Synthesis of deuterium and tritium labelled (RS)??2??amino??3??(5??tert??butyl??3??hydroxy??4??isoxazolyl)??propionic acid (ATPA), a selective kainic acid receptor agonist

…, P Krogsgaard??Larsen

Index: Johansen, Tommy N.; Hawes, Calvin R.; Ellis, Gareth J.; Ebert, Bjarke; Stensbol, Tine B.; Da Graca Thrige, Dorthe; Krogsgaard-Larsen, Povl Journal of Labelled Compounds and Radiopharmaceuticals, 1999 , vol. 42, # 10 p. 937 - 947

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Citation Number: 2

Abstract

Abstract (RS)-2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl) propionic acid (ATPA) is an excitatory amino acid receptor agonist showing selectivity for the kainic acid receptor subtype GluR5. As part of the pharmacological characterization of GluR5 receptors, we now report the synthesis of [3 H] ATPA based on a four-step synthesis using 5-tert-butyl-3- methoxy-4-isoxazolylcarbaldehyde as the starting material. Using this synthetic procedure ...