In vivo distribution of [C]-busulfan in cynomolgus monkey and in the brain of a human patient.

Autor: Hassan, Moustapha, öberg, Gunnar, Ericson, Kaj, Ehrsson, Hans, Eriksson, Lars, Ingvar, Martin, Stone-Elander, Sharon, Thorell, Jan-Olov, Smedmyr, Bengt, Warne, Niklas, Widén, Lennart
Zdroj: Cancer Chemotherapy & Pharmacology; Mar1992, Vol. 30 Issue 2, p81-85, 5p
Abstrakt: 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. [C]-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. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index