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For use dependence of the channel, the percent of current remaining was the peak current amplitude of the initial pulse divided by that of the fifth pulse.
Our structures also provide insight into the structural basis of closed-state blockade, use dependence of blockade, and drug trapping.
A simple two-test pulse protocol (Fig. 3A ) demonstrated the use dependence of Cav1.2 inhibition with verapamil; the inhibitory potency detected by the second test pulse (TP2) was 3.5-times greater than that produced during the first test pulse (TP1).
For example, in patients with diminished LV function, during exercise there may be (sub acute worsening of congestive heart failure, possibly due to use dependence of class I drugs.
However, our Cav3.2 IC50 value obtained with −90 mV prepulse (Table 4 ) was approximately sixfold higher than that reported by Martin et al. The use dependence of mibefradil may account for this discrepancy.
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A rabbit isolated heart model (SCREENIT) has been reported to identify compounds with proarrhythmic potential based on the observance of compound-induced triangulation and instability of the monophasic action potential (MAP), ectopic beats, and reverse-use dependence of prolongation of the MAP duration.
These data are obtained by numerical optimalization of the electrical three layer model, using dependence of surface charge density versus pH.
Interestingly, use-dependence of eCBmGluR reduction was seen when PLC, rather than DAGL, was inhibited, supporting the concept that the DAGLα-PLC pathway is upstream of the depletable source of 2-AG for eCBmGluR.
The use-dependence of the reduction in eCBmGluR is puzzling, and while direct evidence is not available, one speculative scenario is intriguing: decoupling of 2-AG synthesis and release could partly account for the data.
Reverse use-dependence of APD is a physiological capacity of the healthy heart wherein the APD usually shortens at increasing heart rate.
Thank you for submitting your work entitled "The active-zone protein Munc13 controls the use-dependence of presynaptic voltage-gated calcium channels" for peer review at eLife.
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