Compounds > tecastemizole
Page last updated: 2024-09-25

tecastemizole

Cross-References

ID SourceID
PubMed CID123618
CHEMBL ID61301
SCHEMBL ID18200
MeSH IDM0277358

Synonyms (43)

Synonym
r-43512
soltara
tecastemizole
norastemizole
D06021
tecastemizole (usan/inn)
75970-99-9
t 1348
1h-benzimidazol-2-amine, 1-((4-fluorophenyl)methyl)-n-4-piperidinyl-
1-(-fluorobenzyl)-n-(piperidin-4-yl)-1h-benzimidazol-2-amine
1-((4-flurophenyl)methyl)-n-4-piperidinyl-1h-benzimidazol-2-amine
[1-(4-fluoro-benzyl)-1h-benzoimidazol-2-yl]-piperidin-4-yl-amine(norastemizole)
bdbm50117925
1-(4-fluorobenzyl)-n-(piperidin-4-yl)-1h-benzo[d]imidazol-2-amine
[1-(4-fluoro-benzyl)-1h-benzoimidazol-2-yl]-piperidin-4-yl-amine;2hbr
[1-(4-fluoro-benzyl)-1h-benzoimidazol-2-yl]-piperidin-4-yl-amine
CHEMBL61301 ,
norastemizole (trivial name)
1-[(4-fluorophenyl)methyl]-n-piperidin-4-ylbenzimidazol-2-amine
AKOS005067567
w5dco14m05 ,
unii-w5dco14m05
tecastemizole [usan:inn]
tecastemizole [inn]
1-(4-fluorobenzyl)-n-(4-piperidinyl)-1h-benzimidazol-2-amine
tecastemizole [usan]
1h-benzimidazol-2-amine,1-((4-fluorophenyl)methyl)-n-4-piperidinyl-
SCHEMBL18200
DTXSID30226877
1-(4-fluorophenylmethyl)-n-(4-piperidinyl)-1h-benzimidazol-2-amine
1-(4-fluorophenyl-methyl)-n-(4-piperidinyl)-1h-benzimidazol-2-amine
1-[(4 fluorophenyl)methyl]-n-(4-piperidinyl)-1h-benzimidazol-2-amine
(4-fluorophenyl)methyl-n-(4-piperidinyl)-1h-benzimidazol-2-amine
(1(4-fluorobenzyl)-1h-benzimidazol-2-yl)(piperidin-4-yl)amine
SFOVDSLXFUGAIV-UHFFFAOYSA-N
1-[(4-fluorophenyl)methyl]-n-(4-piperidinyl)-1h-benzimidazol-2-amine
(1-(4-fluorobenzyl)-1h-benzimidazol-2-yl)(piperidin-4-yl)amine
DB06457
norastemizole; soltara; tecastemizole
Q27292334
MS-24847
CS-0024692
HY-105014

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)0.02800.00091.901410.0000AID161281; AID222148; AID243188; AID392051; AID408340; AID420668
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (50)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 4 group A member 2Homo sapiens (human)
response to hypoxiaNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
neuron migrationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
response to amphetamineNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
DNA-templated transcriptionNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
transcription by RNA polymerase IINuclear receptor subfamily 4 group A member 2Homo sapiens (human)
adult locomotory behaviorNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
post-embryonic developmentNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
central nervous system projection neuron axonogenesisNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
habenula developmentNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
cellular response to oxidative stressNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
regulation of dopamine metabolic processNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
dopamine biosynthetic processNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
neuron maturationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
negative regulation of neuron apoptotic processNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
regulation of respiratory gaseous exchangeNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
fat cell differentiationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 4 group A member 2Homo sapiens (human)
neuron apoptotic processNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
general adaptation syndromeNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
canonical Wnt signaling pathwayNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
cellular response to corticotropin-releasing hormone stimulusNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
dopaminergic neuron differentiationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
midbrain dopaminergic neuron differentiationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
negative regulation of apoptotic signaling pathwayNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor subfamily 4 group A member 2Homo sapiens (human)
central nervous system neuron differentiationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
DNA bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
beta-catenin bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nuclear retinoid X receptor bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
protein heterodimerization activityNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nuclear glucocorticoid receptor bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
nucleusNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nucleoplasmNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
cytoplasmNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nuclear speckNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
protein-containing complexNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
transcription regulator complexNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nucleusNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (16)

