Robert R. Fenichel

Receptor Binding

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Drug Class Model Receptor IC50 (µM) Relative Potency (IKr/X) Ref Comment
captopril ACE inhibitor AT-1 IKr 10 --- 129
sildenafil PDE inhibitor HERG/HEK IKr 100 --- 56
sildenafil PDE inhibitor PDE5 PDE5 0.001 0.00001 118
vesnarinone PDE inhibitor rabbit VM IKr 5.7 --- 115
vesnarinone PDE inhibitor human heart PDE3 6.2 1.1 87
spironolactone aldosterone antagonist HERG/CHO IKr 23 --- 35
alfuzosin alpha1-blocker HERG/CHO IKr 83.3 --- 92
doxazosin alpha1-blocker HERG/CHO IKr 2.5 --- 92
prazosin alpha1-blocker HERG/CHO IKr 3.4 --- 92
tamsulosin alpha1-blocker HERG/CHO IKr 104.8 --- 92
terazosin alpha1-blocker HERG/CHO IKr 21.4 --- 92
bepridil antianginal guinea-pig VM ICaL 0.5
134
bepridil antianginal guinea-pig AM ICaL 1.55
57
bepridil antianginal sheep PF IK1 >1.8
28
bepridil antianginal HERG/COS IKr 0.55 --- 42
bepridil antianginal IKs/COS IKs 10
42
bepridil antianginal guinea-pig AM INa 4.43
57
bepridil antianginal guinea-pig VM INa 30
134
bepridil antianginal sheep PF Ito <30
28
perhexiline antianginal HERG/CHO IKr 7.8 --- 124
ranolazine antianginal canine VM ICaL(late) 50 4.2 6
ranolazine antianginal canine VM ICaL(peak) 296 49 6
ranolazine antianginal canine VM IK1 >100
140
ranolazine antianginal canine VM IKr 11.5 --- 140
ranolazine antianginal canine VM IKr 12 --- 6
ranolazine antianginal canine VM IKs 13.4
140
ranolazine antianginal canine VM IKs >> 30 >> 5 6 17% at 30 uM
ranolazine antianginal canine VM INa 21
140
ranolazine antianginal canine VM INa(late) 6 0.5 6
ranolazine antianginal canine VM INaCa 91 15 6
ranolazine antianginal canine VM Ito >100 >9 140 17% at 100 uM
almokalant antiarrhythmic rabbit VM IKr 0.005 --- 38
amiodarone antiarrhythmic rat VM ICaL 5.8
93
amiodarone antiarrhythmic rabbit VM IK1 50
29
amiodarone antiarrhythmic guinea-pig AM IKAch 2
24
amiodarone antiarrhythmic guinea-pig VM IKNa 1
23
amiodarone antiarrhythmic AT-1 IKr 0.7 --- 129
amiodarone antiarrhythmic AT-1 IKr 1 --- 130
amiodarone antiarrhythmic HERG/L IKr 1 --- 130
amiodarone antiarrhythmic rabbit VM IKr 2.8 --- 64
amiodarone antiarrhythmic rabbit VM IKr 10 --- 21
amiodarone antiarrhythmic HERG/XO IKr 10 --- 73
amiodarone antiarrhythmic rat VM Ito 4.9
22
amiodarone antiarrhythmic rabbit VM Ito >10
21
aprinidine antiarrhythmic HERG/COS IKr 0.23 --- 59
aprinidine antiarrhythmic COS IKs >10
59
azimilide antiarrhythmic GP VM ICaL >10
54
azimilide antiarrhythmic GP VM IK1 >10
54
azimilide antiarrhythmic GP VM IKr 0.4 --- 54
azimilide antiarrhythmic HERG/XO IKr 1.4 --- 34
azimilide antiarrhythmic GP VM IKs 3
54
clofilium antiarrhythmic AT-1 IKr 1.25 --- 32
disopyramide antiarrhythmic rabbit VM IKr 1.8 --- 120
