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char = c;code = 99
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char = d;code = 100
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char = a;code = 97
char = t;code = 116
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result sql = Concentration-dependent (10-1000 microM) effects of terpenoid phenol derivatives were studied on L-type Ca(2+) current in isolated canine and human ventricular cardiomyocytes using the whole-cell configuration of patch clamp technique. Carvacrol, thymol and eugenol suppressed peak Ca(2+) current at +5 mV, having EC(50) values and Hill coefficients of 98+/-11, 158+/-7 and 187+/-15 microM and 1.42+/-0.05, 2.96+/-0.43 and 1.6+/-0.1, respectively, in canine myocytes. Zingerone displayed a weak effect (estimated EC(50): 2+/-0.37 mM, HILL COEFFICIENT: 0.73+/-0.07), while vanillin and guaiacol failed to substantially modify Ca(2+) current up to the concentration of 1 mM. In addition to tonic block, thymol and carvacrol, but not eugenol, evoked marked rate-dependent block at 2 Hz. Carvacrol and eugenol accelerated inactivation of Ca(2+) current and caused leftward shift in the voltage dependence of steady-state inactivation without altering activation kinetics. Carvacrol, but not eugenol, increased the time constant of recovery from inactivation. These effects of carvacrol and eugenol developed rapidly and were largely reversible. In myocytes isolated from undiseased human hearts, the effect of carvacrol was similar to that observed in canine cells. It is concluded that suppression of cardiac Ca(2+) currents by phenol derivatives is influenced by the substituent in the benzene ring, and the blocking effect of these drugs may involve interactions with the inactivation machinery of the channel.
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char = f;code = 102
char = ;code = 32
char = t;code = 116
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char = p;code = 112
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char = h;code = 104
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char = d;code = 100
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result sql = Effects of terpenoid phenol derivatives on calcium current in canine and human ventricular cardiomyocytes.
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char = l;code = 108
char = ;code = 32
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char = r;code = 114
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char = v;code = 118
char = a;code = 97
char = t;code = 116
char = i;code = 105
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char = e;code = 101
char = s;code = 115
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char = w;code = 119
char = e;code = 101
char = r;code = 114
char = e;code = 101
char = ;code = 32
char = s;code = 115
char = t;code = 116
char = u;code = 117
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char = i;code = 105
char = e;code = 101
char = d;code = 100
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char = ;code = 32
char = L;code = 76
char = -;code = 45
char = t;code = 116
char = y;code = 121
char = p;code = 112
char = e;code = 101
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char = C;code = 67
char = a;code = 97
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char = 2;code = 50
char = +;code = 43
char = );code = 41
char = ;code = 32
char = c;code = 99
char = u;code = 117
char = r;code = 114
char = r;code = 114
char = e;code = 101
char = n;code = 110
char = t;code = 116
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char = i;code = 105
char = n;code = 110
char = ;code = 32
char = i;code = 105
char = s;code = 115
char = o;code = 111
char = l;code = 108
char = a;code = 97
char = t;code = 116
char = e;code = 101
char = d;code = 100
char = ;code = 32
char = c;code = 99
char = a;code = 97
char = n;code = 110
char = i;code = 105
char = n;code = 110
char = e;code = 101
char = ;code = 32
char = a;code = 97
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char = d;code = 100
char = ;code = 32
char = h;code = 104
char = u;code = 117
char = m;code = 109
char = a;code = 97
char = n;code = 110
char = ;code = 32
char = v;code = 118
char = e;code = 101
char = n;code = 110
char = t;code = 116
char = r;code = 114
char = i;code = 105
char = c;code = 99
char = u;code = 117
char = l;code = 108
char = a;code = 97
char = r;code = 114
char = ;code = 32
char = c;code = 99
char = a;code = 97
char = r;code = 114
char = d;code = 100
char = i;code = 105
char = o;code = 111
char = m;code = 109
char = y;code = 121
char = o;code = 111
char = c;code = 99
char = y;code = 121
char = t;code = 116
char = e;code = 101
char = s;code = 115
char = ;code = 32
char = u;code = 117
char = s;code = 115
char = i;code = 105
char = n;code = 110
char = g;code = 103
char = ;code = 32
