Sivvas E, Voukelatou G, Papaioannou D, Aletras A J, Kouvelas E D
Department of Physiology, Medical School, University of Patras, Greece.
J Neurochem. 1994 Oct;63(4):1544-50. doi: 10.1046/j.1471-4159.1994.63041544.x.
The synthesis of (2S,3S,4S)-4-[1-(4-azidobenzamidomethyl)ethenyl]-2-carboxy-3- pyrrolidineacetic acid (ABCPA) is described. This novel kainic acid analogue, bearing a photolabile functionality on the isopropenyl side chain, was proven to be a good inhibitor of [3H]CNQX and [3H]kainic acid binding on chick cerebellar membranes. [3H]ABCPA was photoaffinity cross-linked on the membrane fraction of chick cerebellum. Electrophoretic analysis with sodium dodecyl sulfate-polyacrylamide gel electrophoresis revealed two major radioactive bands with apparent molecular masses of 45 and 33.5 kDa. [3H]ABCPA incorporation in both bands was completely blocked by 2 mM CNQX. When photoaffinity labeling was performed in the presence of 2 mM kainic acid, incorporation of [3H]ABCPA was blocked by approximately 70% in the 45-kDa band and by 18% in the 33.5-kDa band. Incorporation of radioactivity in both bands was blocked by approximately 30% with 10 mM glutamate.
描述了(2S,3S,4S)-4-[1-(4-叠氮基苯甲酰胺基甲基)乙烯基]-2-羧基-3-吡咯烷乙酸(ABCPA)的合成。这种新型红藻氨酸类似物在异丙烯基侧链上带有光不稳定官能团，已被证明是[3H]CNQX和[3H]红藻氨酸与鸡小脑膜结合的良好抑制剂。[3H]ABCPA在鸡小脑的膜部分进行了光亲和交联。用十二烷基硫酸钠-聚丙烯酰胺凝胶电泳进行的电泳分析显示出两条主要的放射性条带，其表观分子量分别为45 kDa和33.5 kDa。2 mM CNQX完全阻断了[3H]ABCPA在两条条带中的掺入。当在2 mM红藻氨酸存在下进行光亲和标记时，[3H]ABCPA在45 kDa条带中的掺入被阻断约70%，在33.5 kDa条带中的掺入被阻断18%。10 mM谷氨酸使两条条带中的放射性掺入均被阻断约30%。
