D'Amico M, Berrino L, Maione S, Filippelli A, de Novellis V, Rossi F
Institute of Pharmacology and Toxicology, Faculty of Medicine and Surgery, II University of Naples, Italy.
Pain. 1996 May-Jun;65(2-3):205-9. doi: 10.1016/0304-3959(95)00178-6.
The aim of the study was to examine whether endothelin-1 (ET-1) injected into dorsolateral periaqueductal gray (PAG) area of mice produces antinociception. ET-1, from 1 to 4 pmol/mouse, induced antinociceptive effect in a dose-dependent manner. This antinociceptive effect was prevented by NMDA receptor antagonists (2-APV and MK-801) injected in the same area (2-APV) or by intraperitoneal route (MK-801). CNQX, a non-NMDA receptor antagonist, did not inhibit the ET-1 effects. Prazosin, an alpha 1-adrenergic blocking agent, also prevented the ET-1 antinociceptive effect. We suggest that the activation of NMDA glutamatergic receptors in the PAG area may be a necessary step for ET-1 induced antinociception.
本研究的目的是检测注射到小鼠背外侧导水管周围灰质（PAG）区域的内皮素-1（ET-1）是否产生抗伤害感受作用。每只小鼠注射1至4皮摩尔的ET-1，以剂量依赖方式诱导抗伤害感受效应。这种抗伤害感受效应可被注射到同一区域（2-氨基-5-磷酰戊酸）或经腹腔途径（地卓西平马来酸盐）的NMDA受体拮抗剂所阻断。非NMDA受体拮抗剂CNQX不抑制ET-1的作用。α1-肾上腺素能阻滞剂哌唑嗪也可阻断ET-1的抗伤害感受效应。我们认为，PAG区域中NMDA谷氨酸能受体的激活可能是ET-1诱导抗伤害感受的必要步骤。