disopyramide antiarrhythmic AT-1 IKr 58 --- 98
disopyramide antiarrhythmic AT-1 IKr 60-100 --- 130
disopyramide antiarrhythmic HERG/L IKr 92
129
disopyramide antiarrhythmic
INa 28
132
disopyramide antiarrhythmic rabbit VM Ito 14
120
dofetilide antiarrhythmic GP VM IK1 >1
61
dofetilide antiarrhythmic rabbit VM IKr 0.0039 --- 39
dofetilide antiarrhythmic HERG/HEK IKr 0.0095 --- 94
dofetilide antiarrhythmic HERG/L IKr 0.0095 --- 94
dofetilide antiarrhythmic AT-1 IKr 0.011 --- 129
dofetilide antiarrhythmic AT-1 IKr 0.012 --- 131
dofetilide antiarrhythmic HERG/HEK IKr 0.012 --- 105
dofetilide antiarrhythmic HERG-HEK IKr 0.015 --- 95
dofetilide antiarrhythmic HERG/L IKr 0.015 --- 129
dofetilide antiarrhythmic HERG IKr 0.015 --- 76 at 22°C
dofetilide antiarrhythmic GP VM IKr 0.032 --- 61
dofetilide antiarrhythmic HL-1 IKr 0.047 --- 43
dofetilide antiarrhythmic mouse heart IKr 0.054 --- 81
dofetilide antiarrhythmic HERG/XO IKr 0.125 --- 80
dofetilide antiarrhythmic GP VM IKs >100
61
dofetilide antiarrhythmic HEK-293 IKv1.5 >10
94
E-4031 antiarrhythmic HERG/HEK IKr 0.0077 --- 137
E-4031 antiarrhythmic ferret heart IKr 0.0103 --- 83
E-4031 antiarrhythmic HERG/XO IKr 0.38 --- 2 +MiRP1
E-4031 antiarrhythmic GP VM IKr 0.397 --- 103
E-4031 antiarrhythmic GP VM IKr <5 --- 99
E-4031 antiarrhythmic HERG/XO IKr 0.588 --- 116
E-4031 antiarrhythmic HERG/XO IKr 1.25 --- 2 WT
E-4031 antiarrhythmic HERG/XO IKr 1.4 --- 34 different lab
encainide antiarrhythmic feline VM IKr 6 --- 55
flecainide antiarrhythmic feline VM IKr 2.2 --- 55
ibutilide antiarrhythmic HERG/L IKr 0.015 --- 129
ibutilide antiarrhythmic AT-1 IKr 0.02 --- 131
LY97241 antiarrhythmic HERG/XO IKr 0.15 --- 109
mexiletine antiarrhythmic rat VM ICaL 5.8 --- 93
MK-499 antiarrhythmic HERG/XO IKr 0.123 --- 106
MK-499 antiarrhythmic guinea-pig VM IKr 0.4 --- 54
procainamide antiarrhythmic AT-1 IKr 380 --- 130
N-acetylprocainamide antiarrhythmic AT-1 IKr 92 --- 98
quinidine antiarrhythmic feline VM IKr 0.18 --- 126
quinidine antiarrhythmic HERG/L IKr 0.3 --- 130
quinidine antiarrhythmic AT-1 IKr 1 --- 130
quinidine antiarrhythmic HERG/XO IKr 8 --- 80
RP-58866 antiarrhythmic guinea-pig VM IKr 0.02 --- 62
RP-58866 antiarrhythmic HERG/XO IKr 0.2 --- 62
d-sotalol antiarrhythmic GP VM IKr 100 --- 103
d-sotalol antiarrhythmic human AM IKv1.5 >500 --- 53
d-sotalol antiarrhythmic human AM Ito >500
53
terikalant antiarrhythmic guinea-pig VM IKr 0.031 --- 62
terikalant antiarrhythmic HERG/XO IKr 0.25 --- 62
WAY-123,398 antiarrhythmic feline VM IKr 0.019 --- 107
clarithromycin antibiotic/macrolide HERG/CHO IKr 20 --- 2 +MiRP1
clarithromycin antibiotic/macrolide HERG/CHO IKr 59 --- 2 WT
erythromycin antibiotic/macrolide AT-1 IKr 54.6 --- 127
erythromycin antibiotic/macrolide GP VM IKr >100 --- 47
