Potencies and stereoselectivities of enantiomers of huperzine A for inhibition of rat cortical acetylcholinesterase.

作者: Michael McKinney , Jacqueline H. Miller , Fumio Yamada , Werner Tuckmantel , Alan P. Kozikowski

DOI: 10.1016/0014-2999(91)90730-E

关键词:

摘要: The stereoselectivities and mechanisms of the inhibition rat cortical acetylcholinesterase by enantiomers huperzine A were determined. (-)-Huperzine was more potent enantiomer with a Ki value 8 nM. (+)-Huperzine inhibited enzyme 38-fold less potently 300 Racemic about two-fold than active isomer, (-)-huperzine A. mechanism for all three drugs mixed linear competitive type.

参考文章(9)
Samuel H. Wilson, Bruce K. Schrier, John L. Farber, Edward J. Thompson, Roger N. Rosenberg, Arthur J. Blume, Marshall W. Nirenberg, Markers for Gene Expression in Cultured Cells from the Nervous System Journal of Biological Chemistry. ,vol. 247, pp. 3159- 3169 ,(1972) , 10.1016/S0021-9258(19)45227-7
Xi-can Tang, Yong-xing Ma, Guo-wei Sang, Ren-min Yang, Rui-wu Zhang, Yan-yi Han, Ci-lu Zhang, Yang-da Zhang, Drug evaluation of huperzine A in the treatment of senile memory disorders Acta Pharmacologica Sinica. ,vol. 12, pp. 250- 252 ,(1991)
Yan Xia, Alan P. Kozikowski, A practical synthesis of the Chinese "nootropic" agent huperzine A: a possible lead in the treatment of Alzheimer's disease Journal of the American Chemical Society. ,vol. 111, pp. 4116- 4117 ,(1989) , 10.1021/JA00193A062
X.-C. Tang, P. De Sarno, K. Sugaya, E. Giacobini, Effect of huperzine A, a new cholinesterase inhibitor, on the central cholinergic system of the rat Journal of Neuroscience Research. ,vol. 24, pp. 276- 285 ,(1989) , 10.1002/JNR.490240220
Fumio Yamada, Alan P. Kozikowski, E. R. Reddy, Yuan Ping Pang, Jacqueline H. Miller, Michael McKinney, A route to optically pure (-)-huperzine A : molecular modeling and in vitro pharmacology Journal of the American Chemical Society. ,vol. 113, pp. 4695- 4696 ,(1991) , 10.1021/JA00012A056
MICHAEL McKINNEY, JOSEPH T. COYLE, The potential for muscarinic receptor subtype-specific pharmacotherapy for Alzheimer's disease. Mayo Clinic proceedings. ,vol. 66, pp. 1225- 1237 ,(1991) , 10.1016/S0025-6196(12)62474-4
Dong-xian Yue, Yue-e Wang, Xi-an Tang, [Anti-cholinesterase activity of huperzine A]. Acta Pharmacologica Sinica. ,vol. 7, pp. 110- 113 ,(1986)
Xi-Can Tang, Xiao-Fang Yan, Wei-Hua Lu, Wci-Jian Lou, Effects of huperzine A and B on skeletal muscle and the electroencephalogram Acta Pharmacologica Sinica. ,vol. 8, pp. 117- 123 ,(1987)