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Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor

Reinscheid, Rainer K., Nothacker, Hans-Peter, Bourson, Anne, Ardati, Ali, Henningsen, Robert A., Bunzow, James R., Grandy, David K., Langen, Hanno, Monsma, Frederick J., Civelli, Olivier·1995·Science

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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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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CoChat. (2026). Citation check: Orphanin FQ: A Neuropeptide That Activates an Opioidlike G Protein-Coupled Receptor. https://app.cochat.ai/papers/10.1126/science.270.5237.792
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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.