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비-혈관평활근에서 새로운 $K^+$ 통로 개방제인 SKP-450의 약리학적 작용의 특성-Levcromakalim의 작용과 비교
In Vitro Pharmacological Characteristics of SKP-450, A Novel $K^+$ Channel Opener, in Non-Vascular Smooth Muscles in Comparison with Levcromakalim

박지영   (부산대학교 의과대학 약리학교실UU0000613  ); 김현희   (부산대학교 의과대학 약리학교실UU0000613  ); 유성은   (대전 한국화학연구소CC0186998  ); 홍기환   (부산대학교 의과대학 약리학교실UU0000613  );
  • 초록

    In the present study, we characterized the non-vascular smooth muscle relaxant effects of a novel benzoyran derivative ,SKP-450 (2-[2'(1',3'-dioxolone)-2-methyl-4- (2'-oxo-1'-pyrrolidinyl) -6-nitro-2H-1- benzopyran) and its metabolite, SKP-310, in comparison with levcromakalim (LCRK). In the rat stomach fundus, the spontaneous motility stimulated by $10^{-6.5}\;M$ bethanechol was completely eliminated not only by $10^{-7}\;M$ SKP-450 but also by $10^{-6}\;M$ LCRK, which were blocked by $10^{-6}\;M$ glibenclamide. The inhibitory effect of SKP-450 $pD_2,\;3.94{\pm}0.66)$ was much less than LCRK $(pD2,\;5.73{\pm}0.38,\;p . In the bethanechol $(10{-6.5 }\;M)-stimulated$ urinary bladder, the tonus was decreased in association with elimination of spontaneous motility by $10^{-7}\;M$ M SKP-450 and $10^{-6}\;M\;LCRK\;(pD2,\;6.77{\pm}0.06)\;(P , which were inhibitable by $10^{-6}\;M$ glibenclamide. The inhibitory effect of SKP-450 $(pD2,\;7.66{\pm}0.05)$ was significantly more potent than that of LCRK $(pD2,\;6.77{\pm}0.06,\;p . In the rat uterus stimulated by $PGF_{2\alpha}\;(10^{-7}\;M)$ , both increased tonus and spontaneous motility were eliminated by $10^{-6}\;M$ LCRK with slight depression of the tonus, but not by SKP-450 $(10^{-5}\;M)$ . The stimulated trachea of guinea-pig by $10^{-6.5}\;M$ bethanechol was moderately suppressed by SKP-450 $(10^{-6}{sim}10^{-5}\;M)$ but little by SKP-310. In association with the relaxant effects, SKP-450 $(10^{-6}\;M)$ and LCRK $(10^{-5}\;M)$ caused a significant stimulation of the $^{86}Rb$ efflux from rat urinary bladder and stomach fundus, which were antagonized by $10^{-5}\;M$ glibenclamide, whereas the $K^+$ channel openers could not exert a stimulation of the $^{86}Rb$ efflux from rat uterus. In conclusion, it is suggested that SKP-450 exerts potent relaxant effects on the urinary bladder detrusor muscle and duodenum, whereas it shows much less effect on stomach fundus and uterus as contrasted to LCRK.


  • 주제어

    Non-Vascular Smooth Muscle .   Levcromakalim .   SKP-450.  

 저자의 다른 논문

  • 박지영 (2)

    1. 1997 "Mechanisms Underlying Relaxations Caused by Angiotensin II and Its Analogs in Isolated Rabbit Mesenteric Artery" The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology 1 (4): 393~402    
    2. 2005 "Gene Transfer of Cu/ZnSOD to Cerebral Vessels Prevents Subarachnoid Hemorrhage-induced Cerebral Vasospasm" The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology 9 (6): 327~332    
  • 김현희 (1)

  • 유성은 (30)

  • 홍기환 (34)

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