title: Orphanin FQ/nociceptin binds to functionally coupled ORL1 receptors on human immune cell lines and alters peripheral blood mononuclear cell proliferation.
abstract: Orphanin FQ/nociceptin (OFQ/N) has been shown to modulate nociception, responses to stress and anxiety. We investigated OFQ/N function in human immune cells. We find that monocytic U937, T lymphocytic CEM, and MOLT-4 cell lines express OFQ/N binding sites at levels comparable to that of human SH-SY5Y neuroblastoma cells. We show that OFQ/N receptors are functionally coupled to G proteins in these cells. Finally OFQ/N decreases proliferation of phytohemagglutinin-stimulated peripheral blood mononuclear cells in vitro at doses ranging from 10(-13) to 10(-8) M. Thus, our data suggest that OFQ/N and OFQ/N receptor may act as an immunomodulatory system.
authors.affiliation: CNRS UPR9050, ESBS and Faculty of Pharmacy, Illkirch, France.
authors.forename: J
authors.initials: J
authors.lastname: Peluso
authors.forename: C
authors.initials: C
authors.lastname: Gavériaux-Ruff
authors.forename: H W
authors.initials: HW
authors.lastname: Matthes
authors.forename: D
authors.initials: D
authors.lastname: Filliol
authors.forename: B L
authors.initials: BL
authors.lastname: Kieffer
mesh_terms: D000328:Adult; D000818:Animals; D001665:Binding Sites / Q000187:drug effects / Q000502:physiology; D016466:CHO Cells / Q000187:drug effects / Q000378:metabolism; D002455:Cell Division / Q000187:drug effects / Q000502:physiology; D002460:Cell Line / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D006224:Cricetinae; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000493:pharmacokinetics; D006801:Humans; D007107:Immune System / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D007963:Leukocytes, Mononuclear / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D009447:Neuroblastoma; D018847:Opioid Peptides / Q000276:immunology / Q000378:metabolism* / Q000494:pharmacology; D010835:Phytohemagglutinins / Q000494:pharmacology; D011869:Radioligand Assay; D011957:Receptors, Opioid / Q000187:drug effects / Q000276:immunology / Q000378:metabolism*; D013462:Sulfur Radioisotopes / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000378:metabolism; D000094942:Nociceptin Receptor; D000097629:Nociceptin
chemical_list: D016244:Guanosine 5'-O-(3-Thiotriphosphate); D018847:Opioid Peptides; D010835:Phytohemagglutinins; D011957:Receptors, Opioid; D013462:Sulfur Radioisotopes; D000094942:Nociceptin Receptor; D000097629:Nociceptin