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- W2000370931 abstract "1 In rabbit aorta, pretreatment with 2-aminoisoquinoline, 1.3 (2H.4H)-dione (AQ, 10−5 M and 10−4 M) shifted the concentration-response relationship to noradrenaline (NA, 10−9 M to 10−4 M) in a parallel manner whereas the agent (10−4 M) failed to affect the response to potassium and only slightly depressed Ca2+-induced contractions in a Ca2+-free medium in the presence of K+ (40 mM). 2 Ca2+-entry blockers such as nifedipine and diltiazem (10−6 M and 10−5 M) had very weak or no apparent effects on the response to NA but markedly attenuated or abolished the K+- and Ca2+-induced contractions. 3 Following incubation of tissues for 15 min in a Ca2+-free medium with low EGTA (0.01 mM) and methoxyverapamil (D600, 10−5 M), NA (3 × 10−7 M) caused a phasic (transient) contraction and the subsequent application of Ca2+ (2mM) resulted in a tonic contraction. This NA-induced, Ca2+-dependent, D600-insensitive contraction was inhibited by AQ (10−5 M and 10−4 M) in a concentration-dependent manner. This suggests that the inhibitory action of AQ may be related to Ca2+ entry through specific receptor activated pathways. 4 Following incubation of tissues for 30 min in a Ca2+-free medium with high EGTA (2.0 mM), NA (10−5 M) caused a contraction of rabbit aorta which is dependent upon release of intracellular Ca2+, but the response was 50% to 60% less than that in a normal medium. This contraction was inhibited by AQ (10−5 M and 10−4 M) and nitroglycerin (10−5 M) but not by nifedipine or diltiazem. The inhibitory action of combined treatment with AQ and nitroglycerin (10−5 M) on the response to NA was not different from that of either agent alone. 5 These results suggest that AQ may have inhibitory actions on the release of intracellular Ca2+ and also on Ca2+-entry through D600-insensitive, receptor-activated Ca2+ pathways in rabbit aorta." @default.
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- W2000370931 date "1986-02-01" @default.
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- W2000370931 title "The mode of vasorelaxant action of 2- aminoisoquinoline, 1.3 (2H.4H)-dione, a novel ‘intracellular calcium inhibitor’" @default.
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- W2000370931 doi "https://doi.org/10.1111/j.1476-5381.1986.tb10828.x" @default.
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