http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Rudolf Gesztelyi,Zita Wachal,Bela Juhasz,Mariann Bombicz,Evelin Csepanyi,Krisztian Pak,Judit Zsuga,Csaba Papp,Zoltan Galajda,Klara Branzaniuc,Robert Porszasz,Andras Jozsef Szentmiklosi,Arpad Tosaki,Zs 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.3
A1 adenosine receptors (A1 receptors) arewidely expressed in mammalian tissues; therefore attainingproper tissue selectivity is a cornerstone of drug development. The fact that partial agonists chiefly act on tissueswith great receptor reserve can be exploited to achieve anappropriate degree of tissue selectivity. To the best of ourknowledge, the A1 receptor reserve has not been yetquantified for the atrial contractility. A1 receptor reservewas determined for the direct negative inotropic effect ofthree A1 receptor full agonists (NECA, CPA and CHA) inisolated, paced guinea pig left atria, with the use of FSCPX, an irreversible A1 receptor antagonist. FSCPXcaused an apparently pure dextral displacement of theconcentration–response curves of A1 receptor agonists. Accordingly, the atrial A1 receptor function converging toinotropy showed a considerably great, approximately80–92 % of receptor reserve for a near maximal (about91–96 %) effect, which is greater than historical atrial A1receptor reserve data for any effects other than inotropy. Consequently, the guinea pig atrial contractility is verysensitive to A1 receptor stimulation. Thus, it is worthwhileconsidering that even partial A1 receptor agonists, given inany indication, might decrease the atrial contractile force,as an undesirable side effect, in humans.