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result sql = An evaluation of the cytochrome P450 inhibition potential of selected pesticides in human hepatic microsomes.
An evaluation of the cytochrome P450 inhibition potential of selected pesticides in human hepatic microsomes.
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char = h;code = 104
char = a;code = 97
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char = e;code = 101
char = s;code = 115
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char = P;code = 80
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char = t;code = 116
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char = r;code = 114
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char = s;code = 115
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char = a;code = 97
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char = r;code = 114
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char = w;code = 119
char = e;code = 101
char = a;code = 97
char = k;code = 107
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char = o;code = 111
char = r;code = 114
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char = i;code = 105
char = n;code = 110
char = a;code = 97
char = c;code = 99
char = t;code = 116
char = i;code = 105
char = v;code = 118
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char = .;code = 46
char = ;code = 32
char = D;code = 68
char = e;code = 101
char = l;code = 108
char = t;code = 116
char = a;code = 97
char = m;code = 109
char = e;code = 101
char = t;code = 116
char = h;code = 104
char = r;code = 114
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char = n;code = 110
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char = a;code = 97
char = n;code = 110
char = d;code = 100
char = ;code = 32
char = f;code = 102
char = e;code = 101
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char = v;code = 118
char = a;code = 97
char = l;code = 108
char = e;code = 101
char = r;code = 114
char = a;code = 97
char = t;code = 116
char = e;code = 101
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char = w;code = 119
char = e;code = 101
char = r;code = 114
char = e;code = 101
char = ;code = 32
char = p;code = 112
char = o;code = 111
char = t;code = 116
char = e;code = 101
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char = t;code = 116
char = ;code = 32
char = i;code = 105
char = n;code = 110
char = h;code = 104
char = i;code = 105
char = b;code = 98
char = i;code = 105
char = t;code = 116
char = o;code = 111
char = r;code = 114
char = s;code = 115
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char = o;code = 111
char = f;code = 102
char = ;code = 32
char = C;code = 67
char = Y;code = 89
char = P;code = 80
char = 2;code = 50
char = D;code = 68
char = 6;code = 54
char = ;code = 32
char = (;code = 40
char = I;code = 73
char = C;code = 67
char = (;code = 40
char = 5;code = 53
char = 0;code = 48
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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
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char = o;code = 111
char = f;code = 102
char = ;code = 32
char = a;code = 97
char = p;code = 112
char = p;code = 112
char = r;code = 114
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char = x;code = 120
char = i;code = 105
char = m;code = 109
char = a;code = 97
char = t;code = 116
char = e;code = 101
char = l;code = 108
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char = ;code = 32
char = 3;code = 51
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char = m;code = 109
char = i;code = 105
char = c;code = 99
char = r;code = 114
char = o;code = 111
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char = M;code = 77
char = );code = 41
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 = l;code = 108
char = a;code = 97
char = m;code = 109
char = b;code = 98
char = d;code = 100
char = a;code = 97
char = -;code = 45
char = c;code = 99
char = y;code = 121
char = h;code = 104
char = a;code = 97
char = l;code = 108
char = o;code = 111
char = t;code = 116
char = h;code = 104
char = r;code = 114
char = i;code = 105
char = n;code = 110
char = ;code = 32
char = p;code = 112
char = o;code = 111
char = t;code = 116
char = e;code = 101
char = n;code = 110
char = t;code = 116
char = l;code = 108
char = y;code = 121
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char = i;code = 105
