Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.
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.
Colabufo
Nicola Antonio
NA
Dipartimento Farmacochimico, Università degli Studi di Bari, via Orabona 4, 70125 Bari, Italy. colabufo@farmchim.uniba.it
Abate
Carmen
C
Contino
Marialessandra
M
Inglese
Carmela
C
Ferorelli
Savina
S
Berardi
Francesco
F
Perrone
Roberto
R
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*
C513937:PB28 compound; D010879:Piperazines; D012333:RNA, Messenger; D017480:Receptors, sigma; C106107:sigma-2 receptor; D014316:Tritium