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F90927: a new member in the class of cardioactive steroids Keller M; Pignier C; Egger M; Niggli ECardiovasc Drug Rev 2007[Fal]; 25 (3): 210-20F90927 is a newly developed cardioactive drug with a steroid-like structure. It acts directly and agonistically on the cardiac L-type Ca2+ channel by shifting its voltage-dependent activation toward more negative potentials. This leads to an increased influx of Ca2+ and, therefore, to a stronger contraction; however, no arrhythmias occur. Calcium current stimulation can already be observed at nanomolar concentrations, but higher concentrations of F90927 elevate intracellular Ca2+ concentration, causing a reduction of the myocardial compliance and an increased diastolic blood pressure. Vessels also react to F90927 and contract in its presence. Binding of F90927 with the L-type Ca2+ channel presumably occurs in the vicinity of the transmembrane domains III and IV of the alpha1 subunit. F90927 exhibits no use dependence and interacts with Ca2+ channel inhibitors of all three known classes of channel modulators (dihydropyridines, phenylalkylamines, and benzothiazepines), suggesting that it is a member of a new class of Ca2+ channel modulators. Due to its adverse effects on blood pressure and vessel contraction, F90927 is not an ideal drug candidate. It has, however, some unique properties, which makes it a promising tool to study the function of the L-type Ca2+ channel.|Animals[MESH]|Calcium Channels, L-Type/physiology[MESH]|Calcium/metabolism[MESH]|Cardiotonic Agents/chemistry/*pharmacology[MESH]|Estrone/*analogs & derivatives/chemistry/pharmacology[MESH]|Humans[MESH]|Membrane Potentials/drug effects[MESH]|Models, Biological[MESH]|Molecular Structure[MESH]|Myocytes, Cardiac/drug effects/metabolism/physiology[MESH] |
