Dialyzable serum cofactor(s) required for the protein-mediated transport of DL-propranolol into rat brain.
To elucidate the characteristics of promotion factor(s) in rat serum required for the protein-mediated transport of drugs into the brain, we examined the brain uptake of DL-propranolol as a model drug using the in vivo brain uptake index (BUI) method in rats. The protein-mediated transport was not observed in rats injected with the buffer solution containing either various concentrations of purified rat alpha 1-acid glycoprotein (alpha 1-AGP) or rat albumin. When the filtrate from rat serum was used as an injection vehicle to which a physiological concentration of purified rat serum protein(s) was added, the protein-mediated transport of DL-propranolol was observed in the rat brain. Moreover, the ability of protein-mediated transport of DL-propranolol was reduced in rats injected with the dialyzed serum compared with the undialyzed serum. These results suggest that the dialyzable promotion factor in serum is required for the protein-mediated transport of DL-propranolol into the brain.
Lin
T H
TH
Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Sugiyama
Y
Y
Sawada
Y
Y
Iga
T
T
Hanano
M
M
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D003956:Dialysis; D007269:Injections, Intra-Arterial; D008297:Male; D009961:Orosomucoid / Q000494:pharmacology; D011433:Propranolol / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains; D012709:Serum Albumin / Q000494:pharmacology
D009961:Orosomucoid; D012709:Serum Albumin; D011433:Propranolol