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Regulation of Adenosine Receptors in Rat Brain following Chronic Carbamazepine Treatment

Park, Kyung-Sun   (Department of Pharmacology and Institute of Basic Medical Sciences, Wonju College of Medicine, Yonsei UniversityUU0000936  ); Yang, Wan-Suk   (Department of Pharmacology and Institute of Basic Medical Sciences, Wonju College of Medicine, Yonsei UniversityUU0000936  ); Kim, Kyung-Hwan   (Department of Pharmacology, College of Medicine, Yonsei UniversityUU0000936  );
  • 초록

    Carbamazepine (CBZ), an anticonvulsant, has beeen 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 Al 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 $[^3CH]DPCPX$ was not significantly altered in membranes prepared from CBZ-treated rats. However, there was a significant decrease in the $A_1$ adenosine receptor-mediated stimulation of $[^{35}S]GTP_{\gamma}S$ 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.


  • 주제어

    Carbamazepine .   $A_1$ Adenosine receptor .   Cerebral cortex .   Adenylyl cyclase activity .   $[^{35}S]GTP_{\gamma}S$ binding .   $[^3H]DPCPX$ binding.  

 저자의 다른 논문

  • 박경선 (6)

    1. 1991 "흰쥐 말초 혈액 림프구의 분자량 44 kD 단백의 인산화" The Korean journal of pharmacology : official journal of the Society of Pharmacology, Republic of Korea 27 (2): 135~144    
    2. 1993 "Streptozotocin으로 당뇨병을 유발시킨 쥐의 지방세포에 나타나는 $A_{1}$, Adenosine Receptor-Adenylyl Cyclase System의 변화" The Korean journal of pharmacology : official journal of the Society of Pharmacology, Republic of Korea 29 (1): 97~105    
    3. 1993 "흰쥐 지방세포에 있어서 Amiloride의 $A_{1}$ Adenosine Receptor- Adenylyl Cyclase System에 대한 작용" The Korean journal of pharmacology : official journal of the Society of Pharmacology, Republic of Korea 29 (2): 245~252    
    4. 1993 "Streptozotocin으로 당뇨병을 유발시킨 흰쥐의 지방세포에서 일어나는 Insulin-Sensitive Phosphodiesterase의 조절에 관한 연구" The Korean journal of pharmacology : official journal of the Society of Pharmacology, Republic of Korea 29 (2): 253~261    
    5. 1996 "흰쥐의 뇌의$A_1$ 아데노신 수용체에 작용하는 역효현제에 관한 연구" The Korean journal of pharmacology : official journal of the Society of Pharmacology, Republic of Korea 32 (1): 23~29    
    6. 1996 "흰쥐 대뇌피질에서 $A_1$ 아데노신 수용체의 탈감작" The Korean journal of pharmacology : official journal of the Society of Pharmacology, Republic of Korea 32 (2): 151~158    
  • Yang, Wan-Suk (2)

  • 김경환 (40)

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