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F15845
F15845 (3-(R)-()amino-3,4-dihydro-2H-1,5 benzoxathiepine bromhydrate) is a cardiac drug proposed to have beneficial effects for the treatment of angina pectoris, arrhythmias and ischemia by inhibiting the persistent sodium current (Vacher et al., 2009; Pignier et al., 2010). The drug, currently in phase II of clinical trials, targets the persistent sodium current with selectivity and produces minimal adverse effects in current experimental studies (Vacher et al., 2009; Létienne et al. 2009; Vie et al. 2009; Pignier et al. 2010).
==Persistent sodium current==
In the cardiac myocyte, the persistent sodium current corresponds to the delayed inactivation of the major sodium channel Nav1.5 (Létienne et al. 2009). In a functional muscle cell, this sodium channel plays an important role in the propagation of an action potential through the heart. Sodium influx is a key component in the initial depolarisation of the cell, followed by quick inactivation to allow for a plateau phase and calcium influx (Vacher et al., 2009). Persistent sodium current prevents this normal action potential pattern, resulting in a prolonged action potential and increased sodium levels within the cardiac myocyte (Undrovinas et al., 1999). Under these conditions the heart is more susceptible to damage and malfunctions (Imahashi et al.,. 1999).
Inhibition of the persistent sodium current is a novel therapeutic target to prevent long term changes in the heart resulting from ischemia (Létienne et al. 2009; Vie et al. 2009). Hypoxia, heart failure and oxygen derived free radicals are all factors believed to activate the persistent sodium current (Vacher et al., 2009). In ischemia, the major damage to the cardiac myocyte, due to hypoxia, is seen following the reperfusion of blood (Vie et al.,. 2009). High intracellular sodium levels from the persistent current results in high influx of calcium during reperfusion; leading to calcium overload, hypercontraction and cardiac myocyte death (Vie et al., 2009). The main contributor to this calcium overload is the sodium/calcium exchanger working in reverse, driven by the high intracellular concentration of sodium exchanging out of the cell with the extracellular calcium moving in (Imahashi et al. 1999).
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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