char = t;code = 116
char = h;code = 104
char = e;code = 101
char = ;code = 32
char = w;code = 119
char = h;code = 104
char = o;code = 111
char = l;code = 108
char = e;code = 101
char = -;code = 45
char = c;code = 99
char = e;code = 101
char = l;code = 108
char = l;code = 108
char = ;code = 32
char = c;code = 99
char = o;code = 111
char = n;code = 110
char = f;code = 102
char = i;code = 105
char = g;code = 103
char = u;code = 117
char = r;code = 114
char = a;code = 97
char = t;code = 116
char = i;code = 105
char = o;code = 111
char = n;code = 110
char = ;code = 32
char = o;code = 111
char = f;code = 102
char = ;code = 32
char = p;code = 112
char = a;code = 97
char = t;code = 116
char = c;code = 99
char = h;code = 104
char = ;code = 32
char = c;code = 99
char = l;code = 108
char = a;code = 97
char = m;code = 109
char = p;code = 112
char = ;code = 32
char = t;code = 116
char = e;code = 101
char = c;code = 99
char = h;code = 104
char = n;code = 110
char = i;code = 105
char = q;code = 113
char = u;code = 117
char = e;code = 101
char = .;code = 46
char = ;code = 32
char = C;code = 67
char = a;code = 97
char = r;code = 114
char = v;code = 118
char = a;code = 97
char = c;code = 99
char = r;code = 114
char = o;code = 111
char = l;code = 108
char = ,;code = 44
char = ;code = 32
char = t;code = 116
char = h;code = 104
char = y;code = 121
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char = o;code = 111
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char = ;code = 32
char = a;code = 97
char = n;code = 110
char = d;code = 100
char = ;code = 32
char = e;code = 101
char = u;code = 117
char = g;code = 103
char = e;code = 101
char = n;code = 110
char = o;code = 111
char = l;code = 108
char = ;code = 32
char = s;code = 115
char = u;code = 117
char = p;code = 112
char = p;code = 112
char = r;code = 114
char = e;code = 101
char = s;code = 115
char = s;code = 115
char = e;code = 101
char = d;code = 100
char = ;code = 32
char = p;code = 112
char = e;code = 101
char = a;code = 97
char = k;code = 107
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char = C;code = 67
char = a;code = 97
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char = 2;code = 50
char = +;code = 43
char = );code = 41
char = ;code = 32
char = c;code = 99
char = u;code = 117
char = r;code = 114
char = r;code = 114
char = e;code = 101
char = n;code = 110
char = t;code = 116
char = ;code = 32
char = a;code = 97
char = t;code = 116
char = ;code = 32
char = +;code = 43
char = 5;code = 53
char = ;code = 32
char = m;code = 109
char = V;code = 86
char = ,;code = 44
char = ;code = 32
char = h;code = 104
char = a;code = 97
char = v;code = 118
char = i;code = 105
char = n;code = 110
char = g;code = 103
char = ;code = 32
char = E;code = 69
char = C;code = 67
char = (;code = 40
char = 5;code = 53
char = 0;code = 48
char = );code = 41
char = ;code = 32
char = v;code = 118
char = a;code = 97
char = l;code = 108
char = u;code = 117
char = e;code = 101
char = s;code = 115
char = ;code = 32
char = a;code = 97
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char = d;code = 100
char = ;code = 32
char = H;code = 72
char = i;code = 105
char = l;code = 108
char = l;code = 108
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char = c;code = 99
char = o;code = 111
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char = f;code = 102
char = f;code = 102
char = i;code = 105
char = c;code = 99
char = i;code = 105
char = e;code = 101
char = n;code = 110
char = t;code = 116
char = s;code = 115
char = ;code = 32
char = o;code = 111
char = f;code = 102
char = ;code = 32
char = 9;code = 57
char = 8;code = 56
char = +;code = 43
char = /;code = 47
char = -;code = 45
char = 1;code = 49
char = 1;code = 49
char = ,;code = 44
char = ;code = 32
char = 1;code = 49
char = 5;code = 53
char = 8;code = 56
char = +;code = 43
char = /;code = 47
char = -;code = 45
char = 7;code = 55
char = ;code = 32
char = a;code = 97
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char = d;code = 100
char = ;code = 32
char = 1;code = 49
char = 8;code = 56
char = 7;code = 55
char = +;code = 43
char = /;code = 47
char = -;code = 45
char = 1;code = 49
char = 5;code = 53
char = ;code = 32
char = m;code = 109
char = i;code = 105
char = c;code = 99
char = r;code = 114
char = o;code = 111
char = M;code = 77
char = ;code = 32
char = a;code = 97
char = n;code = 110
char = d;code = 100
char = ;code = 32
char = 1;code = 49
char = .;code = 46
char = 4;code = 52
char = 2;code = 50
char = +;code = 43
char = /;code = 47
char = -;code = 45
char = 0;code = 48
char = .;code = 46
char = 0;code = 48
char = 5;code = 53
char = ,;code = 44
char = ;code = 32
char = 2;code = 50
char = .;code = 46
char = 9;code = 57
char = 6;code = 54
char = +;code = 43
char = /;code = 47
char = -;code = 45
char = 0;code = 48
char = .;code = 46
char = 4;code = 52
char = 3;code = 51
char = ;code = 32
