Synthesis of tritiated (RS)-2-amino-2-(3-hydroxy-5-methylisoxazol-4-yl)acetic acid (AMAA), a potent and selective NMDA agonist

✍ Scribed by Tommy N. Johansen; Venkataraman Balasubramanian; Ulf Madsen; John W. Ferkany; Povl Krogsgaard-Larsen

• Publisher: John Wiley and Sons
• Year: 1996
• Tongue: French
• Weight: 329 KB
• Volume: 38
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/(sici)1099-1344(199610)38:10<915::aid-jlcr903>3.0.co;2-b

✦ Synopsis

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 followed by hydrogenolysis with tritium gas in the presence of P d C and subsequent deprotection gave [ 3H]AMAA with a specific activity of 25 Cilmmol. Attempts to develop a receptor binding assay based on rat brain homogenates and using [ 3H]AMAA as radioligand for the NMDA receptors have not been successful.