Effects of amiloride on potassium and calcium currents in guinea pig ventricular myocytes / 药学学报

<p><b>AIM</b>To elucidate the possible mechanisms underlying antiarrhythmia of the non-selective Na+/H+ exchanger inhibitor--amiloride.</p><p><b>METHODS</b>Single ventricular cells were isolated using a double-enzyme method. Effects of amiloride on voltage-dependent potassium and calcium currents in isolated guinea pig ventricular myocyte were recorded by using whole-cell patch clamp techniques.</p><p><b>RESULTS</b>Exposure to amiloride (10 -100 micromol x L(-1)), the L-type and T-type calcium currents were depressed. Amiloride resulted in a concentration-dependent inhibition of peak (Ca,L), But amiloride did not change the shape of their I - V curves. It only decreased the amplitudes of the currents of the two types. When myocytes were incubated with 100 micromol x L(-1) amiloride, I(Kr) was slightly depressed and I(Ks) did not change. Amiloride (1 - 100 micromol x L(-10) depressed I(K1) in a concentration-dependent manner.</p><p><b>CONCLUSION</b>Amiloride depressed potassium and calcium currents, which may give support to its uses in some diseases of the cardiovascular system.</p>

Effect of ouabain on the aortic rings of guinea pig and its interactions with Ca2+, norepinephrine / 药学学报

<p><b>AIM</b>To observe the effects of ouabain on vascular smooth muscle (VSM) of the guinea pig and its interactions with Ca2+ and norepinephrine (NE).</p><p><b>METHODS</b>Using isolated thoracic aortic ring of the guinea pig, the degrees of contractile activity of drugs were recorded.</p><p><b>RESULTS</b>Ouabain showed a direct contractile effect in a concentration-dependent manner on thoracic aortic ring of guinea pig. Ouabain shifted the NE dose-response curve to the left without changing in the maxium response. Ouabain shifted the CaCl2 dose-response curve to the left and upward, increased the maximum response to Ca2+; In Ca(2+)-free medium, the ouabain induced contraction was abolished, an increase in extracellular Ca2+ restored the response; nifedipine and verapamil abolished the ouabain induced contraction.</p><p><b>CONCLUSION</b>The ouabain induced contraction is mainly dependent on the extracellular Ca2+ concentration, independent on the presence of endothelia of aorta, suggesting that Ca2+ antagonist may treat the hypertension induced by ouabain. Ouabain, NE and CaCl2 have synergetic contractile effects, suggesting that the synergetic contractile effects of ouabain and NE may contribute to the generation and development of hypertension.</p>

Effects of Rbl on action potentials and force of contraction in guinea pig ventricular papillary muscles / 中国中药杂志

<p><b>OBJECTIVE</b>To evaluate the effects of Rbl on action potentials and force of contraction in guinea pig ventricular papillary muscles.</p><p><b>METHOD</b>The ventricular papillary muscles of guinea pig were isolated regularly and immersed with Tyrode, s solution. The effects of Rbl (purified saponins of panaxnotoginseng) on the action potentials (AP), the slow action potentials and the force of contraction (FC) of the muscles were studied. The AP and FC were measured synchronously.</p><p><b>RESULT</b>Rbl shortened the duration of AP, including APD2O and APD90, and reduced the FC(n = 5, P < 0.01), but didn't affect the rest potential (RP), the amplitude of action potential (APA), overshot (OS) and maximal upstrok velocity (Vmax). Rbl also decreased the APA of slow action potential, but quinidine had no such effects.</p><p><b>CONCLUSION</b>Rbl may be a channel blocker.</p>

Modulation of protein kinase A and protein kinase C on the delayed rectifier potassium current in guinea pig ventricular myocytes / 中国应用生理学杂志

<p><b>AIM</b>To study modulation of protein kinase A (PKA) and protein kinase C (PKC) on the delayed rectifier potassium current (Ik)in guinea pig ventricular myocytes.</p><p><b>METHODS</b>The delayed rectifier potassium current was recorded by using whole cell arrangement of the patch-clamp procedure.</p><p><b>RESULTS</b>cAMP 150 micromol/L increased intracellularly Ik and Ik,tail(pA/pF) from 13.7 +/- 2.1 and 6.1 +/- 0.1 to 18.5 +/- 3.3 and 6.4 +/- 2.1 (P < 0.01, n=6). Ik and Ik,tail(pA/pF) were augmented by 8-CPT-cAMP 150 micromol/L extracellularly from 11.4 +/- 1.8 and 5.3 +/- 0.6 to 17.9 +/- 4.0 and 6.2 +/- 1.3. The half-maximal voltage of activation of Ik was shifted from + 23.3 mV to 18.7 mV by cAMP. Phorbol 12-myristate 13-acetate(PMA, 10.0 micromol/L) applied intracellularly caused an enhance effect on Ik, with increasing Ik and Ik,tail(pA/pF) from 12.9 +/- 1.8 and 5.0 +/- 1.7 to 23.7 +/- 2.8 and 7.5 +/- 1.1. With shifting position potential of depolarization, effect of PMA on Ik was gradually augmented. PMA resulted in shifting the slop of activation curve from +15.3 mV to +25.6 mV, with only a small effect on the half-maximal voltage of activation of Ik.</p><p><b>CONCLUSION</b>Ik was increased by both PKA and PKC, with different characteristics of regulation.</p>

Effects of benzyltetrahydropalmatine on the rapidly activating component of delayed rectifier potassium current in guinea pig ventricular myocytes / 药学学报

<p><b>AIM</b>To investigate the effect of benzyltetrahydropalmatine (BTHP) on the rapidly activating component of delayed rectifier K+ current (Ikr) in single guinea pig ventricular myocytes.</p><p><b>METHODS</b>Whole-cell patch clamp technique was used to record Ikr.</p><p><b>RESULTS</b>Ikr was blocked by 1-100 mumol.L-1 BTHP in concentration-, voltage-, and specifically frequency-dependent fashion, with IC50 of 13.5 mumol.L-1 (95% confidence range: 11.2-15.8 mumol.L-1). 30 mumol.L-1 BTHP reduced Ikr and Ikr.tail by (31 +/- 4)% and (36 +/- 5)% (n = 6, P < 0.01), respectively. The time constant for deactivation (tau') of the tail current was decreased by 30 mumol.L-1 BTHP from (238 +/- 16) ms to (196 +/- 14) ms, while drug had no any effect on the time constant for activation (tau) of Ikr,tail.</p><p><b>CONCLUSION</b>BTHP inhibited Ikr in a frequency-dependent fashion.</p>