char = a;code = 97
char = n;code = 110
char = d;code = 100
char = ;code = 32
char = 1;code = 49
char = .;code = 46
char = 6;code = 54
char = +;code = 43
char = /;code = 47
char = -;code = 45
char = 0;code = 48
char = .;code = 46
char = 1;code = 49
char = ,;code = 44
char = ;code = 32
char = r;code = 114
char = e;code = 101
char = s;code = 115
char = p;code = 112
char = e;code = 101
char = c;code = 99
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char = v;code = 118
char = e;code = 101
char = l;code = 108
char = y;code = 121
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char = i;code = 105
char = n;code = 110
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char = c;code = 99
char = a;code = 97
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char = n;code = 110
char = e;code = 101
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char = m;code = 109
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char = o;code = 111
char = c;code = 99
char = y;code = 121
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char = n;code = 110
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char = d;code = 100
char = i;code = 105
char = s;code = 115
char = p;code = 112
char = l;code = 108
char = a;code = 97
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char = e;code = 101
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char = ;code = 32
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char = w;code = 119
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char = a;code = 97
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char = e;code = 101
char = f;code = 102
char = f;code = 102
char = e;code = 101
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char = a;code = 97
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char = e;code = 101
char = d;code = 100
char = ;code = 32
char = E;code = 69
char = C;code = 67
char = (;code = 40
char = 5;code = 53
char = 0;code = 48
char = );code = 41
char = :;code = 58
char = ;code = 32
char = 2;code = 50
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char = -;code = 45
char = 0;code = 48
char = .;code = 46
char = 3;code = 51
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char = m;code = 109
char = M;code = 77
char = ,;code = 44
char = ;code = 32
char = <;code = 60
char = b;code = 98
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char = H;code = 72
char = I;code = 73
char = L;code = 76
char = L;code = 76
char = ;code = 32
char = C;code = 67
char = O;code = 79
char = E;code = 69
char = F;code = 70
char = F;code = 70
char = I;code = 73
char = C;code = 67
char = I;code = 73
char = E;code = 69
char = N;code = 78
char = T;code = 84
char = :;code = 58
char = ;code = 32
char = <;code = 60
char = /;code = 47
char = b;code = 98
char = >;code = 62
char = ;code = 32
char = 0;code = 48
char = .;code = 46
char = 7;code = 55
char = 3;code = 51
char = +;code = 43
char = /;code = 47
char = -;code = 45
char = 0;code = 48
char = .;code = 46
char = 0;code = 48
char = 7;code = 55
char = );code = 41
char = ,;code = 44
char = ;code = 32
char = w;code = 119
char = h;code = 104
char = i;code = 105
char = l;code = 108
char = e;code = 101
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char = v;code = 118
char = a;code = 97
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char = l;code = 108
char = i;code = 105
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char = a;code = 97
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char = d;code = 100
char = ;code = 32
char = g;code = 103
char = u;code = 117
char = a;code = 97
char = i;code = 105
char = a;code = 97
char = c;code = 99
char = o;code = 111
char = l;code = 108
char = ;code = 32
char = f;code = 102
char = a;code = 97
char = i;code = 105
char = l;code = 108
char = e;code = 101
char = d;code = 100
char = ;code = 32
char = t;code = 116
char = o;code = 111
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char = s;code = 115
char = u;code = 117
char = b;code = 98
char = s;code = 115
char = t;code = 116
char = a;code = 97
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char = i;code = 105
char = a;code = 97
char = l;code = 108
char = l;code = 108
char = y;code = 121
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char = m;code = 109
char = o;code = 111
char = d;code = 100
char = i;code = 105
char = f;code = 102
char = y;code = 121
char = ;code = 32
char = C;code = 67
char = a;code = 97
char = (;code = 40
char = 2;code = 50
char = +;code = 43
char = );code = 41
char = ;code = 32
char = c;code = 99
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char = r;code = 114
char = r;code = 114
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char = n;code = 110
char = t;code = 116
char = ;code = 32
char = u;code = 117
char = p;code = 112
char = ;code = 32
char = t;code = 116
char = o;code = 111
char = ;code = 32
char = t;code = 116
char = h;code = 104