erythromycin antibiotic/macrolide
IKr 387 --- 76 at 32-37°C
erythromycin antibiotic/macrolide
Ito 606
76 at 32-37°C
erythromycin antibiotic/macrolide S. pneumoniae MIC 1.36 <0.014 68
ciprofloxacin antibiotic/quinolone HERG/CHO IKr >100 --- 33 -40 mV
ciprofloxacin antibiotic/quinolone HERG/CHO IKr 966 --- 66
gatifloxacin antibiotic/quinolone AT-1 IKr 26.5 --- 4
gatifloxacin antibiotic/quinolone HERG/CHO IKr 130 --- 66
grepafloxacin antibiotic/quinolone AT-1 IKr 27.2 --- 4
grepafloxacin antibiotic/quinolone HERG/CHO IKr 27.5 --- 33 -40 mV
grepafloxacin antibiotic/quinolone HERG/CHO IKr 50 --- 66
levofloxacin antibiotic/quinolone HERG/CHO IKr 915 --- 66
moxifloxacin antibiotic/quinolone AT-1 IKr 0.75 --- 4
moxifloxacin antibiotic/quinolone HERG/CHO IKr 1 --- 97 -40 mV
moxifloxacin antibiotic/quinolone HERG/CHO IKr 41.2 --- 33 -40 mV
moxifloxacin antibiotic/quinolone HERG/CHO IKr 129 --- 66
ofloxacin antibiotic/quinolone HERG/CHO IKr 1420 --- 66
sparfloxacin antibiotic/quinolone AT-1 IKr 0.23 --- 4
sparfloxacin antibiotic/quinolone HERG/CHO IKr 13.5 --- 33 -40 mV
sparfloxacin antibiotic/quinolone HERG/CHO IKr 18 --- 66
atropine anticholinergic
IKr 0.558 --- 76
amitriptyline antidepressant HERG/CHO IKr >3 --- 112
amitriptyline antidepressant HERG/CHO IKr 10 --- 114
amitriptyline antidepressant rat neuron IKr 10 --- 125
imipramine antidepressant HERG/CHO IKr 3.4 --- 112
valproic acid antiepileptic AT-1 IKr 20 --- 127
tamoxifen antiestrogen rabbit VM IKr 1 --- 84
clotrimazole antifungal GP VM ICaL <25
113 5=IC16, 25 = IC59
ketoconazole antifungal feline VM IKr 2.5 --- 41
ketoconazole antifungal HERG/XO IKr 49 --- 51
ketoconazole antifungal XO IKv1.5 107
51
ketoconazole antifungal feline VM Ito 10
41
astemizole antihistamine GP cerebellum H1 0.052 58 27
astemizole antihistamine GP LM H1 0.079 88 74
astemizole antihistamine GP LM H1 0.3 333 63
astemizole antihistamine guinea-pig VM IK1 >10
31
astemizole antihistamine HERG/HEK IKr 0.0009 --- 138
astemizole antihistamine guinea-pig VM IKr 0.0015 --- 101
astemizole antihistamine HERG/HEK IKr 0.022 --- 46 at 37°C
astemizole antihistamine HERG/XO IKr 0.048 --- 110
astemizole antihistamine HERG/XO IKr 0.069 --- 40
astemizole antihistamine HERG/XO IKr 0.33 --- 111
astemizole antihistamine
IKs >10
101 10uM = IC0.3
astemizole antihistamine XO IKs >60
110
astemizole antihistamine XO IKv1.1 >60
110
astemizole antihistamine XO IRK1 >60
110
astemizole antihistamine guinea-pig VM Ito >10
31
astemizole antihistamine
Ito >10
30 10uM = IC23
desmethylastemizole antihistamine GP LM H1 0.2 10 63
desmethylastemizole antihistamine HERG/HEK IKr 0.001 --- 138
norastemizole antihistamine HERG/HEK IKr 0.028 --- 138
cetirizine antihistamine GP cerebellum H1 0.47 0.004 27
