A METHOD TO ESTIMATE IN-VIVO D-2 RECEPTOR OCCUPANCY BY ANTIPSYCHOTIC-DRUGS

A computational method is presented to estimate in vivo receptor occup ancies of frequently used antipsychotic medications, which may provide a way to determine their central nervous system (CNS) effects in huma ns. The method can be used to estimate occupancies of several receptor types based on the daily dose of antipsychotic medication, Estimates of D-2 receptor occupancy by haloperidol based on this equation were c ompared with those yielded by positron emission tomography (PET) measu res in humans for the same compounds and dosages: the results of this comparison validated the approach.