Neugebauer V, Kornhuber J, Lücke T, Schaible H G
Physiologisches Institut, Universität Würzburg, Germany.
Neuroreport. 1993 Sep 10;4(11):1259-62. doi: 10.1097/00001756-199309000-00012.
In anaesthetized rats antinociceptive effects of the clinically available drug memantine, an NMDA (N-methyl-D-aspartate) antagonist in vitro, were evaluated using extracellular recordings from spinal neurones with knee joint input. Memantine (1-12 mg kg-1) was applied intravenously before (control animals) or after induction of an acute knee joint inflammation which rendered spinal neurones hyperexcitable. Memantine (2 mg kg-1, i.v.) selectively reduced the responses to ionophoretic application of NMDA close to the neurone but not those to AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid). In control animals memantine reduced the neurones' responses to noxious but not to innocuous pressure on to the knee. In rats with acute arthritis memantine reduced the responses to noxious and innocuous pressure. Thus memantine may be useful for the treatment of pain states.
在麻醉大鼠中，使用来自具有膝关节输入的脊髓神经元的细胞外记录，评估了临床上可用的药物美金刚（一种体外NMDA（N-甲基-D-天冬氨酸）拮抗剂）的抗伤害感受作用。在诱导急性膝关节炎症使脊髓神经元兴奋性过高之前（对照动物）或之后，静脉注射美金刚（1-12毫克/千克）。美金刚（2毫克/千克，静脉注射）选择性地降低了靠近神经元处离子电渗法施加NMDA时的反应，但不降低对AMPA（α-氨基-3-羟基-5-甲基-4-异恶唑丙酸）的反应。在对照动物中，美金刚降低了神经元对膝关节有害但非无害压力的反应。在患有急性关节炎的大鼠中，美金刚降低了对有害和无害压力的反应。因此，美金刚可能对疼痛状态的治疗有用。