char = n;code = 110
char = h;code = 104
char = i;code = 105
char = b;code = 98
char = i;code = 105
char = t;code = 116
char = e;code = 101
char = d;code = 100
char = ;code = 32
char = b;code = 98
char = o;code = 111
char = t;code = 116
char = h;code = 104
char = ;code = 32
char = C;code = 67
char = Y;code = 89
char = P;code = 80
char = 2;code = 50
char = D;code = 68
char = 6;code = 54
char = ;code = 32
char = a;code = 97
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char = d;code = 100
char = ;code = 32
char = C;code = 67
char = Y;code = 89
char = P;code = 80
char = 3;code = 51
char = A;code = 65
char = 4;code = 52
char = -;code = 45
char = m;code = 109
char = e;code = 101
char = d;code = 100
char = i;code = 105
char = a;code = 97
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char = e;code = 101
char = d;code = 100
char = ;code = 32
char = a;code = 97
char = c;code = 99
char = t;code = 116
char = i;code = 105
char = v;code = 118
char = i;code = 105
char = t;code = 116
char = i;code = 105
char = e;code = 101
char = s;code = 115
char = ;code = 32
char = (;code = 40
char = I;code = 73
char = C;code = 67
char = (;code = 40
char = 5;code = 53
char = 0;code = 48
char = );code = 41
char = ';code = 39
char = s;code = 115
char = ;code = 32
char = a;code = 97
char = b;code = 98
char = o;code = 111
char = u;code = 117
char = t;code = 116
char = ;code = 32
char = 3;code = 51
char = -;code = 45
char = 4;code = 52
char = ;code = 32
char = m;code = 109
char = i;code = 105
char = c;code = 99
char = r;code = 114
char = o;code = 111
char = ;code = 32
char = M;code = 77
char = );code = 41
char = .;code = 46
char = ;code = 32
char = S;code = 83
char = o;code = 111
char = m;code = 109
char = e;code = 101
char = ;code = 32
char = p;code = 112
char = e;code = 101
char = s;code = 115
char = t;code = 116
char = i;code = 105
char = c;code = 99
char = i;code = 105
char = d;code = 100
char = e;code = 101
char = s;code = 115
char = ;code = 32
char = c;code = 99
char = a;code = 97
char = u;code = 117
char = s;code = 115
char = e;code = 101
char = d;code = 100
char = ;code = 32
char = r;code = 114
char = e;code = 101
char = l;code = 108
char = a;code = 97
char = t;code = 116
char = i;code = 105
char = v;code = 118
char = e;code = 101
char = l;code = 108
char = y;code = 121
char = ;code = 32
char = p;code = 112
char = o;code = 111
char = t;code = 116
char = e;code = 101
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char = t;code = 116
char = ;code = 32
char = i;code = 105
char = n;code = 110
char = h;code = 104
char = i;code = 105
char = b;code = 98
char = i;code = 105
char = t;code = 116
char = i;code = 105
char = o;code = 111
char = n;code = 110
char = s;code = 115
char = ;code = 32
char = s;code = 115
char = p;code = 112
char = o;code = 111
char = r;code = 114
char = a;code = 97
char = d;code = 100
char = i;code = 105
char = c;code = 99
char = a;code = 97
char = l;code = 108
char = l;code = 108
char = y;code = 121
char = ;code = 32
char = (;code = 40
char = c;code = 99
char = a;code = 97
char = r;code = 114
char = b;code = 98
char = e;code = 101
char = n;code = 110
char = d;code = 100
char = a;code = 97
char = z;code = 122
char = i;code = 105
char = m;code = 109
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char = ;code = 32
char = C;code = 67
char = Y;code = 89
char = P;code = 80
char = 2;code = 50
char = D;code = 68
char = 6;code = 54
char = ,;code = 44
char = ;code = 32
char = I;code = 73
char = C;code = 67
char = (;code = 40
char = 5;code = 53
char = 0;code = 48
char = );code = 41
char = ;code = 32
char = =;code = 61
char = ;code = 32
char = 1;code = 49
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char = ;code = 32
char = m;code = 109
char = i;code = 105
char = c;code = 99
char = r;code = 114
char = o;code = 111
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char = M;code = 77
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char = ;code = 32
char = a;code = 97
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char = r;code = 114
char = a;code = 97
char = z;code = 122
char = i;code = 105
char = n;code = 110
char = e;code = 101
char = ,;code = 44
char = ;code = 32
char = C;code = 67
char = Y;code = 89
char = P;code = 80
char = 3;code = 51
char = A;code = 65
char = 4;code = 52
char = ,;code = 44
char = ;code = 32
char = I;code = 73
char = C;code = 67
char = (;code = 40
char = 5;code = 53
