Js. Fowler et al., [(11)]Cocaine: PET studies of cocaine pharmacokinetics, dopamine transporter availability and dopamine transporter occupancy, NUCL MED BI, 28(5), 2001, pp. 561-572
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.