Lallement G, Pernot-Marino I, Foquin-Tarricone A, Baubichon D, Piras A, Blanchet G, Carpentier P
Centre de Recherches du Service de Santé des Armées, Unité de Neurotoxicologie, La Tronche, France.
Neuroreport. 1994 Jan 12;5(4):425-8. doi: 10.1097/00001756-199401120-00013.
The ability of NBQX, a potent antagonist of AMPA glutamatergic receptors, to prevent or stop seizures induced by the organophosphate soman, an irreversible inhibitor of AChE, was studied in rats. NBQX administered concomitantly with soman prevents the onset of seizures (ED50: 29.2 mg kg-1, i.p.). Administered 5 min after the onset of seizures, NBQX greatly reduces the intensity of the epileptic activity. The same decrease of epileptic activity is observed, in the presence of atropine, when the administration of NBQX is delayed 15 min after the onset of seizures. NBQX thus appears as a promising antiepileptic candidate against soman-induced seizures. The roles of AMPA and muscarinic receptors in the onset and propagation of soman-induced epileptic activity are discussed.
在大鼠中研究了AMPA谷氨酸能受体的强效拮抗剂NBQX预防或终止由有机磷酸酯梭曼(一种乙酰胆碱酯酶不可逆抑制剂)诱发癫痫发作的能力。与梭曼同时给药的NBQX可预防癫痫发作的发生(半数有效剂量:29.2毫克/千克,腹腔注射)。在癫痫发作开始5分钟后给药,NBQX可大大降低癫痫活动的强度。当在癫痫发作开始15分钟后延迟给予NBQX时,在阿托品存在的情况下,也观察到癫痫活动有同样程度的降低。因此,NBQX似乎是一种有前景的抗癫痫药物,可对抗梭曼诱发的癫痫发作。文中讨论了AMPA和毒蕈碱受体在梭曼诱发癫痫活动的发生和传播中的作用。