Monaghan D T, Beaton J A
Department of Pharmacology, University of Nebraska Medical Center, Omaha 68198-6260.
Eur J Pharmacol. 1991 Feb 26;194(1):123-5. doi: 10.1016/0014-2999(91)90134-c.
The potency of N-methyl-D-aspartate (NMDA), ibotenate, L-glutamate and quinolinate for inhibiting [3H]L-glutamate binding to rat brain NMDA receptors was determined by quantitative autoradiography. In contrast to NMDA, ibotenate and L-glutamate, quinolinate more potently displaced binding in forebrain regions than in the cerebellum. Of all drug-region combinations, only quinolinate affinity in the cerebellum was best described by a two-affinity component model (Ki = 24 and 275 microM; 45% high affinity). The cerebellum appears to contain a unique quinolinate-insensitive NMDA receptor subtype.
通过定量放射自显影法测定了N-甲基-D-天冬氨酸(NMDA)、鹅膏蕈氨酸、L-谷氨酸和喹啉酸对抑制[3H]L-谷氨酸与大鼠脑NMDA受体结合的效力。与NMDA、鹅膏蕈氨酸和L-谷氨酸不同,喹啉酸在前脑区域比在小脑中更有效地取代结合。在所有药物-区域组合中,只有喹啉酸在小脑中的亲和力能用双亲和力成分模型得到最佳描述(Ki = 24和275 microM;45%为高亲和力)。小脑似乎含有一种独特的对喹啉酸不敏感的NMDA受体亚型。