Assay IDTitleYearJournalArticle
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID1366321Antimalarial activity against Plasmodium falciparum 3D7 infected in ARh+ human erythrocytes at 10 uM after 42 to 48 hrs by Picogreen staining-based 96 well microplate assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID513156Antimalarial activity against Plasmodium falciparum ItG assessed as inhibition of parasite growth after 48 to 96 hrs by [3H]hypoxanthine incorporation assay2006Nature chemical biology, Aug, Volume: 2, Issue:8
A clinical drug library screen identifies astemizole as an antimalarial agent.
AID420668Inhibition of human ERG in MCF7 cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID513160Antimalarial activity against Plasmodium falciparum 3D7 assessed as inhibition of parasite growth after 48 to 96 hrs by [3H]hypoxanthine incorporation assay2006Nature chemical biology, Aug, Volume: 2, Issue:8
A clinical drug library screen identifies astemizole as an antimalarial agent.
AID1571766Binding affinity to Nurr1 (unknown origin) by 1H-STD-NMR spectroscopy2019Journal of medicinal chemistry, Mar-14, Volume: 62, Issue:5
Ligand-Based Fluorine NMR Screening: Principles and Applications in Drug Discovery Projects.
AID513155Antimalarial activity against Plasmodium falciparum Dd2 assessed as inhibition of parasite growth after 48 to 96 hrs by [3H]hypoxanthine incorporation assay2006Nature chemical biology, Aug, Volume: 2, Issue:8
A clinical drug library screen identifies astemizole as an antimalarial agent.
AID243188Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
A two-state homology model of the hERG K+ channel: application to ligand binding.
AID1366325Antimalarial activity against Plasmodium falciparum 3D7 infected in ARh+ human erythrocytes after 42 to 48 hrs by Picogreen staining-based 96 well microplate assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.
AID1366322Antimalarial activity against Plasmodium falciparum 3D7 infected in ARh+ human erythrocytes at 1 uM after 42 to 48 hrs by Picogreen staining-based 96 well microplate assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.
AID392051Inhibition of human ERG channel in HEK293 cells by voltage-clamp method2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation.
AID1366324Antimalarial activity against Plasmodium falciparum 3D7 infected in ARh+ human erythrocytes at 0.01 uM after 42 to 48 hrs by Picogreen staining-based 96 well microplate assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.
AID1366323Antimalarial activity against Plasmodium falciparum 3D7 infected in ARh+ human erythrocytes at 0.1 uM after 42 to 48 hrs by Picogreen staining-based 96 well microplate assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.
AID420669Lipophilicity, log D at pH 7.02009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID222148K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.12002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (16.67)18.2507
2000's12 (66.67)29.6817
2010's3 (16.67)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.56%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (94.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceDescriptionRelationhip StrengthStudiesTrialsClassesRoles
amitriptyline[no description available]medium60carbotricyclic compound;
tertiary amine		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
tropomyosin-related kinase B receptor agonist;
xenobiotic
astemizole[no description available]medium140benzimidazoles;
piperidines		anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
bepridil[no description available]medium50pyrrolidines;
tertiary amine		anti-arrhythmia drug;
antihypertensive agent;
calcium channel blocker;
vasodilator agent
verapamil[no description available]medium60aromatic ether;
nitrile;
polyether;
tertiary amino compound
chlorpromazine[no description available]medium50organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
cisapride[no description available]medium80benzamides
domperidone[no description available]medium40benzimidazoles;
heteroarylpiperidine		antiemetic;
dopaminergic antagonist
droperidol[no description available]medium60aromatic ketone;
benzimidazoles;
organofluorine compound		anaesthesia adjuvant;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic
e 4031[no description available]medium60sulfonamide
fexofenadine[no description available]medium30piperidines;
tertiary amine		anti-allergic agent;
H1-receptor antagonist
glyburide[no description available]medium20monochlorobenzenes;
N-sulfonylurea		anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
granisetron[no description available]medium30aromatic amide;
