Robert R. Fenichel


Receptor Binding

Sorted by receptor/potency

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