Various methods, including functional magnetic resonance imaging (fMRI), ha
ve recently been developed to allow investigators to study functional activ
ity in the living brain. Such techniques are now being used to investigate
regionally specific brain activity associated with the administration of CN
S-active drugs. fMRI in particular is increasingly recognized as being a re
latively non-invasive way to perform pharmacological investigations in expe
rimental animals, healthy human volunteers, and individuals with CNS diseas
e. This use of fMRI, dubbed 'pharmacological MRI' or 'phMRI', holds the pro
mise of providing relatively straightforward pharmacodynamic assays and can
be used to establish brain-penetrability parameters, or dose-ranging infor
mation for novel therapeutic compounds.