title: In vivo distribution of [11C]-busulfan in cynomolgus monkey and in the brain of a human patient.
abstract: The in vivo distribution of the antileukemic agent busulfan labeled with the positron-emitting radionuclide carbon 11 was investigated in cynomolgus monkeys and in a human patient using positron emission tomography. After i.v. injection of the radiotracer, its regional uptake was monitored for about 1 h in the monkey's body and, in a separate experiment, in the monkey's brain. The concentration of radioactivity in the liver, which showed the highest levels of all the organs scanned, increased throughout the experiment and was 9-fold that in the brain at the end of the experiment. [11C]-Busulfan rapidly crossed the blood-brain barrier. The radioactivity peaked in both the cortex and the white matter showing a ratio of 1.25, at 3 min but declined quickly to yield a ratio of approximately 1 after 30 min. In the human brain, radioactivity in the cerebellum, cortex, and white matter reached a maximum within 5 min showing a cortex:white matter ratio of 1.6. The activity in the cortex declined to yield a ratio of 1 within 30 min. Of the delivered dose, 20% penetrated into the brain.
authors.affiliation: Karolinska Pharmacy, Stockholm, Sweden.
authors.forename: M
authors.initials: M
authors.lastname: Hassan
authors.forename: G
authors.initials: G
authors.lastname: Oberg
authors.forename: K
authors.initials: K
authors.lastname: Ericson
authors.forename: H
authors.initials: H
authors.lastname: Ehrsson
authors.forename: L
authors.initials: L
authors.lastname: Eriksson
authors.forename: M
authors.initials: M
authors.lastname: Ingvar
authors.forename: S
authors.initials: S
authors.lastname: Stone-Elander
authors.forename: J O
authors.initials: JO
authors.lastname: Thorell
authors.forename: B
authors.initials: B
authors.lastname: Smedmyr
authors.forename: N
authors.initials: N
authors.lastname: Warne
mesh_terms: D000328:Adult; D000818:Animals; D001921:Brain / Q000378:metabolism*; D002066:Busulfan / Q000493:pharmacokinetics*; D002250:Carbon Radioisotopes; D005260:Female; D006801:Humans; D008252:Macaca fascicularis; D008297:Male; D014055:Tomography, Emission-Computed
chemical_list: D002250:Carbon Radioisotopes; D002066:Busulfan