ABSTRACT
This chapter reviews the distribution of benzodiazepine (BZ) binding sites in post-mortem human brain studied using materials obtained post-mortem. The synthesis of chlordiazepoxide by Sternbach's group at Hoffmann-La Roche Laboratories in the late 1950s was the beginning of the career of a chemical class, the BZs, whose prototype diazepam (Valium) has reached an enormous popularity. BZs were introduced in clinical practice in the 1960s and, for a time, were one of the most widely prescribed psycho-active drugs. BZ receptors were found in nearly every region of the human brain examined. In general, the localization of BZ receptor sites in the human brain is highly comparable with that observed in earlier studies in rats using the same ligand, although the human brain presents lower receptor densities and some regional differences are observed.
