Chopin Philippe, Colpaert Francis C, Marien Marc
Centre de Recherche Pierre Fabre, Castres, France.
J Pharmacol Exp Ther. 2002 Apr;301(1):187-96. doi: 10.1124/jpet.301.1.187.
The present study examined the influence of dexefaroxan, a potent and selective alpha(2)-adrenoceptor antagonist, on cognitive performance in rodents. In young adult rats, dexefaroxan reversed the deficits induced by UK 14304 [5-bromo-N-(4,5-dihydro-1-H-imidazol-2-yl)-6-quinoxalinamine], scopolamine, and diazepam in a passive avoidance task. In this test, dexefaroxan also attenuated the spontaneous forgetting induced by a 15-week training-testing interval. Moreover, dexefaroxan, given immediately after training, increased the memory performance of rats trained with a weak electric footshock in the passive avoidance test, facilitated spatial memory processes in the Morris water maze task in rats, and increased the performance of mice in an object recognition test. Thus, dexefaroxan appears to have a promnesic effect in these tests by facilitating the processes of memory retention, rather than acquisition or other noncognitive influences. The facilitatory effects of dexefaroxan in young adult rats persisted even after a 21- to 25-day constant subcutaneous infusion by using osmotic minipumps, indicating that tolerance to the promnesic effect of the drug did not occur during this prolonged treatment interval. Furthermore, in the passive avoidance and Morris water maze tests, dexefaroxan ameliorated the age-related memory deficits of 24-month-old rats to a level that was comparable to that of young adult animals, and reversed the memory deficits induced by excitotoxin lesions of the nucleus basalis magnocellularis region. Together, these findings support a potential utility of dexefaroxan in the treatment of cognitive deficits occurring in Alzheimer's disease.
本研究考察了强效选择性α₂肾上腺素能受体拮抗剂右苯丙胺对啮齿动物认知能力的影响。在年轻成年大鼠中,右苯丙胺可逆转UK 14304[5-溴-N-(4,5-二氢-1-H-咪唑-2-基)-6-喹喔啉胺]、东莨菪碱和地西泮在被动回避任务中诱导的缺陷。在该试验中,右苯丙胺还可减轻15周训练-测试间隔诱导的自发遗忘。此外,训练后立即给予右苯丙胺,可提高在被动回避试验中接受弱电足电击训练的大鼠的记忆能力,促进大鼠在莫里斯水迷宫任务中的空间记忆过程,并提高小鼠在物体识别试验中的表现。因此,右苯丙胺在这些试验中似乎具有促进记忆的作用,其机制是促进记忆保留过程,而非获取过程或其他非认知影响。即使通过渗透微型泵进行21至25天的持续皮下输注,右苯丙胺对年轻成年大鼠的促进作用仍然存在,这表明在这一延长的治疗间隔期间未出现对该药物促进记忆作用的耐受性。此外,在被动回避和莫里斯水迷宫试验中,右苯丙胺可将24月龄大鼠与年龄相关的记忆缺陷改善至与年轻成年动物相当的水平,并逆转基底大细胞核区域兴奋性毒素损伤诱导的记忆缺陷。总之,这些发现支持右苯丙胺在治疗阿尔茨海默病中出现的认知缺陷方面具有潜在的应用价值。