Daniell L C
Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta 30912-2300.
Pharmacol Biochem Behav. 1990 May;36(1):111-5. doi: 10.1016/0091-3057(90)90134-4.
The potency of general anesthetics from different chemical classes was tested after pretreatment with subanesthetic doses of noncompetitive N-methyl-D-aspartate (NMDA) antagonists in mice. Changes in general anesthetic potency were assessed by determination of alteration of duration of loss of righting reflex for ethanol and pentobarbital and changes in the minimum alveolar concentration (MAC) for the volatile anesthetics, halothane and diethyl ether. The ability of the noncompetitive NMDA antagonists, MK-801 [(+)-5-methyl-10,11-dihydro-5H-dibenzo(a,d)cyclo-hepten-5,10-imine ], phencyclidine (PCP) and ketamine, to increase the potency of general anesthetics paralleled their potency as NMDA antagonists and their affinity for the PCP receptor site of the NMDA receptor-ionophore complex (MK-801 greater than PCP greater than ketamine). These results indicate that block of central NMDA receptors may contribute to the production of anesthesia by a variety of agents.
在用亚麻醉剂量的非竞争性N-甲基-D-天冬氨酸（NMDA）拮抗剂预处理小鼠后，测试了不同化学类别的全身麻醉药的效能。通过测定乙醇和戊巴比妥致翻正反射消失持续时间的改变以及挥发性麻醉药氟烷和乙醚的最低肺泡浓度（MAC）的变化，评估全身麻醉药效能的改变。非竞争性NMDA拮抗剂MK-801[（+）-5-甲基-10,11-二氢-5H-二苯并（a，d）环庚烯-5,10-亚胺]、苯环己哌啶（PCP）和氯胺酮增强全身麻醉药效能的能力与其作为NMDA拮抗剂的效能及其对NMDA受体-离子通道复合物的PCP受体位点的亲和力平行（MK-801＞PCP＞氯胺酮）。这些结果表明，中枢NMDA受体的阻断可能有助于多种药物产生麻醉作用。
