Anti-opioid activities of NPFF1 receptors in a SH-SY5Y model.
In order to elucidate the mechanisms of the neuronal anti-opioid activity of Neuropeptide FF, we have transfected the SH-SY5Y neuroblastoma cell line, which expresses mu- and delta-opioid receptors, with the human NPFF1 receptor. The SH1-C7 clone expresses high affinity NPFF1 receptors in the same range order of density as opioid receptors. Similarly to the opioids, acute stimulation with the NPFF1 agonist NPVF inhibits adenylyl cyclase activity and voltage-gated (N-type) Ca2+ currents and enhances the intracellular Ca2+ release triggered by muscarinic receptors activation. In contrast, preincubation of cells with NPVF decreases the response to opioids on both calcium signaling, thus reproducing the cellular anti-opioid activity described in neurons. SH1-C7 cells are therefore a suitable model to investigate the interactions between NPFF and opioid receptors.
Institut de Pharmacologie et de Biologie Structurale, CNRS, UMR 5089, 205 route de Narbonne, 31077 Toulouse cedex 04, France.
Flavie
F
Kersanté
Catherine
C
Mollereau
Jean-Marie
JM
Zajac
Michel
M
Roumy
D020864:Calcium Channels, N-Type / Q000187:drug effects / Q000502:physiology; D002217:Carbachol / Q000494:pharmacology; D045744:Cell Line, Tumor; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)- / Q000494:pharmacology; D006801:Humans; D009292:Narcotic Antagonists; D009447:Neuroblastoma; D009479:Neuropeptides / Q000494:pharmacology; D009842:Oligopeptides / Q000494:pharmacology; D037342:Pertussis Toxin / Q000494:pharmacology; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000502:physiology; D018013:Receptors, Neuropeptide / Q000502:physiology*; D017450:Receptors, Opioid, mu / Q000819:agonists; D015398:Signal Transduction / Q000187:drug effects; D014162:Transfection
D020864:Calcium Channels, N-Type; D009292:Narcotic Antagonists; D009479:Neuropeptides; D009842:Oligopeptides; D011976:Receptors, Muscarinic; D018013:Receptors, Neuropeptide; D017450:Receptors, Opioid, mu; C083929:neuropeptide FF receptor; C503959:neuropeptide VF; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; C060208:deltorphin I, Ala(2)-; D002217:Carbachol; D037342:Pertussis Toxin