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Blood-Brain Barrier Transport of L-iyrosine Conjugates: a Model Study for the Brain Targeting using Large Neutral Amino Acid Transport System
Ist Teil von
Journal of drug targeting, 2000, Vol.8 (6), p.395-401
Ort / Verlag
Informa UK Ltd
Erscheinungsjahr
2000
Link zum Volltext
Quelle
Alma/SFX Local Collection
Beschreibungen/Notizen
AbstractWe examined the relation ship between the charge of the amino or carboxylic function of a substrate and the substrate recognition by the large neutral amino acid (LNAA) transport carrier, using the in situ brain perfusion technique. Glucose-coupled L-tyrosine (GcpY), which has a free carboxylic function, and 2-(L-tyrosylamide)-2-deoxy-D-glucose (Y-2DG), which has a free amino function were synthesized. The inhibitory effect of GcpY on [3H]L-tyrosine uptake was larger than that of N-methly-L-phenylalanine or N-acetyl-L-phenylalanine, whereas Y-2DG did not affect it. These results indicate that a free amino group is not required for recognition, provided that the modified amino group is able to take a positive charge. Steric factors appeared to be relatively unimportant.