title: [3H]PK11195 binding sites in human neutrophils: effect of fMLP stimulation and modulation in rheumatic diseases.
abstract: OBJECTIVE
  The objectives of this study were to evaluate the [3H]PK11195 binding parameters in a model of acute inflammation, the N-formylmethionine-leucine-phenylalanine (fMLP)-stimulated neutrophil cell membranes, and to analyze if alterations of peripheral-type benzodiazepine receptor (PBR) characteristics occurred in neutrophil cell membranes of patients affected by osteoarthritis (OA), rheumatoid arthritis (RA), and psoriasic arthritis (PA).
  
  
  METHODS
  Neutrophils were obtained from 15 patients with OA, 15 patients with RA, and 15 patients with PA. fMLP stimulation was performed to aliquots of neutrophils from six healthy individuals. Evaluation of kinetic parameters of PBR was performed using [3H]PK11195, as specific radioligand compared with 15 healthy volunteers.
  
  
  RESULTS
  The results showed a significant decrease of Kd and Bmax in fMLP-stimulated neutrophil membranes. Moreover, an increase of PBR binding sites and affinity value was observed in neutrophils membranes from PA patients.
  
  
  CONCLUSIONS
  Our data suggested a fMLP modulation on [3H]PK11195 binding in human neutrophils. Moreover, our results showed an up-regulation of PBR in neutrophils of PA patients.
authors.affiliation: Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Giusti
authors.forename: Laura
authors.initials: L
authors.lastname: Betti
authors.forename: Gino
authors.initials: G
authors.lastname: Giannaccini
authors.forename: Giovanni
authors.initials: G
authors.lastname: Mascia
authors.forename: Laura
authors.initials: L
authors.lastname: Bazzichi
authors.forename: Antonio
authors.initials: A
authors.lastname: Lucacchini
mesh_terms: D000368:Aged; D015535:Arthritis, Psoriatic / Q000097:blood; D001172:Arthritis, Rheumatoid / Q000097:blood*; D001665:Binding Sites; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D005260:Female; D006801:Humans; D007546:Isoquinolines / Q000378:metabolism* / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000378:metabolism / Q000494:pharmacology*; D009504:Neutrophils / Q000378:metabolism*; D010003:Osteoarthritis / Q000097:blood; D011963:Receptors, GABA-A / Q000378:metabolism
chemical_list: D007546:Isoquinolines; D011963:Receptors, GABA-A; D009240:N-Formylmethionine Leucyl-Phenylalanine; C037850:PK 11195