Hunter J C, Singh L
Department of Biology, Parke-Davis Neuroscience Research Centre, Addenbrookes Hospital Site, Cambridge, UK.
Neurosci Lett. 1994 Jun 20;174(2):217-21. doi: 10.1016/0304-3940(94)90025-6.
The relative contribution of the NMDA/glycine allosteric site and non-NMDA (AMPA) types of glutamate receptor to the acute and tonic phases of the behavioural nociceptive response to formalin has been studied in the rat. The AMPA receptor selective antagonist NBQX preferentially inhibited the acute phase indicating that AMPA receptors may be involved in mediating fast acute nociceptive transmission in the dorsal horn. In contrast, the strychnine-insensitive glycine site partial agonist (+)-HA-966 and the NMDA competitive antagonist CGS 19755 preferentially attenuated the tonic nociceptive phase. However, none of these compounds exhibited anti-inflammatory properties. Thus, both NMDA and non-NMDA antagonists can selectively block changes in neuronal excitability while tissue injury in the receptive field continues to evolve.
在大鼠中,已研究了NMDA/甘氨酸变构位点和非NMDA(AMPA)型谷氨酸受体对福尔马林行为性伤害感受反应的急性期和强直期的相对贡献。AMPA受体选择性拮抗剂NBQX优先抑制急性期,表明AMPA受体可能参与介导背角中快速的急性伤害感受性传递。相反,士的宁不敏感的甘氨酸位点部分激动剂(+)-HA-966和NMDA竞争性拮抗剂CGS 19755优先减弱强直伤害感受期。然而,这些化合物均未表现出抗炎特性。因此,NMDA和非NMDA拮抗剂均可选择性地阻断神经元兴奋性的变化,而感受野中的组织损伤仍在继续发展。