CONVULSANT, ANTICONVULSANT AND ANESTHETIC BARBITURATES - 5-ETHYL-5-(3'-METHYL-BUT-2'-ENYL)-BARBITURIC ACID AND RELATED COMPOUNDS

被引:51
作者
ANDREWS, PR [1 ]
JONES, GP [1 ]
LODGE, D [1 ]
机构
[1] AUSTRALIAN NATL UNIV,JOHN CURTIN SCH MED RES,DEPT PHARMACOL,CANBERRA 2601,ACT,AUSTRALIA
关键词
Anaesthetics; Anticonvulsants; Barbiturates; Convulsants; Structure-activity relationship;
D O I
10.1016/0014-2999(79)90382-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Barbiturates derived by minor structural changes to the butenyl sidechain of the convulsant 5-ethyl-5-(3′-methyl-but-2′-enyl)-barbituric acid are almost devoid of convulsant activity, but all have anaesthetic and anticonvulsant effects. Anticonvulsant activity is also observed in the convulsant barbiturate. Increased lipophilic character does not increase anaesthetic potency, only speed of onset, and anticonvulsant activity is reduced in the more lipophilic compounds. The stereochemistry at the 3′-position of the sidechain is vitally important to convulsant activity, and also influences anticonvulsant potency. © 1979.
引用
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页码:115 / 120
页数:6
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