Binding of the A1-selective adenosine antagonist 8-cyclopentyl-1,3-dipropylxanthine to rat brain membranes

1987 ◽  
Vol 335 (1) ◽  
pp. 59-63 ◽  
Author(s):  
Robert F. Bruns ◽  
James H. Fergus ◽  
Edward W. Badger ◽  
James A. Bristol ◽  
Lisa A. Santay ◽  
...  
1981 ◽  
Vol 59 (8) ◽  
pp. 897-900 ◽  
Author(s):  
Michael Williams ◽  
Edwin A. Risley ◽  
Joel R. Huff

The benzodiazepine anxiolytics flurazepam and diazepam and CL 218872, zopiclone and two β-carboline ethyl carboxyl esters, compounds which are potent displacers of specific [3H]diazepam binding from rat brain membranes, have little or no activity in displacing [3H]2-chloroadenosine ([3H]2-CADO) from central A1-adenosine receptors. Conversely, the purine agonists, 1-N6-phenylisopropyladenosine, N6-cyclohexyladenosine, 2-chloroadenosine. and the adenosine antagonist 8-phenyltheophylline have no significant effect on [3H]diazepam binding. Etazolate (SQ 20009) and Avermectin B1a which enhance [3H]diazepam binding in vitro were also without significant effect on [3H]2-CADO binding. The lack of correlation of the activities of the compounds examined in the two binding assays is discussed in relation to the hypothesis that purine-like compounds may be involved in the molecular mechanisms related to anxiolytic action at the receptor level.


1989 ◽  
Vol 264 (1) ◽  
pp. 354-362
Author(s):  
L H Lazarus ◽  
A Guglietta ◽  
W E Wilson ◽  
B J Irons ◽  
R de Castiglione

1991 ◽  
Vol 56 (5) ◽  
pp. 1804-1809 ◽  
Author(s):  
Peter J. Mannon ◽  
Sabrena J. Mervin ◽  
Ian L. Taylor

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