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Chemical Compound Review

AC1MHWSO     (2R)-N-methyl-1-oxo-2- pyridin-3-yl-thiane...

Synonyms: CHEMBL76358, RP-49356, RP-52891, LS-178092, RP 49356, ...
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Disease relevance of RP 49356

  • Aprikalim-induced arterial hypotension was significantly less marked in cirrhotic than in normal rats [1].
  • The ability of aprikalim and the K(ATP) channel antagonists to alter postischemic wall function occurred independently of differences in systemic hemodynamics, area at risk, and collateral blood flow during occlusion, the major determinants of the extent of myocardial stunning [2].
  • Aprikalim, a K+ ATP channel opener, is a potent vasodilator with demonstrated cardioprotective properties against ischemia/reperfusion injury [3].
  • BACKGROUND AND PURPOSE: Cerebral vasodilatation in response to aprikalim, an opener of ATP-sensitive K+ channels, is selectively augmented after subarachnoid hemorrhage (SAH) [4].
  • METHODS: Isovolumetric rat hearts (37 degrees C) were treated with 1 microM (apri 1) or 30 microM (apri 30) aprikalim, or preconditioned with either 10 min of hypoxia (N2PC) or 5 min of ischaemia followed by 5 min of perfusion (IPC5) or 10 min of ischaemia followed by 3 min of perfusion (IPC10) [5].

High impact information on RP 49356


Chemical compound and disease context of RP 49356


Biological context of RP 49356

  • At 2 h of low flow ischaemia systolic pressure was 39(4)%, 37(5)%, 41(4)%, and 37(3)% of control for hearts treated with saline aprikalim, glibenclamide, and SPT, respectively [11].
  • OBJECTIVE: The aim was to compare the effects of a potassium channel opener, aprikalim, and of hypoxic and ischaemic preconditioning on extracellular K+ concentration change, metabolism, and ventricular function in isolated globally ischaemic rat hearts [5].
  • Inhibition of vasoconstriction by potassium channel opener aprikalim in human conduit arteries used as bypass grafts [12].
  • The assay was used successfully to determine aprikalim pharmacokinetics in mice, monkeys, and dogs [13].
  • In a normothermic (37 degrees C) isolated rabbit heart preparation, aprikalim was found to rapidly shorten the action potential duration and produce cardiac asystole that was maintained during 20 minutes of "no-flow" global ischemia without a rise in end-diastolic pressure [14].

Anatomical context of RP 49356


Associations of RP 49356 with other chemical compounds


Gene context of RP 49356

  • Arteriolar responses to aprikalim (10(-8) and 10(-6) mol/L), a pharmacological activator of ATP-sensitive K+ channels, and iloprost (0.1 and 1 microgram/mL), a physiological activator of these channels, were determined before and 1, 2, and 4 hours after a 10-minute period of total global ischemia [24].
  • In rat Langendorff-perfused heart with base-line coronary flow reduced by the addition of ET-1 to the perfusion medium, nicorandil and aprikalim increased coronary flow, while nitroglycerin did not [25].
  • In contrast, aprikalim did not significantly depress the contraction induced by ET-1 (p > 0.05) [26].
  • The inside-out patch clamp technique was used to record the effects of K+ channel openers (EMD 52692, RP 49356 and Cromakalim) on single channel currents in membrane blebs of human skeletal muscle [27].
  • Aprikalim is a potent, specific, and selective opener of ATP-sensitive K+ (KATP) channels [28].

Analytical, diagnostic and therapeutic context of RP 49356

  • However, administration of aprikalim immediately before reperfusion had no beneficial effect [2].
  • The mechanism whereby RP 49356, a novel potassium channel opener, activates ATP-sensitive K+ channels (K+-ATP channels) in isolated cardiac cells was investigated with the patch-clamp technique [15].
  • RESULTS: At constant coronary flow aprikalim reduced perfusion pressure from 53(SEM 5) to 25(1) mm Hg (p < 0.001) in piglet hearts and from 55(5) to 39(5) mm Hg (p < 0.05) in rabbit hearts [11].
  • Aprikalim also attenuated significantly the [Ca2+]i elevated during cardioplegia [23].
  • Aprikalim: radioimmunoassay and pharmacokinetic studies in mouse, monkey, and dog [13].


