Considerable progress has been achieved over the past 15 years in unco
vering the biological basis of major psychiatric disorders. Since psyc
hopharmacological treatment is thought to act on the underlying biolog
ical basis of the disease, brain imaging techniques enable us to under
stand the mechanism of action of such compounds. One important tool us
ed to determine patterns of brain dysfunction and how psychopharmacolo
gical agents such as antipsychotic compounds work is single-photon emi
ssion computerised tomography (SPECT). This technique allows determina
tion of striatal D-2 receptor occupancy rates, which are associated wi
th the extrapyramidal side effects (EPS) of antipsychotic drugs. Studi
es have confirmed that atypical antipsychotic agents have lower occupa
ncy rates than typical agents. No association has been found between D
-2 receptor occupancy rates in the striatum and antipsychotic efficacy
, and it therefore appears that striatal D-2 receptor occupancy rates
are not necessary for the antipsychotic effect of such agents in schiz
ophrenia. The availability of more refined radioligands will help us n
ot only to understand the action of antipsychotics but also the pathop
hysiology of schizophrenia.