Danysz W, Fadda E, Wroblewski J T, Costa E
Fidia-Georgetown Institute for the Neurosciences, Georgetown University School of Medicine, Washington, D.C. 20007.
Life Sci. 1990;46(3):155-64. doi: 10.1016/0024-3205(90)90100-6.
In the central nervous system, glycine binds to two recognition sites; one of them (G2), associated with the glutamate receptor, is insensitive to strychnine. Strychnine-insensitive sites were predominant in the forebrain areas and bound D-serine and D-alanine better than the respective L stereoisomers. [3H]D-serine was a more selective radioligand than [3H]glycine for the strychnine-insensitive sites. In the forebrain, the binding of both ligands was inhibited by the putative G2 receptor antagonists, 7-chlorokynurenate and 3-amino-1-hydroxy-2-pyrrolidone, while in pons and in spinal cord only the latter drug was effective. This may indicate the heterogeneity of strychnine-insensitive glycine recognition sites.
在中枢神经系统中,甘氨酸与两个识别位点结合;其中一个(G2)与谷氨酸受体相关,对士的宁不敏感。士的宁不敏感位点在前脑区域占主导地位,与D-丝氨酸和D-丙氨酸的结合比各自的L型立体异构体更好。对于士的宁不敏感位点,[3H]D-丝氨酸是比[3H]甘氨酸更具选择性的放射性配体。在前脑中,两种配体的结合均被推定的G2受体拮抗剂7-氯犬尿氨酸和3-氨基-1-羟基-2-吡咯烷酮抑制,而在脑桥和脊髓中只有后一种药物有效。这可能表明士的宁不敏感甘氨酸识别位点的异质性。