title: Methodological aspects for in vitro characterization of receptor binding using 11C-labeled receptor ligands: a detailed study with the benzodiazepine receptor antagonist [11C]Ro 15-1788.
abstract: As a complement to in vivo studies with positron emission tomography (PET), it is desirable to perform in vitro characterization of newly developed 11C tracers. In this report we describe the technique for determination of receptor-ligand kinetics utilizing ligands labeled with the short-lived radionuclide 11C. The limitations and advantages are discussed. The benzodiazepine antagonist [11C]Ro 15-1788 was used as a model substance, and the use of storage phosphor plates for quantification of radioactivity was validated. Storage phosphor plates showed an excellent linear range (approximately 10[3]) and acceptable resolution (approximately 0.5 mm). Receptor-ligand kinetics, including depletion, association and dissociation, saturation and displacement were evaluated with good results through the use of short-lived radiotracers and storage phosphor plates.
authors.affiliation: Subfemtomole Biorecognition Project, Uppsala University PET Centre, Sweden.
authors.forename: W
authors.initials: W
authors.lastname: Sihver
authors.forename: S
authors.initials: S
authors.lastname: Sihver
authors.forename: M
authors.initials: M
authors.lastname: Bergström
authors.forename: T
authors.initials: T
authors.lastname: Murata
authors.forename: K
authors.initials: K
authors.lastname: Matsumura
authors.forename: H
authors.initials: H
authors.lastname: Onoe
authors.forename: Y
authors.initials: Y
authors.lastname: Andersson
authors.forename: P
authors.initials: P
authors.lastname: Bjurling
authors.forename: K J
authors.initials: KJ
authors.lastname: Fasth
authors.forename: G
authors.initials: G
authors.lastname: Westerberg
authors.forename: M
authors.initials: M
authors.lastname: Ogren
authors.forename: G
authors.initials: G
authors.lastname: Jacobsson
authors.forename: H
authors.initials: H
authors.lastname: Lundqvist
authors.forename: L
authors.initials: L
authors.lastname: Oreland
authors.forename: Y
authors.initials: Y
authors.lastname: Watanabe
authors.forename: B
authors.initials: B
authors.lastname: Långström
mesh_terms: D000818:Animals; D002250:Carbon Radioisotopes; D005442:Flumazenil / Q000378:metabolism* / Q000494:pharmacology; D018757:GABA Modulators / Q000378:metabolism* / Q000494:pharmacology; D058787:GABA-A Receptor Antagonists; D008024:Ligands; D008297:Male; D011869:Radioligand Assay / Q000379:methods; D019275:Radiopharmaceuticals / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011963:Receptors, GABA-A / Q000032:analysis*; D012680:Sensitivity and Specificity; D014055:Tomography, Emission-Computed
chemical_list: D002250:Carbon Radioisotopes; D018757:GABA Modulators; D058787:GABA-A Receptor Antagonists; D008024:Ligands; D019275:Radiopharmaceuticals; D011963:Receptors, GABA-A; D005442:Flumazenil