Kornhuber J, Weller M
Psychiatrische Klinik, Universität Würzburg.
Nervenarzt. 1996 Jan;67(1):77-82.
Glutamate receptor antagonists with selective action at the N-methyl-D-aspartate (NMDA) receptor are promising agents for the neuroprotective and symptomatic pharmacotherapy of various neuropsychiatric disorders. Although NMDA receptor antagonists of the phencyclidine (PCP) type are precluded from clinical use because of their psychotomimetic properties, amantadine and memantine have been administered to human patients with idiopathic Parkinson's disease and spasticity for many years without serious adverse effects. The mechanisms underlying these differences in psychotogenicity of different NMDA receptor antagonist are currently being discussed. Different affinity to the PCP binding site of the NMDA receptor, region-specific pharmacology, as well as different binding profiles to neurotransmitter receptors other than the NMDA type glutamate receptor, most likely play a role in determining whether an NMDA receptor antagonist drug will be tolerated clinically or not.
对N-甲基-D-天冬氨酸（NMDA）受体具有选择性作用的谷氨酸受体拮抗剂，有望用于多种神经精神疾病的神经保护和对症药物治疗。尽管苯环己哌啶（PCP）类NMDA受体拮抗剂因其拟精神病特性而无法用于临床，但金刚烷胺和美金刚已用于特发性帕金森病和痉挛患者多年，且无严重不良反应。目前正在探讨不同NMDA受体拮抗剂致精神障碍性差异的潜在机制。对NMDA受体PCP结合位点的不同亲和力、区域特异性药理学，以及对NMDA型谷氨酸受体以外的神经递质受体的不同结合模式，很可能在决定一种NMDA受体拮抗剂药物是否能被临床耐受方面发挥作用。
