흰쥐 대뇌피질에서 A1 아데노신 수용체의 탈감작

• 영문명: Desensitization of A₁ Adenosine Receptors in Rat Cerebral Cortex
• 발행기관: 대한약리학회
• 저자명: 박경선(Kyung Sun Park) 양완숙(Wan Suk Yang) 김경환(Kyung Hwan Kim)
• 간행물 정보: 『대한약리학잡지』제32권 제2호, 151~158쪽, 전체 8쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1996.09.30

영문 초록

Following the subcutaneous administration of R(-)N⁶-(2-phenylisopropyl)adenosine(600 nmol/kg/hr) to rats for 1 week using tAlzet^？？ mini-osmotic pumps, A₁ adenosine receptor functions were determined using [³H]DPCPX binding, [³⁵S]GTP_γS binding, and adenylyl cyclase assays. A₁ adenosine receptor binding and the inhibition of adenylyl cyclase activity by PIA was not altered in cerebrocortical membranes prepared from PIA-treated rats. However, there was a significant decrease in the A₁ adenosine receptor-mediated stimulation of [³⁵S]GTP_γS binding to cerebrocortical membranes prepared from PIA-treated rats(22.0% decrease in basal activity; 19.7% decrease in maximal activity). These results suggest that the desensitization of A₁ adenosine receptors following chronic administration involves agonist-induced uncoupling of the receptors from G proteins rather than alteration of A₁ adenosine receptor molecules. It is also suggested that the determination of stimulation of [³⁵S]GTP_γS binding to G proteins is a suitable tool in studying the receptor regulation including desensitization

키워드

Desensitization Cerebral cortex A₁ adenosine receptor Adenylyl cyclase activity [³⁵S]GTP_γS binding [³H]DPCPX binding