[(11)]Cocaine: PET studies of cocaine pharmacokinetics, dopamine transporter availability and dopamine transporter occupancy

Cocaine was initially labeled with carbon-11 in order to track the distribu tion and pharmacokinetics of this powerful stimulant and drug of abuse in t he human brain and body. It was soon discovered that [C-11]cocaine was not only useful for measuring cocaine pharmacokinetics and its relationship to behavior but that it is also a sensitive radiotracer for dopamine transport er (DAT) availability. Measures of DAT availability were facilitated by the development of a graphical analysis method (Logan Plot) for reversible sys tems which streamlined kinetic analysis. This expanded the applications of [C-11]cocaine to studies of DAT availability in the human brain and allowed the first comparative measures of the degree of DAT occupancy by cocaine a nd another stimulant drug methylphenidate. This article will summarize prec linical and clinical research with [C-11]cocaine. (C) 2001 Elsevier Science Inc. All rights reserved.