  1. Altered control of vascular tone by adenosine triphosphate-sensitive potassium channels in rats with cirrhosis. Moreau, R., Komeichi, H., Kirstetter, P., Ohsuga, M., Cailmail, S., Lebrec, D. Gastroenterology (1994) [Pubmed]
  2. Pharmacological evidence for a role of ATP-dependent potassium channels in myocardial stunning. Auchampach, J.A., Maruyama, M., Cavero, I., Gross, G.J. Circulation (1992) [Pubmed]
  3. Protective effects of the K+ ATP channel opener, aprikalim, against free radicals in isolated rabbit hearts. Pignac, J., Lacaille, C., Dumont, L. Free Radic. Biol. Med. (1996) [Pubmed]
  4. Effect of subarachnoid hemorrhage on cerebral vasodilatation in response to activation of ATP-sensitive K+ channels in chronically hypertensive rats. Sobey, C.G., Heistad, D.D., Faraci, F.M. Stroke (1997) [Pubmed]
  5. Comparison of effects of aprikalim and of hypoxic and ischaemic preconditioning on extracellular potassium accumulation, metabolism, and functional recovery of the globally ischaemic rat heart. Guo, A.C., Diacono, J., Feuvray, D. Cardiovasc. Res. (1994) [Pubmed]
  6. Contributory mechanisms for the beneficial effects of myocyte preconditioning during cardioplegic arrest. O, S.J., Zellner, J.L., Cox, M.H., Hebbar, L., Brothers, T.E., Mukherjee, R., Tempel, G.E., Dorman, B.H., Crawford, F.A., Spinale, F.G. Circulation (1996) [Pubmed]
  7. ATP-sensitive K+ channels mediate dilatation of cerebral arterioles during hypoxia. Taguchi, H., Heistad, D.D., Kitazono, T., Faraci, F.M. Circ. Res. (1994) [Pubmed]
  8. Effects of several potassium channel openers and glibenclamide on the uterus of the rat. Piper, I., Minshall, E., Downing, S.J., Hollingsworth, M., Sadraei, H. Br. J. Pharmacol. (1990) [Pubmed]
  9. Hyperpolarized cardiac arrest with a potassium-channel opener, aprikalim. Maskal, S.L., Cohen, N.M., Hsia, P.W., Wechsler, A.S., Damiano, R.J. J. Thorac. Cardiovasc. Surg. (1995) [Pubmed]
  10. Relationship of severity of myocardial stunning to ATP dependent potassium channel modulation. Warltier, D.C., Auchampach, J.A., Gross, G.J. Journal of cardiac surgery. (1993) [Pubmed]
  11. ATP gated potassium channels in acute myocardial hibernation and reperfusion. Offstad, J., Kirkebøen, K.A., Ilebekk, A., Downing, S.E. Cardiovasc. Res. (1994) [Pubmed]
  12. Inhibition of vasoconstriction by potassium channel opener aprikalim in human conduit arteries used as bypass grafts. He, G.W., Yang, C.Q. British journal of clinical pharmacology. (1997) [Pubmed]
  13. Aprikalim: radioimmunoassay and pharmacokinetic studies in mouse, monkey, and dog. Chevalier, P., Rouillard, C., Montay, G., Frydman, A. Journal of pharmaceutical sciences. (1994) [Pubmed]
  14. Elective cardiac arrest with a hyperpolarizing adenosine triphosphate-sensitive potassium channel opener. A novel form of myocardial protection? Cohen, N.M., Wise, R.M., Wechsler, A.S., Damiano, R.J. J. Thorac. Cardiovasc. Surg. (1993) [Pubmed]
  15. Apparent competition between ATP and the potassium channel opener RP 49356 on ATP-sensitive K+ channels of cardiac myocytes. Thuringer, D., Escande, D. Mol. Pharmacol. (1989) [Pubmed]
  16. RP 49356 and cromakalim relax airway smooth muscle in vitro by opening a sulphonylurea-sensitive K+ channel: a comparison with nifedipine. Raeburn, D., Brown, T.J. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  17. The new K+ channel opener Aprikalim (RP 52891) reduces experimental infarct size in dogs in the absence of hemodynamic changes. Auchampach, J.A., Maruyama, M., Cavero, I., Gross, G.J. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  18. Effects of P1060 and aprikalim on whole-cell currents in rat portal vein; inhibition by glibenclamide and phentolamine. Ibbotson, T., Edwards, G., Noack, T., Weston, A.H. Br. J. Pharmacol. (1993) [Pubmed]
  19. Anti-ischaemic actions of potassium channel openers in experimental myocardial ischaemia/reperfusion injury in dogs. Auchampach, J.A., Gross, G.J. Eur. Heart J. (1993) [Pubmed]
  20. Cellular pharmacology of potassium channel openers in vascular smooth muscle. Quast, U., Guillon, J.M., Cavero, I. Cardiovasc. Res. (1994) [Pubmed]
  21. Effects of the K+ channel activators, RP 52891, cromakalim and diazoxide, on the plasma insulin level, plasma renin activity and blood pressure in rats. Pratz, J., Mondot, S., Montier, F., Cavero, I. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  22. Effects of two K+ channel openers, aprikalim and pinacidil, on hypoxic pulmonary vasoconstriction. Dumas, J.P., Dumas, M., Sgro, C., Advenier, C., Giudicelli, J.F. Eur. J. Pharmacol. (1994) [Pubmed]
  23. Aprikalim reduces the Na+-Ca2+ exchange outward current enhanced by hyperkalemia in rat ventricular myocytes. Li, H.Y., Wu, S., He, G.W., Wong, T.M. Ann. Thorac. Surg. (2002) [Pubmed]
  24. Global ischemia impairs ATP-sensitive K+ channel function in cerebral arterioles in piglets. Bari, F., Louis, T.M., Meng, W., Busija, D.W. Stroke (1996) [Pubmed]
  25. Nicorandil: differential contribution of K+ channel opening and guanylate cyclase stimulation to its vasorelaxant effects on various endothelin-1-contracted arterial preparations. Comparison to aprikalim (RP 52891) and nitroglycerin. Borg, C., Mondot, S., Mestre, M., Cavero, I. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  26. Effects of potassium channel opener aprikalim on the receptor-mediated vasoconstriction in the human internal mammary artery. Liu, M.H., Floten, H.S., Furnary, A.P., Yim, A.P., He, G.W. Ann. Thorac. Surg. (2001) [Pubmed]
  27. Two different types of potassium channels in human skeletal muscle activated by potassium channel openers. Quasthoff, S., Franke, C., Hatt, H., Richter-Turtur, M. Neurosci. Lett. (1990) [Pubmed]
  28. The myocardial lesions produced by the potassium channel opener aprikalim in monkeys and rats are prevented by blockade of cardiac beta-adrenoceptors. Belin, V., Hodge, T., Picaut, P., Jordan, R., Algate, C., Gosselin, S., Nohynek, G., Cavero, I. Fundamental and applied toxicology : official journal of the Society of Toxicology. (1996) [Pubmed]
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