ChemInform Abstract: Excitatory Amino-Acid Receptor Agonists. Synthesis and Pharmacology of Analogues of 2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid.
β Scribed by F. A. SLOEK; B. EBERT; Y. LANG; P. KROGSGAARD-LARSEN; S. M. LENZ; U. MADSEN
- Publisher
- John Wiley and Sons
- Year
- 2010
- Weight
- 32 KB
- Volume
- 28
- Category
- Article
- ISSN
- 0931-7597
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We have previously shown that whereas (RS)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid (APPA) shows the characteristics of a partial agonist at (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptors, (S)-APPA is a full AMPA receptor agonist and (R)-APPA a weak
RS)-2-Amino-2-(3-hydroxy-5-methylisoxazol-4-yl)acetic acid (AMAA) is a potent and selective agonist at the NMDA subgroup of excitatory amino acid receptors. To probe its interaction with these receptors we have developed a synthesis of [3H]AMAA. Bromination of a protected form of AMAA with NBS follo
We have previously shown that (RS)-2-amino-2-(5-tert-butyl-3-hydroxyisoxazol-4-yl)acetic acid (ATAA) is an antagonist at N-methyl-D-aspartic acid (NMDA) and (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptors. We have now resolved ATAA via diastereomeric salt formation us