Robert R. Fenichel

Receptor Binding

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