Robert R. Fenichel

Receptor Binding

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