char = e;code = 101
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char = c;code = 99
char = o;code = 111
char = n;code = 110
char = c;code = 99
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char = n;code = 110
char = t;code = 116
char = r;code = 114
char = a;code = 97
char = t;code = 116
char = i;code = 105
char = o;code = 111
char = n;code = 110
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char = o;code = 111
char = f;code = 102
char = ;code = 32
char = 1;code = 49
char = ;code = 32
char = m;code = 109
char = M;code = 77
char = .;code = 46
char = ;code = 32
char = I;code = 73
char = n;code = 110
char = ;code = 32
char = a;code = 97
char = d;code = 100
char = d;code = 100
char = i;code = 105
char = t;code = 116
char = i;code = 105
char = o;code = 111
char = n;code = 110
char = ;code = 32
char = t;code = 116
char = o;code = 111
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char = t;code = 116
char = o;code = 111
char = n;code = 110
char = i;code = 105
char = c;code = 99
char = ;code = 32
char = b;code = 98
char = l;code = 108
char = o;code = 111
char = c;code = 99
char = k;code = 107
char = ,;code = 44
char = ;code = 32
char = t;code = 116
char = h;code = 104
char = y;code = 121
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char = o;code = 111
char = l;code = 108
char = ;code = 32
char = a;code = 97
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char = d;code = 100
char = ;code = 32
char = c;code = 99
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char = v;code = 118
char = a;code = 97
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char = l;code = 108
char = ,;code = 44
char = ;code = 32
char = b;code = 98
char = u;code = 117
char = t;code = 116
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char = n;code = 110
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char = t;code = 116
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char = e;code = 101
char = u;code = 117
char = g;code = 103
char = e;code = 101
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char = o;code = 111
char = c;code = 99
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char = a;code = 97
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char = 2;code = 50
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char = H;code = 72
char = z;code = 122
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char = ;code = 32
char = C;code = 67
char = a;code = 97
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char = v;code = 118
char = a;code = 97
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char = a;code = 97
char = c;code = 99
char = c;code = 99
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char = r;code = 114
char = a;code = 97
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char = i;code = 105
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char = i;code = 105
char = o;code = 111
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char = o;code = 111
char = f;code = 102
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char = C;code = 67
char = a;code = 97
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char = 2;code = 50
char = +;code = 43
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char = a;code = 97
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char = d;code = 100
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char = s;code = 115
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char = d;code = 100
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char = l;code = 108
char = e;code = 101
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char = t;code = 116
char = w;code = 119
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char = s;code = 115
char = h;code = 104
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char = v;code = 118
char = o;code = 111
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char = a;code = 97
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char = o;code = 111
char = f;code = 102
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char = s;code = 115
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char = e;code = 101
char = a;code = 97
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char = y;code = 121
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char = e;code = 101
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char = o;code = 111
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char = w;code = 119
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char = t;code = 116
char = h;code = 104
char = o;code = 111
char = u;code = 117
char = t;code = 116
char = ;code = 32
char = a;code = 97
char = l;code = 108
char = t;code = 116
char = e;code = 101
char = r;code = 114
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char = n;code = 110
char = g;code = 103
char = ;code = 32
char = a;code = 97
