152564-58-4Relevant articles and documents
Synthesis and Binding Properties of 2-Amino-5-phosphono-3-pentenoic Acid Photoaffinity Ligands as Probes for the Glutamate Recognition Site of the NMDA Receptor
Heckendorn, Roland,Allgeier, Hans,Baud, Jaqueline,Gunzenhauser, Wilfried,Angst, Christof
, p. 3721 - 3726 (2007/10/02)
Four ω-benzoylated (E)-2,10-diamino-4-(phosphonomethyl)dec-3-enoic acids have been synthesized and tested in vitro for binding to the glutamate recognition site of the NMDA (N-methyl-D-aspartate) receptor.The ω-4-azidosalicylamide derivative 24 was iodinated to give the photoaffinity ligand 25 (CGP 55802 A) which showed an IC50 value of 34 nM in the in vitro 3H>CGP 39653 binding assay.This compound and its radioactive 125I-form are the first photoaffinity ligands for the NMDA receptor with high affinity to the glutamate recognition site.