The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia
Open accessAbstract
Neuropeptide FF (NPFF) has been proposed to play a role in pain modulation, opioid tolerance, and several other physiological processes. However, pharmacological agents that would help define physiological roles for this peptide are still missing. Here we report the discovery of a potent and selective NPFF receptor antagonist, RF9, that can be administered systemically. This compound does not show any effects by itself but can block efficiently the increase in blood pressure and heart rate evoked by NPFF. When chronically coinjected with heroin, RF9 completely blocks the delayed and long-lasting paradoxical opioid-induced hyperalgesia and prevents the development of associated tolerance. Our data indicate that NPFF receptors are part of a bona fide antiopioid system and that selective antagonists of these receptors could represent useful therapeutic agents for improving the efficacy of opioids in chronic pain treatment.
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Citations
Cites
Long-lasting Hyperalgesia Induced by Fentanyl in Rats: Preventive Effect of Ketamine
Célèrier, E., Rivat, C., Jun, Y., Laulin, J.-P., Larcher, A., Reynier, P., & Simonnet, G. (2000) · Anesthesiology · doi:10.1097/00000542-200002000-00029 · Cited by 584
Self-citationCélèrier, E., Laulin, J.-P., Corcuff, J.-B., Le Moal, M., & Simonnet, G. (2001) · The Journal of Neuroscience · doi:10.1523/jneurosci.21-11-04074.2001 · Cited by 315
Self-citationOpioid-induced hyperalgesia: abnormal or normal pain?
Simonnet, G., & Rivat, C. (2003) · NeuroReport · doi:10.1097/00001756-200301200-00001 · Cited by 273
Self-citation
Cited by
The Lipophilic Bullet Hits the Targets: Medicinal Chemistry of Adamantane Derivatives
Wanka, L., Iqbal, K., & Schreiner, P. R. (2013) · Chemical Reviews · doi:10.1021/cr100264t · Cited by 696
Multiple primary cilia modulate the fluid transcytosis in choroid plexus epithelium
Narita, K., Kawate, T., Kakinuma, N., & Takeda, S. (2010) · Traffic · doi:10.1111/j.1600-0854.2009.01016.x · Cited by 97
RF9 Rescues Cortisol-Induced Repression of Testosterone Levels in Adult Male Macaques
Ullah, R., Naz, R., Batool, A., Wazir, M., Rahman, T. U., Nabi, G., Wahab, F., Fu, J., & Shahab, M. (2021) · Frontiers in Physiology · doi:10.3389/fphys.2021.630796 · Cited by 8
Metadata
- Authors
- Simonin, F., Schmitt, M., Laulin, J.-P., Laboureyras, E., Jhamandas, J. H., MacTavish, D., Matifas, A., Mollereau, C., Laurent, P., Parmentier, M., Kieffer, B. L., Bourguignon, J.-J., & Simonnet, G.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2006-01-03
- Volume
- 103
- Issue
- 2
- Pages
- 466-471
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W1984553637
- Cited by
- 230
- References
- 3
- FWCI
- 3.47
- Type
- journal article
- Language
- en
- Open access
- green
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- The paper
- Simonin, F., Schmitt, M., Laulin, J.-P., Laboureyras, E., Jhamandas, J. H., MacTavish, D., Matifas, A., Mollereau, C., Laurent, P., Parmentier, M., Kieffer, B. L., Bourguignon, J.-J., & Simonnet, G. (2006). RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.0502090103
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