“…In view of the obvious difficulty in obtaining tissue samples and measuring drug concentrations in the human brain, the present studies were undertaken to discover the extent of penetration of three /adrenoceptor antagonists, propranolol, pindolol and atenolol, into cerebrospinal fluid (CSF), a more accessible compartment in the central nervous system (CNS). Furthermore, if, as has been suggested, there is free movement of molecules between CSF and brain extracellular water (Matsen & West, 1972;Matakas, Stechele & Keller, 1978), then knowledge of drug concentration in CSF rather than in brain 0306-5251/81/100549-11 $01.00 tissue may be more important when considering drug action. It is believed by some that 8-adrenoceptors are situated on the surface of cells.…”