reviews · doi:10.1152/physrev.00012.2004 · Cited by 2,810
Kotani, M., Detheux, M., Vandenbogaerde, A., Communi, D., Vanderwinden, J.-M., Le Poul, E., Brézillon, S., Tyldesley, R., Suarez-Huerta, N., Vandeput, F., et al. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.m104847200 · Cited by 1,546
Models and Mechanisms of Hyperalgesia and Allodynia
Sandkühler, J. (2009) · Physiological Reviews · doi:10.1152/physrev.00025.2008 · Cited by 1,148
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Han, J.-S. (2003) · Trends in Neurosciences · doi:10.1016/s0166-2236(02)00006-1 · Cited by 1,084
Metadata
- Authors
- Reinscheid, R. K., Nothacker, H.-P., Bourson, A., Ardati, A., Henningsen, R. A., Bunzow, J. R., Grandy, D. K., Langen, H., Monsma, F. J., & Civelli, O.
- Venue
- Science
- Published
- 1995-11-03
- Volume
- 270
- Issue
- 5237
- Pages
- 792-794
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2016562510
- Cited by
- 1,821
- References
- 0
- FWCI
- 29.48
- Type
- journal article
- Language
- en
- Open access
- closed
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- The paper
- Reinscheid, R. K., Nothacker, H.-P., Bourson, A., Ardati, A., Henningsen, R. A., Bunzow, J. R., Grandy, D. K., Langen, H., Monsma, F. J., & Civelli, O. (1995). Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor. Science. https://doi.org/10.1126/science.270.5237.792
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.