STRUCTURE AND ACTIVITY OF HYDROGENATED DERIVATIVES OF (+)-5-METHYL-10,11-DIHYDRO-5H-DIBENZO[A,D]CYCLOHEPTEN-5,10-IMINE (MK-801)

被引:17
作者
LYLE, TA [1 ]
MAGILL, CA [1 ]
BRITCHER, SF [1 ]
DENNY, GH [1 ]
THOMPSON, WJ [1 ]
MURPHY, JS [1 ]
KNIGHT, AR [1 ]
KEMP, JA [1 ]
MARSHALL, GR [1 ]
MIDDLEMISS, DN [1 ]
WONG, EHF [1 ]
ANDERSON, PS [1 ]
机构
[1] NEUROSCI RES CTR,HARLOW CM 20 2QR,ESSEX,ENGLAND
关键词
D O I
10.1021/jm00165a026
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several hydrogenated derivatives of the potent NMDA antagonist 1 have been prepared and evaluated as competitive inhibitors of [3H]-1 binding. These compounds were also tested for their ability to act as noncompetitive antagonists of NMDA in vitro. These studies indicate that two aromatic rings are not strictly required for high-affinity binding or NMDA antagonism. © 1990, American Chemical Society. All rights reserved.
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页码:1047 / 1052
页数:6
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