Heckendorn R, Allgeier H, Baud J, Gunzenhauser W, Angst C
Research Department, Ciba-Geigy Ltd., Basel, Switzerland.
J Med Chem. 1993 Nov 12;36(23):3721-6. doi: 10.1021/jm00075a029.
Four omega-benzoylated (E)-2,10-diamino-4-(phosphonomethyl)dec-3-enoic acids have been synthesized and tested in vitro for binding affinity to the glutamate recognition site of the NMDA (N-methyl-D-aspartate) receptor. The omega-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.
已合成了四种ω-苯甲酰化的（E）-2,10-二氨基-4-（膦酰甲基）癸-3-烯酸，并在体外测试了它们与NMDA（N-甲基-D-天冬氨酸）受体谷氨酸识别位点的结合亲和力。ω-4-叠氮基水杨酰胺衍生物24经碘化得到光亲和配体25（CGP 55802 A），在体外[3H]CGP 39653结合试验中，其IC50值为34 nM。该化合物及其放射性125I形式是对谷氨酸识别位点具有高亲和力的首个NMDA受体光亲和配体。
