Nehls D G, Kurumaji A, Park C K, McCulloch J
Wellcome Surgical Institute, University of Glasgow, U.K.
Neurosci Lett. 1988 Aug 31;91(2):204-10. doi: 10.1016/0304-3940(88)90769-0.
The effects on cerebral glucose utilisation of 3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid (CPP, a competitive N-methyl-D-aspartate (NMDA) receptor antagonist), and (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (MK-801, a non-competitive NMDA receptor antagonist) have been examined in conscious rats. Cerebral glucose utilisation was assessed quantitatively with 14C-2-deoxyglucose autoradiography. MK-801 (0.05-5 mg/kg, i.v.) markedly increased glucose use in a number of limbic brain areas such as the mamillary body, anterior thalamic nucleus, posterior cingulate cortex and hippocampus. CPP (3-30 mg/kg, i.v.), in contrast, effected minimal alterations in glucose use in the limbic system. The functional consequences in vivo, as reflected in local cerebral glucose use, of competitive blockade of the NMDA receptor differ markedly from blockade with non-competitive antagonists.
在清醒大鼠中研究了3-(2-羧基哌嗪-4-基)丙基-1-膦酸（CPP，一种竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂）和(+)-5-甲基-10,11-二氢-5H-二苯并[a,d]环庚烯-5,10-亚胺（MK-801，一种非竞争性NMDA受体拮抗剂）对脑葡萄糖利用的影响。用14C-2-脱氧葡萄糖放射自显影法定量评估脑葡萄糖利用情况。MK-801（0.05-5毫克/千克，静脉注射）显著增加了多个边缘脑区的葡萄糖利用，如乳头体、丘脑前核、后扣带回皮质和海马体。相比之下，CPP（3-30毫克/千克，静脉注射）对边缘系统的葡萄糖利用影响极小。NMDA受体竞争性阻断在体内的功能后果，如局部脑葡萄糖利用所反映的，与非竞争性拮抗剂阻断有显著差异。
