Emission tomography techniques and, in particular, positron emission tomogr
aphy (PET) enable the in vivo study of several physiological and neurochemi
cal variables in human subjects using methods originally developed for quan
titative autoradiography. In particular, PET allows one to evaluate in huma
n subjects: (a) the effect of specific neurochemical challenges on regional
brain function at rest or under activation; (b) the activity of neurotrans
mitters and the regional expression of specific molecular targets during pa
thology including their modulation by drug treatment;, (c) the kinetics of
drug disposition and activity directly in the target organ. This is of prim
ary interest in the field of biological psychiatry and in psychoactive drug
s development, where it is particularly difficult to reproduce human diseas
es using animal models in view of the peculiarity of this field and the lar
ge heterogeneity of each psychiatric illness also inside the same clinical
definition. The aim of this paper is to review the principal strategies and
the main results of the use of PET in psychopharmacology. (C) 2001 Academi
c Press.