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- W2883100811 abstract "Dantrolene protects cardiac muscle from arrhythmia and heart failure by inhibiting Ca2+ release from the sarcoplasmic reticulum (SR). Single-channel recordings were obtained from SR calcium release channels (RyR2) isolated from sheep and human heart and incorporated into artificial lipid bilayers. Dantrolene inhibition was measured by exposing RyR2 both in the absence and presence of exogenous 100 nM CaM. In diastolic cytoplasmic [Ca2+] (100 nM), dantrolene (50 μM) reduced the mean open probability of RyR2 to 45 ± 6% in the presence of CaM (n = 7, p<0.05, Student's paired t-test) but had no significant effect when CaM was absent (95 ± 9%, n = 20, p = 0.24). Dantrolene exhibited a hyperbolic dose response in the presence of CaM with an IC50 of 0.16 ± 0.03 μM and with a saturating relative Po (Emax) of 52 ± 4%. Emax increased to 1 as cytoplasmic Ca2+ was increased to levels >1 μM. In saponin-permeablised mouse cardiomyocytes supplemented with 100 nM CaM, dantrolene reduced the frequency and amplitude of Ca2+ waves, with an IC50 of 0.3 μM. However, when cells were depleted of CaM, dantrolene had no effect. Thus, CaM is essential for inhibitory action of dantrolene. Incubation of RyR2 to rapamycin prior to single-channel recording, known to dissociate FKBP12.6 from RyR2, removed the inhibitory action of dantrolene. This could be restored by adding FKBP12.6 to the bathing media. We conclude that the dantrolene inhibition required the presence of both CaM and FKBP12.6 in the RyR2 complex." @default.
- W2883100811 created "2018-08-03" @default.
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- W2883100811 date "2018-01-01" @default.
- W2883100811 modified "2023-10-02" @default.
- W2883100811 title "RyR2 Inhibition by Dantrolene Requires both Calmodulin and FKBP12.6" @default.
- W2883100811 doi "https://doi.org/10.1016/j.hlc.2018.06.334" @default.
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