cetirizine antihistamine rabbit VM IK1 >1000
37
cetirizine antihistamine HERG/XO IKr >30 --- 111
cetirizine antihistamine rabbit VM IKr 108 --- 37
cetirizine antihistamine rabbit VM IKs >1000
37 1mM = IC44
chlorpheniramine antihistamine GP LM H1 0.002 0.001 74
chlorpheniramine antihistamine
IK1 >10
101 10uM=IC0.6
chlorpheniramine antihistamine
IKr 1.1 --- 101
chlorpheniramine antihistamine GP VM IKr 1.6 --- 102
chlorpheniramine antihistamine HERG/XO IKr 21 --- 110
chlorpheniramine antihistamine
IKs >10
101 10uM = IC9.7
cyproheptadine antihistamine GP cerebellum H1 0.003
27
diphenhydramine antihistamine GP LM H1 0.042 0.038 74
diphenhydramine antihistamine GP VM IKr 0.03 --- 72
diphenhydramine antihistamine GP VM IKr 1.1 --- 102
diphenhydramine antihistamine HERG/XO IKr 27 --- 110
ebastine antihistamine GP LM H1 0.27 1.9 74
ebastine antihistamine rat VM IK1 >3
75
ebastine antihistamine guinea-pig VM IKr 0.14 --- 75
ebastine antihistamine guinea-pig VM IKs 2
75
ebastine antihistamine
IKv1.5 >1
20 1uM = IC6.5
ebastine antihistamine rat VM Ito >3
75
epinastine antihistamine HERG/XO IKr >100 --- 40
fexofenadine antihistamine GP LM H1 0.26 0.024 74
fexofenadine antihistamine feline VM IKr >5 --- 126
fexofenadine antihistamine
IKr >10
96
fexofenadine antihistamine HERG IKr 13.1 --- 76 at 32-37°C
fexofenadine antihistamine HERG/HEK IKr 21.57 --- 46 at 37°C
fexofenadine antihistamine HERG/XO IKr >500 --- 100
fexofenadine antihistamine
IKs 20.4
76 at 32-37°C
fexofenadine antihistamine
IKv1.5 >50
128
fexofenadine antihistamine feline VM IKv1.5 214
96
fexofenadine antihistamine
IKv1.5 389
76 at 32-37°C
fexofenadine antihistamine XO IKv1.5 >500
100
fexofenadine antihistamine
Ito 112
76 at 32-37°C
loratidine antihistamine GP cerebellum H1 1 0.3 27
loratidine antihistamine HERG/HEK IK1 >1
45
loratidine antihistamine rat VM IK1 >10
50
loratidine antihistamine HERG/HEK IKr 0.173 --- 45
loratidine antihistamine
IKr >1 --- 50 1uM = IC5
loratidine antihistamine HERG/XO IKr 100 --- 111
loratidine antihistamine
IKs <10
50 10uM = IC58
loratidine antihistamine guinea-pig VM IKs <25
50
loratidine antihistamine HEK 293 IKv1.5 0.8
77
loratidine antihistamine
IKv1.5 1.2
19
loratidine antihistamine HERG/HEK Isus >1
45
loratidine antihistamine HERG/HEK Ito >1
45
loratidine antihistamine rat VM Ito 2.6
50
loratidine antihistamine
Ito >10
50 10uM = IC12
DC-loratidine antihistamine HERG/HEK IKr 1.82 --- 46 at 37°C
mizolastine antihistamine HERG/HEK IKr 0.441 --- 46 at 37°C
pyrilamine antihistamine GP cerebellum H1 0.006 0.005 27
pyrilamine antihistamine
IK1 >10
101 10uM = IC1.3
pyrilamine antihistamine guinea-pig VM IKr 1.1 --- 102
pyrilamine antihistamine
IKr 1.1 --- 101
pyrilamine antihistamine
IKs >10
