title: Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.
abstract: A potent sigma-2 receptor ligand, known as PB28, was tritium radiolabelled and biologically evaluated. The results showed that [(3)H]PB28 and the corresponding unlabelled PB28 had superimposed pharmacodynamic properties. This radioligand appears as a potential candidate for receptor binding and in living cells assays.
authors.affiliation: Dipartimento Farmacochimico, Università degli Studi di Bari, via Orabona 4, 70125 Bari, Italy. colabufo@farmchim.uniba.it
authors.forename: Nicola Antonio
authors.initials: NA
authors.lastname: Colabufo
authors.forename: Carmen
authors.initials: C
authors.lastname: Abate
authors.forename: Marialessandra
authors.initials: M
authors.lastname: Contino
authors.forename: Carmela
authors.initials: C
authors.lastname: Inglese
authors.forename: Savina
authors.initials: S
authors.lastname: Ferorelli
authors.forename: Francesco
authors.initials: F
authors.lastname: Berardi
authors.forename: Roberto
authors.initials: R
authors.lastname: Perrone
mesh_terms: D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D008099:Liver / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D015394:Molecular Structure; D010879:Piperazines / Q000493:pharmacokinetics / Q000494:pharmacology*; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D017480:Receptors, sigma / Q000819:agonists*; D014316:Tritium / Q000493:pharmacokinetics*
chemical_list: C513937:PB28 compound; D010879:Piperazines; D012333:RNA, Messenger; D017480:Receptors, sigma; C106107:sigma-2 receptor; D014316:Tritium