indazoles
haloperidol[no description available]medium60aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
imipramine[no description available]medium50dibenzoazepineadrenergic uptake inhibitor;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
loratadine[no description available]medium50benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide		anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
perhexiline[no description available]medium50piperidinescardiovascular drug
risperidone[no description available]medium501,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist
gatifloxacin[no description available]medium50N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
terfenadine[no description available]medium70diarylmethane
thioridazine[no description available]medium50phenothiazines;
piperidines		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
pimozide[no description available]medium60benzimidazoles;
heteroarylpiperidine;
organofluorine compound		antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
halofantrine[no description available]medium50phenanthrenes
diltiazem[no description available]medium505-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetateantihypertensive agent;
calcium channel blocker;
vasodilator agent
sertindole[no description available]medium50heteroarylpiperidine;
imidazolidinone;
organochlorine compound;
organofluorine compound;
phenylindole		alpha-adrenergic antagonist;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic antagonist
sparfloxacin[no description available]medium50fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
mibefradil[no description available]medium50tetralinsT-type calcium channel blocker
ziprasidone[no description available]medium401,2-benzisothiazole;
indolones;
organochlorine compound;
piperazines		antipsychotic agent;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
psychotropic drug;
serotonergic antagonist
mizolastine[no description available]medium50benzimidazoles
uk 68798[no description available]medium50aromatic ether;
sulfonamide;
tertiary amino compound		anti-arrhythmia drug;
potassium channel blocker
grepafloxacin[no description available]medium50fluoroquinolone antibiotic;
quinolines;
quinolone antibiotic
moxifloxacin[no description available]medium50aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
cocaine[no description available]medium50benzoate ester;
methyl ester;
tertiary amino compound;
tropane alkaloid		adrenergic uptake inhibitor;
central nervous system stimulant;
dopamine uptake inhibitor;
environmental contaminant;
local anaesthetic;
mouse metabolite;
plant metabolite;
serotonin uptake inhibitor;
sodium channel blocker;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
dolasetron[no description available]medium50indolyl carboxylic acid
azimilide[no description available]medium40imidazolidine-2,4-dione
clozapine[no description available]medium50benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
sildenafil[no description available]medium40piperazines;
pyrazolopyrimidine;
sulfonamide		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
alosetron[no description available]medium20imidazoles;
pyridoindole		antiemetic;
gastrointestinal drug;
serotonergic antagonist
amiodarone[no description available]medium201-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound		cardiovascular drug
carvedilol[no description available]medium20carbazoles;
secondary alcohol;
secondary amino compound		alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
cetirizine[no description available]medium30ether;
monocarboxylic acid;
monochlorobenzenes;
piperazines		anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic
chlorpheniramine[no description available]medium20monochlorobenzenes;
pyridines;
tertiary amino compound		anti-allergic agent;
antidepressant;
antipruritic drug;
H1-receptor antagonist;
histamine antagonist;
serotonin uptake inhibitor
ciprofloxacin[no description available]medium20aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
citalopram[no description available]medium202-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound
desipramine[no description available]medium20dibenzoazepine;
secondary amino compound		adrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
cholinergic antagonist;
drug allergen;
EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
serotonin uptake inhibitor
diphenhydramine[no description available]medium20ether;
tertiary amino compound		anti-allergic agent;
antidyskinesia agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
antitussive;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
oneirogen;
sedative