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char = );code = 41
char = ;code = 32
char = =;code = 61
char = ;code = 32
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char = 8;code = 56
char = ;code = 32
char = m;code = 109
char = i;code = 105
char = c;code = 99
char = r;code = 114
char = o;code = 111
char = ;code = 32
char = M;code = 77
char = ;;code = 59
char = ;code = 32
char = g;code = 103
char = l;code = 108
char = y;code = 121
char = p;code = 112
char = h;code = 104
char = o;code = 111
char = s;code = 115
char = a;code = 97
char = t;code = 116
char = e;code = 101
char = ,;code = 44
char = ;code = 32
char = C;code = 67
char = Y;code = 89
char = P;code = 80
char = 2;code = 50
char = C;code = 67
char = 9;code = 57
char = ,;code = 44
char = ;code = 32
char = I;code = 73
char = C;code = 67
char = (;code = 40
char = 5;code = 53
char = 0;code = 48
char = );code = 41
char = ;code = 32
char = =;code = 61
char = ;code = 32
char = 3;code = 51
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char = 7;code = 55
char = ;code = 32
char = m;code = 109
char = i;code = 105
char = c;code = 99
char = r;code = 114
char = o;code = 111
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char = M;code = 77
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char = ;code = 32
char = h;code = 104
char = e;code = 101
char = x;code = 120
char = a;code = 97
char = f;code = 102
char = l;code = 108
char = u;code = 117
char = m;code = 109
char = u;code = 117
char = r;code = 114
char = o;code = 111
char = n;code = 110
char = ,;code = 44
char = ;code = 32
char = I;code = 73
char = C;code = 67
char = (;code = 40
char = 5;code = 53
char = 0;code = 48
char = );code = 41
char = ;code = 32
char = =;code = 61
char = ;code = 32
char = 6;code = 54
char = .;code = 46
char = 0;code = 48
char = ;code = 32
char = m;code = 109
char = i;code = 105
char = c;code = 99
char = r;code = 114
char = o;code = 111
char = ;code = 32
char = M;code = 77
char = );code = 41
char = .;code = 46
char = ;code = 32
char = W;code = 87
char = i;code = 105
char = t;code = 116
char = h;code = 104
char = ;code = 32
char = t;code = 116
char = h;code = 104
char = e;code = 101
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char = e;code = 101
char = x;code = 120
char = c;code = 99
char = e;code = 101
char = p;code = 112
char = t;code = 116
char = i;code = 105
char = o;code = 111
char = n;code = 110
char = s;code = 115
char = ;code = 32
char = o;code = 111
char = f;code = 102
char = ;code = 32
char = a;code = 97
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char = p;code = 112
char = h;code = 104
char = a;code = 97
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char = c;code = 99
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char = p;code = 112
char = e;code = 101
char = r;code = 114
char = m;code = 109
char = e;code = 101
char = t;code = 116
char = h;code = 104
char = r;code = 114
char = i;code = 105
char = n;code = 110
char = ,;code = 44
char = ;code = 32
char = c;code = 99
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char = p;code = 112
char = e;code = 101
char = r;code = 114
char = m;code = 109
char = e;code = 101
char = t;code = 116
char = h;code = 104
char = r;code = 114
char = i;code = 105
char = n;code = 110
char = ,;code = 44
char = ;code = 32
char = i;code = 105
char = s;code = 115
char = o;code = 111
char = p;code = 112
char = r;code = 114
char = o;code = 111
char = t;code = 116
char = u;code = 117
char = r;code = 114
char = o;code = 111
char = n;code = 110
char = ,;code = 44
char = ;code = 32
char = c;code = 99
char = a;code = 97
char = r;code = 114
char = b;code = 98
char = a;code = 97
char = r;code = 114
char = y;code = 121
char = l;code = 108
char = ;code = 32
char = a;code = 97
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char = d;code = 100
char = ;code = 32
char = a;code = 97
char = b;code = 98
char = a;code = 97
char = m;code = 109
char = e;code = 101
char = c;code = 99
char = t;code = 116
char = i;code = 105
char = n;code = 110
char = ,;code = 44
char = ;code = 32
char = m;code = 109
char = o;code = 111
char = s;code = 115
char = t;code = 116
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char = p;code = 112
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char = s;code = 115
char = t;code = 116
char = i;code = 105
char = c;code = 99
char = i;code = 105
char = d;code = 100
char = e;code = 101
