Blood-Brain Barrier Transport of L-iyrosine Conjugates: a Model Study for the Brain Targeting using Large Neutral Amino Acid Transport System
| Autor: | Shoji Awazu, Toshimasa Ohnishi, Sohei Higashi, Tetsu Maruyama |
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| Rok vydání: | 2000 |
| Předmět: |
Male
Steric effects chemistry.chemical_classification Amino Acid Transport Systems Stereochemistry Pharmaceutical Science Substrate (chemistry) Biology Blood–brain barrier Rats Amino acid Drug Delivery Systems Glucose medicine.anatomical_structure chemistry Blood-Brain Barrier Neutral amino acid transport medicine Animals Tyrosine Rats Wistar Carrier Proteins Function (biology) Conjugate |
| Zdroj: | Journal of Drug Targeting. 8:395-401 |
| ISSN: | 1029-2330 1061-186X |
| DOI: | 10.3109/10611860008997915 |
| Popis: | We 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 [3 H]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. |
| Databáze: | OpenAIRE |
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