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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Effects of NMDA receptor antagonists on acute mu-opioid analgesia in the rat.
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Effects of NMDA receptor antagonists on acute mu-opioid analgesia in the rat.

机译：NMDA受体拮抗剂对大鼠急性阿片类镇痛的作用。

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Mixed research findings have led to a debate regarding the effect of N-methyl-D-aspartate (NMDA) receptor antagonists on opiate analgesia. NMDA antagonists have been found in various studies to enhance, to inhibit, or to have no effect on opiate analgesia. The present research used a single protocol to explore the effects of six NMDA receptor antagonists on acute morphine (3.0 mg/kg s.c.) and fentanyl (0.05 mg/kg s.c.) analgesia in adult male Sprague-Dawley rats. NMDA receptor antagonists were selected based on their abilities to block various sites on the NMDA receptor complex, including the noncompetitive antagonists MK-801 (0.1 and 0.3 mg/kg i.p.), dextromethorphan (10.0 and 30.0 mg/kg i.p.), and memantine (3.0 and 10.0 mg/kg i.p.), a glycine site antagonist, (+)-HA-966 (10.0 and 30.0 mg/kg i.p.), a competitive antagonist, LY235959 (1.0 and 3.0 mg/kg i.p.), and a polyamine site antagonist, ifenprodil (1.0 and 3.0 mg/kg i.p.). Analgesia was assessed using the tail-flick test. A single dose of each opiate was used. The low doses of the antagonists, which are known to produce significant neural and behavioral actions at NMDA receptors, had no effect on morphine or fentanyl analgesia. At the higher doses, morphine analgesia was significantly enhanced by LY235959 (3.0 mg/kg), and fentanyl analgesia was significantly enhanced by LY235959 (3.0 mg/kg), dextromethorphan (30.0 mg/kg), and (+)-HA-966 (30.0 mg/kg). Enhancement of analgesia occurred without any apparent adverse side effects. None of the NMDA antagonists affected tail-flick responses on their own, except the higher dose of LY235959 (3.0 mg/kg), which produced a mild analgesic effect. Because no consistent effects were observed, the data suggest that NMDA receptors are not involved in acute mu-opioid analgesia. The mechanisms underlying the enhancement of opiate analgesia by selected NMDA antagonists, such as LY235959, dextromethorphan, and (+)-HA-966, remain to be determined.
机译：混杂的研究发现导致了有关N-甲基-D-天冬氨酸（NMDA）受体拮抗剂对阿片类镇痛作用的争论。在各种研究中已经发现NMDA拮抗剂可增强，抑制或对阿片类镇痛没有作用。本研究使用单一方案探讨了六种NMDA受体拮抗剂对成年雄性Sprague-Dawley大鼠急性吗啡（3.0 mg / kg s.c.）和芬太尼（0.05 mg / kg s.c.）镇痛的作用。根据NMDA受体拮抗剂阻断NMDA受体复合物各个部位的能力来选择NMDA受体拮抗剂，包括非竞争性拮抗剂MK-801（0.1和0.3 mg / kg ip），右美沙芬（10.0和30.0 mg / kg ip）和美金刚（ 3.0和10.0 mg / kg ip），甘氨酸位点拮抗剂，（+）-HA-966（10.0和30.0 mg / kg ip ip），竞争性拮抗剂LY235959（1.0和3.0 mg / kg ip ip）和多胺位点拮抗剂，艾芬地尔（1.0和3.0 mg / kg ip）。使用甩尾试验评估镇痛效果。每种鸦片均使用一剂。已知对NMDA受体产生明显神经和行为作用的低剂量拮抗剂对吗啡或芬太尼镇痛没有作用。在较高剂量下，LY235959（3.0 mg / kg）可显着增强吗啡镇痛作用，LY235959（3.0 mg / kg），右美沙芬（30.0 mg / kg）和（+）-HA-966显着增强吗啡镇痛作用（30.0 mg / kg）。镇痛作用增强，没有任何明显的不良副作用。除较高剂量的LY235959（3.0 mg / kg）产生轻微的镇痛作用外，没有NMDA拮抗剂独自影响甩尾反应。由于未观察到一致的作用，因此数据表明NMDA受体不参与急性阿片类镇痛。选定的NMDA拮抗剂（例如LY235959，右美沙芬和（+）-HA-966）增强阿片类镇痛作用的机制尚待确定。

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