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Gasser R et al.  
Indiscriminative Effects of Repaglinide and Other Specific Modulators of Transmembrane KATP-Channel Gating Properties upon Ischaemic/Hypoxic Bovine Coronary Artery Smooth Muscle Relaxation

Journal of Clinical and Basic Cardiology 2003; 6 (1-4): 81-85

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Koronararterien - Muskelrelaxation
Figure 1a-b: A: Intrinsic relaxing activity of repaglinide in bovine coronary artery in percent of maximal contraction (obtained at the end of each experiment by the addition of 2.66 × 10–4 M papaverine). Strips stabilised in length within 90 min of incubation at about 60 % of maximal shortening; B: Intrinsic relaxing activity of glimepiride at different concentrations like in 1A.

Keywords: coronary arterydiagramDiagrammGlatte MuskulaturGlimepiridglimepirideKATP-channelKATP-KanalKoronararterieRelaxationRepaglinidRepaglinidesmooth muscle
Koronararterien - KATP-Kanalöffner-Hemmung
Figure 2a-b: Experiment like in Fig. 1A; repaglinide shows competitive inhibition of specific K channel openers (here shown: pinacidil).

Keywords: coronary arteryCromakalimCromakalimdiagramDiagrammHemmunginhibitionKATP-channelKATP-KanalKoronararteriePinacidilPinacidilRepaglinidRepaglinid
Koronararterien - Relaxation
Figure 3a-c: A: Relaxation of bovine coronary arteries during hypoxia (open symbols) and its reversibility by reoxygenation; glibenclamide (2 µM) inhibits hypoxic vasodilation; glibenclamide’s intrinsic relaxing activity can be seen in the reoxygenation curve in form of a slight diminution of recovery; B: Dose dependent inhibition by repaglinide of hypoxic vasodilation; C: Dose dependent inhibition by glimepiride of hypoxic vasodilation. The intrinsic relaxing activity of glimepiride can be seen in form of a 17 % initial relaxation of the arteries. This effect was not so pronounced with repaglinide (B).

Keywords: coronary arterydiagramDiagrammGlibenclamidglibenclamideGlimepiridglimepiridehypoxiaHypoxieKoronararterieRelaxationRelaxationRepaglinidRepaglinide
Koronararterien - Relaxation
Figure 4a-c: A: Dinitrophenole (1 mM), an uncoupler of oxidative phosphorylation invariably leads to vasodilation, the latter is partially inhibited by glibenclamide in a dose-dependent manner; B: Dose dependent inhibition of DNP-induced vasodilation; note repaglinide’s intrinsic relaxing activity at higher doses; the inhibition of relaxation is not as pronounced as with glimepiride and glibenclamide; C: Inhibition of DNP induced relaxation is maximal under 3 µM glimepiride; the effect of a similar dose of glibenclamide is also introduced in this figure in order to demonstrate the approximate equimolar inhibition; glimepiride is a stronger inhibitor of DNP-induced vasorelaxation than glibenclamide.

Keywords: coronary arterydiagramDiagrammGilbenclamidGilbenclamideGlimepiridglimepirideKoronararterierealxationRelaxationRepaglinidRepaglinide
Koronararterien - Relaxation
Figure 5a-c: A: Iodoacetic acid (IAA), an inhibitor of the glycolytic enzyme G3P-dehydrogenase leads to vasodilation; inhibition by glibenclamide, repaglinide and glimepiride (B) is insignificant; only a dose of 1 µM repaglinide is able to inhibit IAA-induced vasorelaxation after 10 min by 20 %.

Keywords: coronary arterydiagramDiagrammGlibenclamidglibenclamideGlimepiridglimepirideKoronararterieRelaxationRelaxationRepaglinidRepaglinide
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