Evaluation of GSK 2487213 A on [ 3 H ] Ryanodine Binding to RyR 1 . Final Report
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بررسی اثر مهار گیرنده رایانیدینی(RYR) بر فعالیت پیسمیکری
Background & Aim: The role of ryanodine receptor(RYR) on pacemaker activity of heart cells is controversial. Some investigators have suggested that it is obligatory, while others believe it is partial and not obligatory. The principle aim of this study was once more to characterize the role of ryanodine receptor(RyR) on the pacemaker activity of the sinoatrial node(SAN) and the atrioventric...
متن کاملThe interaction of an impermeant cation with the sheep cardiac RyR channel alters ryanoid association.
In previous studies, we have demonstrated that the interaction of ryanoids with the sarcoplasmic reticulum Ca(2+)-release channel [ryanodine receptor (RyR)] incorporated into planar lipid bilayers reduced the effectiveness of tetraethylammonium (TEA(+)) as a blocker of K(+) translocation (J Gen Physiol 117: 385-393, 2001). In the current study, we investigated both the effect of TEA(+) on [(3)H...
متن کاملRyanodine receptor/calcium release channel conformations as reflected in the different effects of propranolol on its ryanodine binding and channel activity.
1. Propranolol, a beta-blocker, inhibited or stimulated ryanodine binding to both the membrane-bound and purified ryanodine receptor (RyR) depending on the assay conditions. At high NaCl concentrations, propranolol increased the number of ryanodine-binding sites (Bmax) with no effect on the binding affinity. In the presence of 0.2 M NaCl, ryanodine binding was inhibited by propranolol. Half-max...
متن کاملAltered stoichiometry of FKBP12.6 versus ryanodine receptor as a cause of abnormal Ca(2+) leak through ryanodine receptor in heart failure.
BACKGROUND In the pathogenesis of cardiac dysfunction in heart failure, a decrease in the activity of the sarcoplasmic reticulum (SR) Ca(2+)-ATPase is believed to be a major determinant. Here, we report a novel mechanism of cardiac dysfunction revealed by assessing the functional interaction of FK506-binding protein (FKBP12.6) with the cardiac ryanodine receptor (RyR) in a canine model of pacin...
متن کاملTectoridins modulate skeletal and cardiac muscle sarcoplasmic reticulum calcium-release channels.
The isoflavones tectoridin (TTR) and 3'-hydroxy TTR (3'-TTR) were isolated from an Ayurvedic herbal preparation Vacä and evaluated for their affinity and effect on ryanodine receptors (RyR) using junctional sarcoplasmic reticulum vesicles (JSRVs). In [(3)H]ryanodine displacement binding affinity assays, TTR and 3'-TTR exhibited IC(50) values of 17.3 +/- 1.3 microM (K(d) = 6.7 +/- 0.4 microM) an...
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