Imaging neuroreceptors to study drug action in living human brain

The principles of imaging of neuroreceptors had their origins in in vitro binding studies of the 1970s (Seeman et al., 1976; Creese et al., 1976). The potential for this methodology gained plausibility with the development of receptor autoradiography (Kuhar et al., 1978). These studies were carried out both in vitro and in vivo, using tritiated compounds in which the radioisotope had a negligible effect on the pharmacology of the unlabeled ligand.