101 10uM = IC16
terfenadine antihistamine GP cerebellum H1 0.45 9 27
terfenadine antihistamine GP LM H1 0.56 3.7 74
terfenadine antihistamine guinea-pig VM ICa <3
90
terfenadine antihistamine rat VM ICaL 0.14
82
terfenadine antihistamine HERG/HEK IK1 >1
45
terfenadine antihistamine
IK1 >10
31
terfenadine antihistamine guinea-pig VM IK1 >10
31
terfenadine antihistamine guinea-pig VM IKr 0.05 --- 101
terfenadine antihistamine HERG/HEK IKr 0.056 --- 95
terfenadine antihistamine HERG IKr 0.056 --- 76 at 32-37°C
terfenadine antihistamine rabbit VM IKr 0.096 --- 37
terfenadine antihistamine AT-1 IKr 0.097 --- 127
terfenadine antihistamine feline VM IKr 0.15 --- 126
terfenadine antihistamine HERG/HEK IKr 0.204 --- 45
terfenadine antihistamine HERG/XO IKr 0.246 --- 110
terfenadine antihistamine HERG/XO IKr 0.431 --- 40
terfenadine antihistamine HERG/XO IKr 0.48 --- 111
terfenadine antihistamine
IKs 4.4
76 at 32-37°C
terfenadine antihistamine
IKs <10
101 10uM = IC58
terfenadine antihistamine XO IKs 29
110
terfenadine antihistamine XO IKv1.1 34
110
terfenadine antihistamine
IKv1.5 0.367
76 at 32-37°C
terfenadine antihistamine feline VM IKv1.5 0.37
96
terfenadine antihistamine XO IKv1.5 1
128
terfenadine antihistamine
IKv1.5 1.1
18
terfenadine antihistamine XO IKv1.5 2.6
100
terfenadine antihistamine guinea-pig VM INa <3
90
terfenadine antihistamine XO IRK1 23
110
terfenadine antihistamine HERG/HEK Isus >1
45
terfenadine antihistamine guinea-pig VM Ito >1
31
terfenadine antihistamine HERG/HEK Ito >1
45
terfenadine antihistamine
Ito >1
30 1uM = IC11
terfenadine antihistamine
Ito 2.7
76 at 32-37°C
trimethaphan antihypertensive AT-1 IKr 10 --- 127
chlorpromazine antipsychotic HERG/CHO IKr 1.47 --- 114
clozapine antipsychotic human AM IK1 >100
46
clozapine antipsychotic HERG/HEK IKr 0.191 --- 46 at 37°C
clozapine antipsychotic human AM INa 29.0
46
clozapine antipsychotic human AM Isus >100
46
clozapine antipsychotic human AM Ito 50-100
46
haloperidol antipsychotic human AM IK1 >100
46
haloperidol antipsychotic HERG/HEK IKr 0.0281 --- 46 at 37°C
haloperidol antipsychotic HERG/XO IKr 1 --- 108
haloperidol antipsychotic human AM INa 14.4
46
haloperidol antipsychotic human AM Isus 10-100
46
haloperidol antipsychotic human AM Ito 10-100
46
olanzipine antipsychotic human AM IK1 >>100
46
olanzipine antipsychotic HERG/HEK IKr 0.181 --- 46 at 37°C
olanzipine antipsychotic human AM INa >100
46
olanzipine antipsychotic human AM Isus >100
46
olanzipine antipsychotic human AM Ito >100
46
pimozide antipsychotic rat brain 5HT2 0.031 1.7 44
pimozide antipsychotic human AM IK1 >100
46
pimozide antipsychotic HERG IKr 0.018 --- 65
pimozide antipsychotic HERG/HEK IKr 0.0497 --- 46 at 37°C
pimozide antipsychotic HERG IKs >10
65
