Ryanodine-pretreated E4032A channels become responsive to RyR agonists.
(A) In an E4032A-expressing 1B5 myotube pretreated with
500 μM ryanodine for 30 min, responses to 40 mM KCl, 40 mM caffeine
and 0.5 mM 4-chloro-m-cresol are restored. (Bars =
0.05 340/380 units vs. 50 sec.) (B) The degree of
restoration of E4032A activity by ryanodine is indicated. A small
percentage of the total number of cells examined for changes in calcium
respond to RyR agonists in dishes containing untreated
E4032A-expresssing 1B5 cells (clear bar). Upon treatment with 500 μM
ryanodine for 24 h, the percentage of total cells responding to
each of the RyR agonists significantly increased (Black bars: *,
P < 0.001). (Inset):
E4032A-expressing 1B5 myotubes were incubated with increasing
concentrations of ryanodine for 24 h. The percentage of the total
number of cells examined that responded to 40 mM caffeine is plotted
vs. the ryanodine concentration used in the preincubation.
(C) Ryanodine restores skeletal-type
excitation–contraction coupling of E4032A. Addition of 40 mM KCl
(black bar) to an E4032A-expressing cell pretreated with 500 μM
ryanodine for 24 h produced calcium transients in both the
presence and absence of extracellular calcium, indicating a functional
interaction between RyR and DHPR. (Bar = 0.05 340/380 units vs.
60 sec.) (D) E4032A activity can be restored by
ryanodine in single-channel studies. Single-channel measurements of
E4032A channels reconstituted in BLM were conducted as described in
Materials and Methods. E4032A channels isolated from 1B5
cells pretreated for 24 h with 200 μM ryanodine are active at 7
μM calcium cis (upper trace). Of 15 channels reconstituted, all
exhibited substate behavior approximating 3/4, 1/2, and 1/4
transitions whose frequency of occurrence were approximately the same.
Of these reconstitutions, 50% of the channels exhibited frequent
transitions to full open similar to wt. For the channel shown, the open
probability for transitions from closed to 1/4 state (dashed line)
and 1/4 state to fully open were 0.83 and 0.028, respectively. In
E4032A channels pretreated with ryanodine, channel activity depended on
the level of calcium in the cis chamber of the bilayer, since lowering
the level of calcium to 3.4 nM (≈1 min before recording) fully
inactivated the channel (lower trace).