char = s;code = 115
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char = i;code = 105
char = n;code = 110
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char = i;code = 105
char = b;code = 98
char = i;code = 105
char = t;code = 116
char = e;code = 101
char = d;code = 100
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char = r;code = 114
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char = l;code = 108
char = a;code = 97
char = t;code = 116
char = i;code = 105
char = v;code = 118
char = e;code = 101
char = l;code = 108
char = y;code = 121
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char = p;code = 112
char = o;code = 111
char = t;code = 116
char = e;code = 101
char = n;code = 110
char = t;code = 116
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char = y;code = 121
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char = a;code = 97
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char = ;code = 32
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char = a;code = 97
char = s;code = 115
char = t;code = 116
char = ;code = 32
char = o;code = 111
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char = e;code = 101
char = ;code = 32
char = C;code = 67
char = Y;code = 89
char = P;code = 80
char = -;code = 45
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char = l;code = 108
char = e;code = 101
char = c;code = 99
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char = y;code = 121
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char = w;code = 119
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char = i;code = 105
char = c;code = 99
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char = h;code = 104
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char = r;code = 114
char = e;code = 101
char = l;code = 108
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char = a;code = 97
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char = p;code = 112
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char = i;code = 105
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char = a;code = 97
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char = n;code = 110
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char = c;code = 99
char = c;code = 99
char = u;code = 117
char = p;code = 112
char = a;code = 97
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char = i;code = 105
char = o;code = 111
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char = a;code = 97
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char = e;code = 101
char = x;code = 120
char = p;code = 112
char = o;code = 111
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char = u;code = 117
char = r;code = 114
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char = s;code = 115
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char = a;code = 97
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char = d;code = 100
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char = f;code = 102
char = o;code = 111
char = r;code = 114
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char = f;code = 102
char = u;code = 117
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char = t;code = 116
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char = e;code = 101
char = r;code = 114
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char = s;code = 115
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char = u;code = 117
char = d;code = 100
char = i;code = 105
char = e;code = 101
char = s;code = 115
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char = o;code = 111
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char = ;code = 32
char = t;code = 116
char = h;code = 104
char = e;code = 101
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char = C;code = 67
char = Y;code = 89
char = P;code = 80
char = -;code = 45
char = a;code = 97
char = s;code = 115
char = s;code = 115
char = o;code = 111
char = c;code = 99
char = i;code = 105
char = a;code = 97
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char = e;code = 101
char = d;code = 100
char = ;code = 32
char = m;code = 109
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char = t;code = 116
char = a;code = 97
char = b;code = 98
char = o;code = 111
char = l;code = 108
char = i;code = 105
char = s;code = 115
char = m;code = 109
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char = o;code = 111
