|
KMID : 0811719970010010013
|
|
Korean Journal of Physiology & Pharmacology
1997 Volume.1 No. 1 p.13 ~ p.17
|
|
|
Regulation of Adenosine Receptors in Rat Brain following Chronic CarbamaBepine Treatments
|
|
Kyung Sun Park
Wan Suk Yang/Kyung Hwan Kim
|
|
|
Abstract
|
|
|
|
Carbamazepine (CBZ), an anticonvulsant, has been reported to displace ligands at adenosine receptors. Several studies have demonstrated that as far as A-2 adenosine receptors is concerned, CBZ acts as an antagonist. However, the situation with regard to A-1 receptors is less straightforward. In this study, we describe the effects of one-week CBZ treatment (25 mg/kg/day) on cerebrocortical A-1 adenosine receptors. A-1 adenosine receptor bindings as determined by using (3H)DPCPX was not significantly altered in membranes prepared from CBZ-treated rats. However, there was a significant decrease in the A, adenosine receptor-mediated stimulation of (35S)GTP-gamma-S binding to cerebrocortical membranes prepared from CBZ-treated rats (20.0% decrease in basal activity; 17.8% decrease in maximal activity). The basal and 10-4 M forskolin-stimulated adenylyl cyclase activities were relatively unaffected by CBZ treatment, but 10 mM NaF-stimulated adenylyl cyclase activity was significantly reduced in CBZ-treated rats. It appears that one-week CBZ treatment caused an uncoupling of adenosine receptors from G proteins without alteration of A-1 adenosine receptor molecules, suggesting that CBZ acts as an agonist at A-1 adenosine receptors in rat brain.
|
|
|
KEYWORD
|
|
|
|
|
|
FullTexts / Linksout information
|
|
|
|
|
Listed journal information
|
|
  
|