pimozide antipsychotic HERG IKv1.5 >10
65
pimozide antipsychotic human AM INa 21.9
46
pimozide antipsychotic human AM Isus >>100
46
pimozide antipsychotic human AM Ito >>100
46
risperidone antipsychotic
5HT2 0.00016 0.0004 104
risperidone antipsychotic
D2 0.0033 0.008 104
risperidone antipsychotic human AM IK1 >100
46
risperidone antipsychotic HERG/HEK IKr 0.163 --- 46 at 37°C
risperidone antipsychotic
IKr 0.394 --- 76 at 32-37°C
risperidone antipsychotic
IKs 9.7
76 at 32-37°C
risperidone antipsychotic
IKv1.5 9.5
76 at 32-37°C
risperidone antipsychotic human AM INa 50-100
46
risperidone antipsychotic human AM Isus >100
46
risperidone antipsychotic
Ito 25.5
76 at 32-37°C
risperidone antipsychotic human AM Ito >100
46
sertindole antipsychotic
5HT2 0.00085 0.17 104
sertindole antipsychotic
D2 0.0074 1.5 104
sertindole antipsychotic human AM IK1 >10
46
sertindole antipsychotic HERG IKr 0.005 --- 76 at 32-37°C
sertindole antipsychotic HERG/HEK IKr 0.0126 --- 46 at 37°C
sertindole antipsychotic HERG/L IKr 0.014 --- 94
sertindole antipsychotic
IKs 0.88
76 at 32-37°C
sertindole antipsychotic HEK IKv1.5 2.12
94
sertindole antipsychotic
IKv1.5 4
76 at 32-37°C
sertindole antipsychotic human AM INa >10
46
sertindole antipsychotic human AM Isus >10
46
sertindole antipsychotic
Ito 8.8
76 at 32-37°C
sertindole antipsychotic human AM Ito >10
46
thioridazine antipsychotic human AM IK1 >100
46
thioridazine antipsychotic HERG/HEK IKr 0.0357 --- 46 at 37°C
thioridazine antipsychotic HERG/CHO IKr 1.07 --- 114
thioridazine antipsychotic HERG/tsA-201 IKr 1.25 --- 49
thioridazine antipsychotic guinea-pig VM IKr 1.25 --- 49
thioridazine antipsychotic guinea-pig VM IKs 14
49
thioridazine antipsychotic human AM INa 7.0
46
thioridazine antipsychotic human AM Isus >100
46
thioridazine antipsychotic human AM Ito 27
46
ziprasidone antipsychotic human AM IK1 >10
46
ziprasidone antipsychotic HERG/HEK IKr 0.152 --- 46 at 37°C
ziprasidone antipsychotic human AM INa >10
46
ziprasidone antipsychotic human AM Isus >10
46
ziprasidone antipsychotic human AM Ito >10
46
terodiline antispasmodic AT-1 IKr 0.0037 --- 127
terodiline antispasmodic guinea-pig VM IKr 0.7 --- 60
clobutinol antitussive
IKr 2.9 --- 26
lopinavir antiviral HERG/HEK IKr 8.6 --- 5
nelfinavir antiviral HERG/HEK IKr 11.5 --- 5
ritonavir antiviral HERK/HEK IKr 8.2 --- 5
saquinavir antiviral HERG/HEK IKr 15.3 --- 5
propranolol beta blocker AT-1 IKr 15 --- 127
carvedilol beta-blocker HERG/XO IKr 10.42 --- 69
diltiazem calcium antagonist HERG/COS IKr >10 --- 42
diltiazem calcium antagonist HERG/HEK IKr 17.3 --- 136
diltiazem calcium antagonist IKs/COS IKs >10
42
mibefradil calcium antagonist guinea pig ICaL 0.2
52 -50 mV
mibefradil calcium antagonist guinea pig ICaL 12
