Quantification of [Carbonyl- 11C]WAY-100635 binding: considerations on the cerebellum

• Published in: Nuclear medicine and biology Vol. 27; no. 5; pp. 483 - 486
• Main Authors: Oikonen, Vesa, Allonen, Topias, Någren, Kjell, Kajander, Jaana, Hietala, Jarmo
• Format: Journal Article Conference Proceeding
• Language: English
• Published: Amsterdam Elsevier Inc 01.07.2000; Elsevier
• Subjects: Adult; Biological and medical sciences; Cerebellum; Cerebellum - metabolism; Contrast media. Radiopharmaceuticals; Female; Humans; Investigative techniques, diagnostic techniques (general aspects); Male; Medical sciences; Models, Biological; Nervous system; PET; Pharmacology. Drug treatments; Piperazines - pharmacokinetics; Pyridines - pharmacokinetics; Radionuclide investigations; Receptors, Serotonin - analysis; Receptors, Serotonin, 5-HT1; Serotonin 5-HT 1A receptor; Serotonin Antagonists - pharmacokinetics; WAY-100635; Cerebellum; WAY-100635; Serotonin 5-HT 1A receptor; PET; Radionuclide study; Human; Radiolabelling; Volunteer; Central nervous system; Carbon; Kinetic model; Compartmental model; Binding capacity; Radiopharmaceuticals; Quantitative analysis; Brain (vertebrata); Positron; Emission tomography
• ISSN: 0969-8051; 1872-9614
• DOI: 10.1016/S0969-8051(00)00116-5

The specific binding of [carbonyl- 11C]WAY-100635 to 5-hydroxytryptamine 1A receptors was quantitated using different kinetic models. Ten healthy subjects were studied using a GE Advance PET scanner. We suggest that tissue heterogeneity explains part of the nonspecific binding seen in cerebellum, which leads to an underestimation of binding potential with reference tissue methods. The nonlinear three-compartmental model with metabolite-corrected plasma input provides accurate estimates of receptor binding because of the favorable kinetics of tracer in the brain and circulation.