Back to Search
Start Over
RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia
- Source :
- Proceedings of the National Academy of Sciences of the United States of America, Proceedings of the National Academy of Sciences of the United States of America, National Academy of Sciences, 2006, 103 (2), pp.466-71. ⟨10.1073/pnas.0502090103⟩, Proceedings of the National Academy of Sciences of the United States of America, National Academy of Sciences, 2006, 103, pp.466-471
- Publication Year :
- 2006
- Publisher :
- HAL CCSD, 2006.
-
Abstract
- International audience; 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.
- Subjects :
- Receptors, Neuropeptide
Neuropeptide FF receptor
Adamantane
Blood Pressure
Pharmacology
Ligands
MESH: Analgesics, Opioid
0302 clinical medicine
MESH: Dipeptides
Heart Rate
Drug tolerance
Chlorocebus aethiops
MESH: Ligands
MESH: Animals
Neuropeptide FF
MESH: Heart Rate
Receptor
0303 health sciences
Multidisciplinary
Molecular Structure
Chemistry
MESH: Receptors, Neuropeptide
Chronic pain
Sciences du Vivant [q-bio]/Biotechnologies
Dipeptides
Drug Tolerance
MESH: Adamantane
MESH: Blood Pressure
Biological Sciences
MESH: Amides
3. Good health
Analgesics, Opioid
MESH: COS Cells
Hyperalgesia
COS Cells
MESH: Heroin
medicine.symptom
medicine.drug
MESH: Rats
MESH: Drug Tolerance
MESH: Molecular Structure
03 medical and health sciences
medicine
Animals
Humans
030304 developmental biology
MESH: Humans
Antagonist
[SDV.BBM.BM]Life Sciences [q-bio]/Biochemistry, Molecular Biology/Molecular biology
medicine.disease
Amides
MESH: Hyperalgesia
MESH: Cercopithecus aethiops
Rats
Heroin
Opioid
030217 neurology & neurosurgery
Subjects
Details
- Language :
- English
- ISSN :
- 00278424 and 10916490
- Database :
- OpenAIRE
- Journal :
- Proceedings of the National Academy of Sciences of the United States of America, Proceedings of the National Academy of Sciences of the United States of America, National Academy of Sciences, 2006, 103 (2), pp.466-71. ⟨10.1073/pnas.0502090103⟩, Proceedings of the National Academy of Sciences of the United States of America, National Academy of Sciences, 2006, 103, pp.466-471
- Accession number :
- edsair.doi.dedup.....71a395a851dbe8bb2ccae817ae506023