char = f;code = 102
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
char = t;code = 116
char = i;code = 105
char = v;code = 118
char = e;code = 101
char = ;code = 32
char = p;code = 112
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char = s;code = 115
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char = i;code = 105
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char = d;code = 100
char = e;code = 101
char = s;code = 115
char = .;code = 46
char = <;code = 60
char = b;code = 98
char = r;code = 114
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result sql = The goal of this work was to study the ability of 18 pesticides to inhibit selective model activities for all major xenobiotic-metabolizing enzymes, namely CYP1A1/2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4. Generally organophosphorus insecticides were the most potent and extensive inhibitors, especially towards CYP1A1/2 (IC(50) values of chlorpyrifos, fenitrothion and profenofos approximately 3 micro M), CYP2B6 (IC(50) values of chlorpyrifos and fenitrothion 2.5 micro M), CYP2C8 (fenitrothion 4.3 micro M), CYP2C9 (fenitrothion and malathion 4.8 and 2.5 micro M, respectively), CYP2D6 (chlorpyrifos and phenthoate approximately 3 micro M) and CYP3A4 (chlorpyrifos, fenitrothion and phenthoate 3-4 micro M). Otherwise there were quite considerable differences in potency and extent of inhibition between different organophosphates. Pyrethroids were in general very weak or inactive. Deltamethrin and fenvalerate were potent inhibitors of CYP2D6 (IC(50) values of approximately 3 micro M) while lambda-cyhalothrin potently inhibited both CYP2D6 and CYP3A4-mediated activities (IC(50)'s about 3-4 micro M). Some pesticides caused relatively potent inhibitions sporadically (carbendazim, CYP2D6, IC(50) = 12 micro M; atrazine, CYP3A4, IC(50) = 2.8 micro M; glyphosate, CYP2C9, IC(50) = 3.7 micro M; hexaflumuron, IC(50) = 6.0 micro M). With the exceptions of alpha-cypermethrin, cypermethrin, isoproturon, carbaryl and abamectin, most pesticides inhibited relatively potently at least one CYP-selective activity, which may have relevance for potential interactions in occupational exposures and for further studies on the CYP-associated metabolism of respective pesticides.

Publication: J Environ Sci Health B 2009 Aug ;44(6)::553-63. :doi: 10.1080/03601230902997766.
Publication Date: 2009 Aug
Study Author(s): Abass, Khaled;Turpeinen, Miia;Pelkonen, Olavi;
Institution: Pharmacology and Toxicology Unit, Institute of Biomedicine, University of Oulu, Oulu, Finland. [email protected]
Shortcut link to this study:
The goal of this work was to study the ability of 18 pesticides to inhibit selective model activities for all major xenobiotic-metabolizing enzymes, namely CYP1A1/2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4. Generally organophosphorus insecticides were the most potent and extensive inhibitors, especially towards CYP1A1/2 (IC(50) values of chlorpyrifos, fenitrothion and profenofos approximately 3 micro M), CYP2B6 (IC(50) values of chlorpyrifos and fenitrothion 2.5 micro M), CYP2C8 (fenitrothion 4.3 micro M), CYP2C9 (fenitrothion and malathion 4.8 and 2.5 micro M, respectively), CYP2D6 (chlorpyrifos and phenthoate approximately 3 micro M) and CYP3A4 (chlorpyrifos, fenitrothion and phenthoate 3-4 micro M). Otherwise there were quite considerable differences in potency and extent of inhibition between different organophosphates. Pyrethroids were in general very weak or inactive. Deltamethrin and fenvalerate were potent inhibitors of CYP2D6 (IC(50) values of approximately 3 micro M) while lambda-cyhalothrin potently inhibited both CYP2D6 and CYP3A4-mediated activities (IC(50)'s about 3-4 micro M). Some pesticides caused relatively potent inhibitions sporadically (carbendazim, CYP2D6, IC(50) = 12 micro M; atrazine, CYP3A4, IC(50) = 2.8 micro M; glyphosate, CYP2C9, IC(50) = 3.7 micro M; hexaflumuron, IC(50) = 6.0 micro M). With the exceptions of alpha-cypermethrin, cypermethrin, isoproturon, carbaryl and abamectin, most pesticides inhibited relatively potently at least one CYP-selective activity, which may have relevance for potential interactions in occupational exposures and for further studies on the CYP-associated metabolism of respective pesticides.
PMID: 20183062

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