Permeability of the blood-brain barrier for atenolol studied by positron emission tomography.
The permeability of the blood-brain barrier for atenolol, a hydrophilic beta-adrenergic blocking agent, has been assessed in dogs, by studying the distribution of [11C]atenolol in brain tissue with positron emission tomography. The passage of atenolol into the brain was very limited, but a measurable small net influx into the brain tissues did occur. Osmotic opening of the blood-brain barrier resulted in a marked increase of the atenolol concentrations in brain tissue. The approach described, with sequential non-invasive measurements in brain tissue, is applicable to pharmacokinetic studies of atenolol in man.
Agon
P
P
Heymans Institute of Pharmacology, University of Gent, Belgium.
Goethals
P
P
Van Haver
D
D
Kaufman
J M
JM
D000818:Animals; D001262:Atenolol / Q000494:pharmacology*; D001812:Blood-Brain Barrier / Q000187:drug effects*; D002463:Cell Membrane Permeability / Q000187:drug effects; D004285:Dogs; D007275:Injections, Intravenous; D008353:Mannitol / Q000494:pharmacology; D014055:Tomography, Emission-Computed
D008353:Mannitol; D001262:Atenolol