약학회지 (YAKHAK HOEJI)

  • 제51권5호
  • /
  • Pages.301-306
  • /
  • 2007
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  • 0377-9556(pISSN)
  • /
  • 2383-9457(eISSN)
대한약학회 (The Pharmaceutical Society of Korea)
권호 표지

항당뇨약 Rosiglitazone의 혈관 수축성에 대한 이중성 조절

Biphasic Effects of Rosiglitazone on Agonist-induced Regulation of Vascular Contractility

  • 박진건 (대구가톨릭대학교 약학대학 약물학교실) ;
  • 제현동 (대구가톨릭대학교 약학대학 약물학교실)
  • Park, Jin-Gun (Department of Pharmacology, College of Pharmacy, Catholic University of Daegu) ;
  • Je, Hyun-Dong (Department of Pharmacology, College of Pharmacy, Catholic University of Daegu)
  • 발행 : 2007.10.31
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초록

Rosiglitazone ($Avandia^{(R)}$) represents a new class of antidiabetic drugs which are $PPAR{\gamma}$ agonists. The present study was undertaken to determine whether the new antidiabetic rosiglitazone influences on the agonist-induced regulation of vascular smooth muscle contraction as an antihypertensive and, if so, to investigate the related mechanism. Endothelium-denuded arterial rings from male Sprague-Dawley rats were used and isometric contractions were recorded using a computerized data acquisition system. Rosiglitazone decreased Rho-kinase activating agonist (NaF or thromboxane $A_2$ mimetic)-induced contraction but not depolarization- or phorbol ester-induced contraction. Surprisingly, it slightly potentiated the latter contraction possibly opening a voltage-dependent calcium channel by its chemical structure on 50 mM KCI- or $1{\mu}M$ phorbol 12,13-dibutyrate-induced vasoconstriction. In conclusion, this study provides the evidence and possible related mechanism concerning the biphasic effect of an antidiabetic rosiglitazone as a possible antihypertensive on the agonistinduced contraction in rat aortic rings regardless of endothelial function.

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