disopyramide[no description available]medium20monocarboxylic acid amide;
pyridines;
tertiary amino compound		anti-arrhythmia drug
epinastine[no description available]medium20benzazepine;
guanidines		anti-allergic agent;
H1-receptor antagonist;
histamine antagonist;
ophthalmology drug
flecainide[no description available]medium20aromatic ether;
monocarboxylic acid amide;
organofluorine compound;
piperidines		anti-arrhythmia drug
fluoxetine[no description available]medium20(trifluoromethyl)benzenes;
aromatic ether;
secondary amino compound
ketoconazole[no description available]medium20dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
mefloquine hydrochloride[no description available]medium30organofluorine compound;
piperidines;
quinolines;
secondary alcohol
mesoridazine[no description available]medium20phenothiazines;
sulfoxide;
tertiary amino compound		dopaminergic antagonist;
first generation antipsychotic
nifedipine[no description available]medium20C-nitro compound;
dihydropyridine;
methyl ester		calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
nitrendipine[no description available]medium20C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
ethyl ester;
methyl ester		antihypertensive agent;
calcium channel blocker;
geroprotector;
vasodilator agent
ofloxacin[no description available]medium203-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline
ondansetron[no description available]medium20carbazoles
trimethoprim[no description available]medium20aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic
vesnarinone[no description available]medium20organic molecular entity
ibutilide[no description available]medium20benzenes;
organic amino compound
terikalant[no description available]medium20piperidines
clarithromycin[no description available]medium20macrolide antibioticantibacterial drug;
environmental contaminant;
protein synthesis inhibitor;
xenobiotic
nicotine[no description available]medium303-(1-methylpyrrolidin-2-yl)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
levofloxacin[no description available]medium209-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
desmethylastemizole[no description available]medium60benzimidazoles
quinidine[no description available]medium50cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
mefloquine hydrochloride[no description available]medium10
1-[4-[4-[[(2R)-2-(2,4-dichlorophenyl)-2-(1-imidazolylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]ethanone[no description available]medium10piperazines
olanzapine[no description available]medium20benzodiazepine;
N-arylpiperazine;
N-methylpiperazine		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor
norclozapine[no description available]medium20dibenzodiazepine;
organochlorine compound;
piperazines		delta-opioid receptor agonist;
metabolite;
serotonergic antagonist
quinacrine[no description available]medium10acridines;
aromatic ether;
organochlorine compound;
tertiary amino compound		antimalarial;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor
ampicillin[no description available]medium10beta-lactam antibiotic;
penicillin allergen;
penicillin		antibacterial drug
quinine[no description available]medium10cinchona alkaloidantimalarial;
muscle relaxant;
non-narcotic analgesic
8-hydroxy-2-(di-n-propylamino)tetralin[no description available]medium10phenols;
tertiary amino compound;
tetralins		serotonergic antagonist
lidocaine[no description available]medium10benzenes;
monocarboxylic acid amide;
tertiary amino compound		anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic
lamotrigine[no description available]medium101,2,4-triazines;
dichlorobenzene;
primary arylamine		anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic
meperidine[no description available]medium10ethyl ester;
piperidinecarboxylate ester;
tertiary amino compound		antispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
nisoxetine[no description available]medium10aromatic ether;
secondary amino compound		adrenergic uptake inhibitor;
antidepressant
phenobarbital[no description available]medium10barbituratesanticonvulsant;
drug allergen;
excitatory amino acid antagonist;
sedative
pilsicainide[no description available]medium10organic heterobicyclic compound;
secondary carboxamide		anti-arrhythmia drug;
sodium channel blocker
pirenperone[no description available]medium10aromatic ketone
ritanserin[no description available]medium10organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
sotalol[no description available]medium10ethanolamines;
secondary alcohol;
secondary amino compound;
sulfonamide		anti-arrhythmia drug;
beta-adrenergic antagonist;
environmental contaminant;
xenobiotic
