In vivo evidence for carrier-mediated brain uptake of a new 2-amino-2-oxazoline (COR3224) via the purine transport system in rat.
We studied the brain uptake of a new 2-amino-2-oxazolamines derivative (COR3224) in the rat by means of the rapid intracarotid injection technique described by Oldendorf. The brain uptake index (BUI) of labelled COR3224 decreased progressively from 10% to 5% when concentrations of unlabelled compound were increased. The effect of various compounds indicated that COR3224 is transported into the brain by the purine carrier. The affinity of COR3224 for this carrier (Km = 5.68 microM) was higher than that of adenine.
Laboratoire Pharmacologie et de Pharmacocinétique, Faculté de Pharmacie, Chatenay-Malabry, France.
M I
MI
Damaj
S
S
Urien
J H
JH
Trouvin
E
E
Chanut
B
B
Lambrey
C
C
Jacquot
D000818:Animals; D000928:Antidepressive Agents / Q000378:metabolism*; D001667:Binding, Competitive; D001812:Blood-Brain Barrier; D001921:Brain / Q000378:metabolism*; D002250:Carbon Radioisotopes; D007700:Kinetics; D008297:Male; D008433:Mathematics; D008962:Models, Theoretical; D010080:Oxazoles / Q000378:metabolism*; D011687:Purines / Q000378:metabolism*; D011865:Radioisotope Dilution Technique; D051381:Rats; D011919:Rats, Inbred Strains; D014316:Tritium
D000928:Antidepressive Agents; D002250:Carbon Radioisotopes; D010080:Oxazoles; D011687:Purines; D014316:Tritium; C056984:COR 32-24