Arginine-vasopressin induces mode-2 gating in L-type Ca2+ channels (smooth muscle cells of the urinary bladder of the guinea-pig).

The effect of arginine-vasopressin (AVP, 0.1 microM) on elementary Ca2+ channel currents (L-type) was studied in cell-attached patches with 10 mM BaCl2 as the charge carrier. At a constant potential of -30 mV, bath applied AVP increased the channel openness (NPo) by a factor of 4.7 +/- 3.0 (mean +/- SD, n = 9), the effect resulted from an increase in the frequency of opening (factor 2.5 +/- 0.8) and from a longer mean open time. Under control, openings longer than 5 ms contributed only 4% of the total, however, with the application of AVP this contribution increased to 29%. Under control, the open times were distributed along a single exponential (tau o1 = 0.8 +/- 0.4 ms), a double exponential distribution was obtained during AVP (tau o1 = 0.8 +/- 0.5 ms, tau o2 = 7.5 +/- 0.7 ms). The Ca2+ agonist BAYk8644 (1 microM) changed the open time distribution similarly to AVP (tau o1 = 1.0 +/- 0.5 ms, tau o2 = 9 +/- 2.8 ms). With 1 microM BAYk8644 in the bath, AVP did not significantly increase the relative contribution of long openings, however, AVP increased the frequency of openings by a factor of 2.0 +/- 1 (n = 6). The results are compatible with the idea that AVP can change the gating of L-type Ca2+ channels from mode 1 to mode 2.