spiperone[no description available]medium10aromatic ketone;
azaspiro compound;
organofluorine compound;
piperidines;
tertiary amino compound		alpha-adrenergic antagonist;
antipsychotic agent;
dopaminergic antagonist;
psychotropic drug;
serotonergic antagonist
tetracaine[no description available]medium10benzoate ester;
tertiary amino compound		local anaesthetic
trifluperidol[no description available]medium10aromatic ketone
tadalafil[no description available]medium10benzodioxoles;
pyrazinopyridoindole		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
anhydroecgonine methyl ester[no description available]medium10N-alkylpyrrolidine
l 706000[no description available]medium10
desmethylolanzapine[no description available]medium10benzodiazepine
mdl 74156[no description available]medium10
fluphenazine[no description available]medium10N-alkylpiperazine;
organofluorine compound;
phenothiazines		anticoronaviral agent;
dopaminergic antagonist;
phenothiazine antipsychotic drug
nortriptyline[no description available]medium10organic tricyclic compound;
secondary amine		adrenergic uptake inhibitor;
analgesic;
antidepressant;
antineoplastic agent;
apoptosis inducer;
drug metabolite
promazine[no description available]medium10phenothiazines;
tertiary amine		antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
muscarinic antagonist;
phenothiazine antipsychotic drug;
serotonergic antagonist
5-bromo-4-chloro-3-indoxyl phosphate[no description available]medium10aryl phosphate;
indoles;
organobromine compound;
organochlorine compound		chromogenic compound
palladium[no description available]medium10metal allergen;
nickel group element atom;
platinum group metal atom
piperidines[no description available]medium90
cyanides[no description available]medium10pseudohalide anionEC 1.9.3.1 (cytochrome c oxidase) inhibitor
inosine triphosphate[no description available]medium10inosine phosphate;
purine ribonucleoside 5'-triphosphate		Escherichia coli metabolite;
human metabolite;
mouse metabolite
triprolidine[no description available]medium10N-alkylpyrrolidine;
olefinic compound;
pyridines		H1-receptor antagonist
ebastine[no description available]medium10organic molecular entity
acrivastine[no description available]medium10alpha,beta-unsaturated monocarboxylic acid;
N-alkylpyrrolidine;
olefinic compound;
pyridines		H1-receptor antagonist
carebastine[no description available]medium10diarylmethane
ConditionIndicatedRelationship StrengthStudiesTrials
Airway Hyper-Responsiveness0low10
Anaphylactic Reaction0low10
Anaphylactoid Reaction0low10
Anaphylactoid Shock0low10
Anaphylaxis0low10
Arrhythmia0low30
Arrhythmias, Cardiac0low30
Arrythmia0low30
Cardiac Arrhythmia0low30
Cardiac Arrhythmias0low30
Cardiac Diseases0low20
Cardiac Disorders0low20
Cardiac Dysrhythmia0low30
Dermatitis, Atopic0low10
Disease Models, Animal0low20
Eczema, Atopic0low10
Eczema, Infantile0low10
Electrocardiogram QT Prolonged0low20
Extravascular Hemolysis0low10
Haemolysis0low10
Hay Fever0low10
Hayfever0low10
Heart Diseases0low20
Heart Disorders0low20
Hemolysis0low10
Hypersensitivity, Respiratory0low10
Inflammation0low10
Innate Inflammatory Response0low10
Intravascular Hemolysis0low10
Long QT Syndrome0low20
Neurodermatitis, Atopic0low10
Neurodermatitis, Disseminated0low10
Pollen Allergy0low10
Pollinosis0low10
Respiratory Hypersensitivity0low10
Rhinitis, Allergic, Seasonal0low10
Seasonal Allergic Rhinitis0low10
Shock, Anaphylactic0low10

Research Highlights

Safety/Toxicity (2)

ArticleYear
Cardiotoxicity of new antihistamines and cisapride.
Toxicology letters, Feb-28, Volume: 127, Issue: 1-3		2002
Comparative analysis of the cardiotoxicity proclivities of second generation antihistamines in an experimental model predictive of adverse clinical ECG effects.
Arzneimittel-Forschung, Volume: 46, Issue: 2		1996
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (1)

ArticleYear
Magnetic resonance spectroscopy for measuring the biodistribution and in situ in vivo pharmacokinetics of fluorinated compounds: validation using an investigation of liver and heart disposition of tecastemizole.
Journal of clinical pharmacy and therapeutics, Volume: 31, Issue: 3		2006
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (2)

ArticleYear
Magnetic resonance spectroscopy for measuring the biodistribution and in situ in vivo pharmacokinetics of fluorinated compounds: validation using an investigation of liver and heart disposition of tecastemizole.
Journal of clinical pharmacy and therapeutics, Volume: 31, Issue: 3		2006
Cardiotoxicity of new antihistamines and cisapride.
Toxicology letters, Feb-28, Volume: 127, Issue: 1-3		2002
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]