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Excessive ATP hydrolysis in ischemic myocardium by mitochondrial F1F0-ATPase: effect of selective pharmacological inhibition of mitochondrial ATPase hydrolase activity.
Excessive ATP hydrolysis by F(1)F(0)-ATPase contributes to the decline in cardiac energy reserve during ischemia and selective inhibition of ATP hydrolase activity can protect ischemic myocardium. Expand
Triphenylphosphine oxide is a potent and selective inhibitor of the transient receptor potential melastatin-5 ion channel.
triphenylphosphine oxide (TPPO) is the most potent TRPM5 inhibitor described to date and is the first demonstrated to exhibit selectivity over other channels. Expand
Small molecule mitochondrial F1F0 ATPase hydrolase inhibitors as cardioprotective agents. Identification of 4-(N-arylimidazole)-substituted benzopyran derivatives as selective hydrolase inhibitors.
It is shown that 4-aryl-CH2-imidazole-substituted benzopyran compounds with 3S,4R-stereochemistry are cardioprotective by inhibiting the F1F0 mitochondrial ATP hydrolase by acting as mitochondrial KATP openers. Expand
Pharmacology and Structure‐Activity Relationships for KATP Modulators: Tissue‐Selective KATP Openers
  • K. Atwal
  • Chemistry, Medicine
  • Journal of cardiovascular pharmacology
  • 1994
It is demonstrated that no correlation exists between anti‐ischemic and smooth‐muscle relaxing potencies for a variety of structurally different KATP openers, and the discovery of tissue‐selective agents that may offer advantages over the first‐generation agents for the treatment of cardiovascular diseases is described. Expand
Nucleotide regulation and characteristics of potassium channel opener binding to skeletal muscle membranes.
In contrast, rose bengal and the ATP-regulated potassium channel antagonist glyburide increased the rate of [3H]P1075 dissociation in a manner consistent with noncompetitive interaction, and significant metabolism by membrane nucleotidases was confirmed by high performance liquid chromatographic analysis. Expand
Dihydropyrimidine calcium channel blockers. 2. 3-substituted-4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.
The results strengthen the requirement of an enamino ester for binding to the dihydropyridine receptor and indicate a nonspecific role for the N3-substituent. Expand
Cardioprotective Profile of the Cardiac‐Selective ATP‐Sensitive Potassium Channel Opener BMS‐180448
The identification of the arylcyanoguanidine analogue BMS-180448 provides the opportunity to explore the cardioprotective actions of this class of agents without the possible complications (hypotension, coronary steal) that may be caused by the currently available KATP openers. Expand
Dihydropyrimidine calcium channel blockers. 4. Basic 3-substituted-4-aryl-1,4-dihydropyrimidine-5-carboxylic acid esters. Potent antihypertensive agents.
Dihydropyrimidine 12a is both more potent and longer acting than nifedipine and compares most favorably with the long-acting dihydropyridine derivative amlodipine in vitro and has the potential advantage of being a single enantiomer in vivo. Expand
Cardioprotective effects of the potassium channel opener cromakalim: stereoselectivity and effects on myocardial adenine nucleotides.
It is significant that cromakalim can preserve adenine nucleotides despite its lack of negative inotropic effects and may be due partly to preservation of myocardial energy reserves. Expand
Pharmacologic characterization of BMS-191095, a mitochondrial K(ATP) opener with no peripheral vasodilator or cardiac action potential shortening activity.
The results show that the cardioprotective effects of BMS-191095 are dissociated from peripheral vasodilator and cardiac sarcolemmal K(ATP) activation. Expand