Davies S N, Church J, Blake J, Lodge D, Lessor R A, Rice K C, Jacobson A E
Life Sci. 1986 Jun 30;38(26):2441-5. doi: 10.1016/0024-3205(86)90614-4.
The dissociative anaesthetics, phencyclidine and ketamine, block excitation of central neurones by N-methylaspartate. Using the technique of microelectrophoresis on rat spinal neurones in vivo Metaphit, a phencyclidine receptor acylating agent, was tested to see whether it would antagonise this effect of dissociative anaesthetics. The predominant effect of Metaphit was, however, to reduce N-methylaspartate induced excitation. It is concluded that Metaphit has mixed agonist/antagonist effects at the phencyclidine receptor.
分离麻醉药苯环己哌啶和氯胺酮可阻断N-甲基天冬氨酸对中枢神经元的兴奋作用。运用在体大鼠脊髓神经元微电泳技术,对苯环己哌啶受体酰化剂美他西泮进行测试,以观察其是否会拮抗分离麻醉药的这一作用。然而,美他西泮的主要作用却是减弱N-甲基天冬氨酸诱导的兴奋。得出的结论是,美他西泮在苯环己哌啶受体上具有激动/拮抗混合效应。