52 -80 mV
mibefradil calcium antagonist
ICaL 18.6
88
mibefradil calcium antagonist
ICaT 2.7
88
mibefradil calcium antagonist AT-1 IKr 0.4-0.8 --- 130
mibefradil calcium antagonist AT-1 IKr 0.75 --- 98
mibefradil calcium antagonist HERG/COS IKr 1.43 --- 42
mibefradil calcium antagonist IKs/COS IKs 11.8
42
verapamil calcium antagonist guinea pig ICaL 0.7
52
verapamil calcium antagonist HERG/HEK IKr 0.143 --- 136
verapamil calcium antagonist HERG/L IKr 0.34 --- 129
verapamil calcium antagonist AT-1 IKr 0.3-1 --- 130
verapamil calcium antagonist HERG/COS IKr 0.83 --- 42
verapamil calcium antagonist AT-1 IKr 1.3 --- 98
verapamil calcium antagonist HERG/XO IKr 3.8 --- 122
verapamil calcium antagonist IKs/COS IKs >10
42
cromakalim chromanol deriv GP VM IKr >20 --- 58
cromakalim chromanol deriv IKs/COS IKs >10
85
cromakalim chromanol deriv GP VM IKs >20
58
amlodipine dihydropyridine AT-1 IKr 1 --- 130
amlodipine dihydropyridine AT-1 IKr 3
129
nifedipine dihydropyridine HERG/HEK IKr >50 --- 136
nitrendipine dihydropyridine HERG/COS IKr >10 --- 42
nitrendipine dihydropyridine IKs/COS IKs >10
42
nitrendipine dihydropyridine rat VM INa 3
133
indapamide diuretic GP VM IKs 196
117
hesperetin flavonoid HERG/XO IKr 288.8 --- 139
morin flavonoid HERG/XO IKr 111.4 --- 139
naringenin flavonoid HERK/HEK IKr 36.5 --- 139 13.8% @ 1 uM
naringenin flavonoid HERG/XO IKr 102.3 --- 139
OPC-18790 inotrope AT-1 IKr 0.96 --- 129
cocaine local anesthetic HERG/HEK IKr 7.2 --- 135
buprenorphine opiate HERG/HEK IKr 7.5 --- 71
codeine opiate HERG/HEK IKr > 300 --- 71
EDDP opiate HERG/HEK IKr >50 --- 71 methadone metabolite
fentanyl opiate HERG/HEK IKr 1.8 --- 71
LAAM opiate HERG/HEK IKr 2.2 --- 71
meperidine opiate HERG/HEK IKr 75 --- 71
methadone opiate HERG/HEK IKr 9.8 --- 71
methadone opiate HERG/HEK IKr 10 --- 70
morphine opiate HERG/HEK IKr > 1000 --- 71
cisapride prokinetic various 5HT4 0.023-0.031 0.5 89
cisapride prokinetic HERG/HEK IKr 0.0065 --- 91 different lab
cisapride prokinetic rabbit VM IKr 0.009 --- 36
cisapride prokinetic guinea-pig VM IKr 0.015 --- 48
cisapride prokinetic HERG/CHO IKr 0.016 --- 123 at 20-22°C
cisapride prokinetic HERG/CHO IKr 0.024 --- 123 at 37°C
cisapride prokinetic HERG/HEK IKr 0.044 --- 95
cisapride prokinetic HERG IKr 0.044 --- 76 at 32-37°C
cisapride prokinetic
IKs 3.39
76 at 32-37°C
cisapride prokinetic guinea-pig VM IKs >10
48
cisapride prokinetic
IKv1.5 21.2
76 at 32-37°C
cisapride prokinetic
Ito 9.33
76 at 32-37°C
ketanserin serotonin antagonist guinea-pig VM IKr >32 --- 79
ketanserin serotonin antagonist rabbit VM Ito 2.25
78
glibenclamide sulfonylurea neuroblastoma IKr 74.8 --- 99
glibenclamide sulfonylurea GP VM IKr <100 --- 99
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