Nakahara N, Fujise N, Kawanishi G, Mizobe F
Research Institute of Life Science, Snow Brand Milk Products Co. Ltd., Tochigi, Japan.
Brain Res. 1990 Jan 15;507(1):172-5. doi: 10.1016/0006-8993(90)90541-i.
Effects of FKS-508 (AF102B; cis-2-methylspiro (1,3-oxathiolane-5,3')-quinuclidine), a novel M1-selective agonist, on central muscarinic responses in mice were examined in comparison with oxotremorine. FKS-508 was slightly less potent (6 times) in reversal of scopolamine-induced amnesia (passive avoidance failure), but far less potent (260 and 55 times) in producing hypothermia and tremor than oxotremorine. These results show that the selective M1 agonist FKS-508 differentiates highly between the central muscarinic effects.
将新型M1选择性激动剂FKS-508(AF102B;顺式-2-甲基螺(1,3-氧硫杂环戊烷-5,3')-奎宁环)与氧化震颤素进行比较,研究了其对小鼠中枢毒蕈碱反应的影响。FKS-508在逆转东莨菪碱引起的失忆(被动回避失败)方面效力略低(6倍),但在产生体温过低和震颤方面的效力远低于氧化震颤素(分别为260倍和55倍)。这些结果表明,选择性M1激动剂FKS-508在中枢毒蕈碱效应之间具有高度差异。