Jansen Michaela, Dannhardt Gerd
Department of Medicinal and Pharmaceutical Chemistry, Institute of Pharmacy, Johannes Gutenberg-University of Mainz, Staudinger Weg 5, 55099, Mainz, Germany.
Eur J Med Chem. 2003 Jul-Aug;38(7-8):661-70. doi: 10.1016/s0223-5234(03)00113-2.
For decades neuroreceptor research has focused on the development of NMDA glycine-site antagonists, after Johnson and Ascher found out in 1987 about the co-agonistic character of this achiral amino acid at the NMDA receptor. Contrary to the inhibitory glycine receptor (glycine(A)) the glycine binding site on the NMDA receptor (glycine(B)) is strychnine-insensitive. A great diversity of diseases showing a disturbed glutamate neurotransmission have been linked to the NMDA receptor. Glycine site antagonists have been investigated for acute diseases like stroke and head trauma as well as chronic ones like dementia and chronic pain.
自1987年约翰逊和阿舍尔发现这种非手性氨基酸在NMDA受体上具有协同激动特性后，数十年来神经受体研究一直聚焦于NMDA甘氨酸位点拮抗剂的开发。与抑制性甘氨酸受体（甘氨酸(A)）相反，NMDA受体上的甘氨酸结合位点（甘氨酸(B)）对士的宁不敏感。多种显示谷氨酸神经传递紊乱的疾病都与NMDA受体有关。甘氨酸位点拮抗剂已针对中风和头部创伤等急性疾病以及痴呆和慢性疼痛等慢性疾病进行了研究。
