[3H]Dipyridamole Binding to Guinea Pig Brain Membranes: Possible Heterogeneity of Central Adenosine Uptake Sites

1987 ◽  
Vol 48 (4) ◽  
pp. 1231-1236 ◽  
Author(s):  
Paul J. Marangos ◽  
Jurgen Deckert
1988 ◽  
Vol 42 (2) ◽  
pp. 313-316 ◽  
Author(s):  
Jürgen Deckert ◽  
Philipp F. Morgan ◽  
Jean-Luc Daval ◽  
Takashi Nakajima ◽  
Paul J. Marangos

1982 ◽  
Vol 60 (3) ◽  
pp. 302-307 ◽  
Author(s):  
M. J. York ◽  
L. P. Davies

We have used the adenosine-stimulated adenylate cyclase of guinea-pig brain to examine the potency of diazepam as an adenosine uptake inhibitor. Diazepam at concentrations in the range 10–500 μM stimulates the production of cAMP in incubated slices of guinea-pig cerebral cortex, with maximal fivefold stimulations over basal levels by 200 μM diazepam. The increases can be largely (but not completely) blocked by the adenosine antagonist theophylline or by addition of excess adenosine deaminase to the system. It appears that the stimulation of cAMP production is due to a blockade of adenosine uptake which results in an increase in extracellular adenosine and concomitant activation of the adenosine receptor coupled to adenylate cyclase. Since the cAMP response to standard adenosine uptake blockers (dipyridamole, dilazep) can be completely blocked by theophylline or adenosine deaminase, a small component of the diazepam response cannot be explained by an adenosine effect. The concentration of diazepam at which the first significant cAMP increase occurs is 10 μM or slightly lower. This is significantly higher than the concentration of diazepam needed to saturate the pharmacologically characterized central nervous system receptors for benzodiazepines.


1993 ◽  
Vol 238 (1) ◽  
pp. 93-100
Author(s):  
Tanaka Makoto ◽  
Shinsuke Kaku ◽  
Makoto Muramatsu ◽  
Susumu Otomo

1994 ◽  
Vol 267 (3) ◽  
pp. 297-305 ◽  
Author(s):  
Jean-Christophe Lallement ◽  
Jean-Claude Galleyrand ◽  
Ana-Christina Lima-Leite ◽  
Pierre Fulcrand ◽  
Jean Martinez

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