scholarly journals Inhibitory effects of quinolone antibacterial agents on gamma-aminobutyric acid binding to receptor sites in rat brain membranes.

1988 ◽  
Vol 32 (2) ◽  
pp. 190-194 ◽  
Author(s):  
A Tsuji ◽  
H Sato ◽  
Y Kume ◽  
I Tamai ◽  
E Okezaki ◽  
...  
1989 ◽  
Vol 42 (7) ◽  
pp. 1133 ◽  
Author(s):  
GB Barlin ◽  
LP Davies ◽  
SJ Ireland ◽  
MML Ngu

Syntheses are reported for a number of 3-alkoxy-6-benzylthio(substituted benzylthio and other phenylalkylthio )-2-phenyl(and substituted phenyl)imidazo[l,2-b]pyridazines. These compounds were then examined for their ability to displace 3H-diazepam from rat brain membranes. In preliminary tests, in the presence of 100 �m γ- aminobutyric acid (GABA) and under standard assay conditions (see Experimental), 6-benzylthio-3-methoxy-2-phenylimidazo[l,2- b]pyridazine gave an lC50 value of 25nM (IC50 for unlabelled diazepam is 4.3 nM ); its 6-(m- aminophenyl ), 6-(p- aminophenyl ) and 6-(m- nitrophenyl ) analogues gave values of 15, 9 and 8 nM respectively.


1996 ◽  
Vol 27 (1) ◽  
pp. 137-140 ◽  
Author(s):  
Ying-Li Qu ◽  
Kentaro Sugiyama ◽  
Kaoru Hattori ◽  
Ayumi Yamamoto ◽  
Kenichi Watanabe ◽  
...  

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