2-IMINO-1,3,4-THIADIAZOLE DERIVATIVES OF GABA AS GABA-A ANTAGONISTS

被引:5
作者
ALLAN, RD
APOSTOPOULOS, C
RICHARDSON, JA
机构
[1] Department of Pharmacology, University of Sydney, NSW
关键词
D O I
10.1071/CH9901767
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
New heterocyclic derivatives of GABA, with a GABA moiety on the 3 position of a 2-imino-1, 3, 4- thiadiazole ring, have been readily prepared by alkylation of 2-amino-5-aryl-1, 3, 4-thiadiazoles in dimethylformamide. They are active as GABAA antagonists, inhibiting the action of gaba on the guinea-pig ileum about 5 times less potently than bicuculline. © 1990 ASEG.
引用
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页码:1767 / 1772
页数:6
相关论文
共 19 条
[1]  
ALBERT A, 1962, IONIZATION CONSTANTS, P69
[2]  
BOWMAN WC, 1980, TXB PHARM
[3]  
FOYE WO, 1981, PRINCIPLES MED CHEM
[4]   A STEROID DERIVATIVE, R-5135, ANTAGONIZES THE GABA-BENZODIAZEPINE RECEPTOR INTERACTION [J].
HUNT, P ;
CLEMENTSJEWERY, S .
NEUROPHARMACOLOGY, 1981, 20 (04) :357-361
[5]  
JOHNSTON GAR, 1976, GABA NERVOUS SYSTEM, P395
[6]  
JOHNSTON GAR, 1986, BENZODIAZEPINE GABA, P57
[7]  
KORNIS G, 1984, COMPREHENSIVE HETERO, P545
[8]   GABA INDUCED EXCITATORY RESPONSES IN THE GUINEA-PIG SMALL-INTESTINE ARE ANTAGONIZED BY BICUCULLINE, PICROTOXININ AND CHLORIDE-ION BLOCKERS [J].
KRANTIS, A ;
KERR, DIB .
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1981, 317 (03) :257-261
[9]  
MALBEC F, 1984, J HETEROCYCLIC CHEM, V21, P1689, DOI 10.1002/jhet.5570210624
[10]  
ONG J, 1983, European Journal of Pharmacology, V86, P9