In vivo distribution of [11C]-busulfan in cynomolgus monkey and in the brain of a human patient.
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.
Hassan
M
M
Karolinska Pharmacy, Stockholm, Sweden.
Oberg
G
G
Ericson
K
K
Ehrsson
H
H
Eriksson
L
L
Ingvar
M
M
Stone-Elander
S
S
Thorell
J O
JO
Smedmyr
B
B
Warne
N
N
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
D002250:Carbon Radioisotopes; D002066:Busulfan