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char = t;code = 116
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char = v;code = 118
char = a;code = 97
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char = i;code = 105
char = o;code = 111
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char = k;code = 107
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char = n;code = 110
char = e;code = 101
char = t;code = 116
char = i;code = 105
char = c;code = 99
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char = .;code = 46
char = ;code = 32
char = C;code = 67
char = a;code = 97
char = r;code = 114
char = v;code = 118
char = a;code = 97
char = c;code = 99
char = r;code = 114
char = o;code = 111
char = l;code = 108
char = ,;code = 44
char = ;code = 32
char = b;code = 98
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char = c;code = 99
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char = t;code = 116
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char = p;code = 112
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char = ;code = 32
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result sql = Concentration-dependent (10-1000 microM) effects of terpenoid phenol derivatives were studied on L-type Ca(2+) current in isolated canine and human ventricular cardiomyocytes using the whole-cell configuration of patch clamp technique. Carvacrol, thymol and eugenol suppressed peak Ca(2+) current at +5 mV, having EC(50) values and Hill coefficients of 98+/-11, 158+/-7 and 187+/-15 microM and 1.42+/-0.05, 2.96+/-0.43 and 1.6+/-0.1, respectively, in canine myocytes. Zingerone displayed a weak effect (estimated EC(50): 2+/-0.37 mM, HILL COEFFICIENT: 0.73+/-0.07), while vanillin and guaiacol failed to substantially modify Ca(2+) current up to the concentration of 1 mM. In addition to tonic block, thymol and carvacrol, but not eugenol, evoked marked rate-dependent block at 2 Hz. Carvacrol and eugenol accelerated inactivation of Ca(2+) current and caused leftward shift in the voltage dependence of steady-state inactivation without altering activation kinetics. Carvacrol, but not eugenol, increased the time constant of recovery from inactivation. These effects of carvacrol and eugenol developed rapidly and were largely reversible. In myocytes isolated from undiseased human hearts, the effect of carvacrol was similar to that observed in canine cells. It is concluded that suppression of cardiac Ca(2+) currents by phenol derivatives is influenced by the substituent in the benzene ring, and the blocking effect of these drugs may involve interactions with the inactivation machinery of the channel.
Publication: Eur. J. Pharmacol. 2004 Mar 8 ;487(1-3)::29-36.
Publication Date: 2004 Mar 8
Study Author(s): Magyar, János;Szentandrássy, Norbert;Bányász, Tamás;Fülöp, László;Varró, András;Nánási, Péter P;
Institution: Department of Physiology, University Medical School of Debrecen, P.O. Box 22, H-4012 Debrecen, Hungary.
Shortcut link to this study:
Publication Date: 2004 Mar 8
Study Author(s): Magyar, János;Szentandrássy, Norbert;Bányász, Tamás;Fülöp, László;Varró, András;Nánási, Péter P;
Institution: Department of Physiology, University Medical School of Debrecen, P.O. Box 22, H-4012 Debrecen, Hungary.
Shortcut link to this study:
Concentration-dependent (10-1000 microM) effects of terpenoid phenol derivatives were studied on L-type Ca(2+) current in isolated canine and human ventricular cardiomyocytes using the whole-cell configuration of patch clamp technique. Carvacrol, thymol and eugenol suppressed peak Ca(2+) current at +5 mV, having EC(50) values and Hill coefficients of 98+/-11, 158+/-7 and 187+/-15 microM and 1.42+/-0.05, 2.96+/-0.43 and 1.6+/-0.1, respectively, in canine myocytes. Zingerone displayed a weak effect (estimated EC(50): 2+/-0.37 mM, HILL COEFFICIENT: 0.73+/-0.07), while vanillin and guaiacol failed to substantially modify Ca(2+) current up to the concentration of 1 mM. In addition to tonic block, thymol and carvacrol, but not eugenol, evoked marked rate-dependent block at 2 Hz. Carvacrol and eugenol accelerated inactivation of Ca(2+) current and caused leftward shift in the voltage dependence of steady-state inactivation without altering activation kinetics. Carvacrol, but not eugenol, increased the time constant of recovery from inactivation. These effects of carvacrol and eugenol developed rapidly and were largely reversible. In myocytes isolated from undiseased human hearts, the effect of carvacrol was similar to that observed in canine cells. It is concluded that suppression of cardiac Ca(2+) currents by phenol derivatives is influenced by the substituent in the benzene ring, and the blocking effect of these drugs may involve interactions with the inactivation machinery of the channel.
PMID: 15033373
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