title: PET and plasma pharmacokinetic studies after bolus intravenous administration of [11C]melatonin in humans.
abstract: A human PET study was performed with carbon-11 labelled melatonin in a healthy volunteer. Plasma pharmacokinetics of melatonin and 6-sulfatoxymelatonin were simultaneously determined using radioimmunoassay. Analysis of tracer kinetics showed maximum activity in the brain 8.5 min following injection, which was different from the curve observed for the plasma radioactivity (maximum at 3.5 min). The results confirmed that melatonin readily crosses the blood-brain barrier and that 6-sulfatoxymelatonin is the main plasma metabolite. The distribution of tracer as a function of time in this study failed to reveal any specific binding.
authors.affiliation: MRC Cycloton Unit, Hammersmith Hospital, London, England.
authors.forename: D
authors.initials: D
authors.lastname: Le Bars
authors.forename: P
authors.initials: P
authors.lastname: Thivolle
authors.forename: P A
authors.initials: PA
authors.lastname: Vitte
authors.forename: C
authors.initials: C
authors.lastname: Bojkowski
authors.forename: G
authors.initials: G
authors.lastname: Chazot
authors.forename: J
authors.initials: J
authors.lastname: Arendt
authors.forename: R S
authors.initials: RS
authors.lastname: Frackowiak
authors.forename: B
authors.initials: B
authors.lastname: Claustrat
mesh_terms: D000328:Adult; D001921:Brain / Q000000981:diagnostic imaging; D001923:Brain Chemistry; D002247:Carbon Isotopes; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D008550:Melatonin / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D011863:Radioimmunoassay; D014055:Tomography, Emission-Computed
chemical_list: D002247:Carbon Isotopes; C054513:6-sulfatoxymelatonin; D008550:Melatonin