Page last updated: 2024-09-03

tecastemizole and astemizole

tecastemizole has been researched along with astemizole in 14 studies

Compound Research Comparison

Studies
(tecastemizole)
Trials
(tecastemizole)
Recent Studies (post-2010)
(tecastemizole)
Studies
(astemizole)
Trials
(astemizole)
Recent Studies (post-2010) (astemizole)
18031,130117578

Protein Interaction Comparison

ProteinTaxonomytecastemizole (IC50)astemizole (IC50)
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)1.1
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)0.179
Bile salt export pumpHomo sapiens (human)10
Epidermal growth factor receptorHomo sapiens (human)6.057
Tyrosine-protein kinase FynHomo sapiens (human)2.847
ATP-dependent translocase ABCB1Mus musculus (house mouse)1.7
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)1.375
Muscarinic acetylcholine receptor M2Homo sapiens (human)1.409
Muscarinic acetylcholine receptor M4Homo sapiens (human)1.861
ATP-dependent translocase ABCB1Homo sapiens (human)0.9667
Cytochrome P450 3A4Homo sapiens (human)3.3
Muscarinic acetylcholine receptor M5Homo sapiens (human)0.703
Alpha-2A adrenergic receptorHomo sapiens (human)4.846
Muscarinic acetylcholine receptor M1Homo sapiens (human)1.066
Beta-3 adrenergic receptorHomo sapiens (human)8.06
D(2) dopamine receptorHomo sapiens (human)4.521
Alpha-2B adrenergic receptorHomo sapiens (human)3.839
Alpha-2C adrenergic receptorHomo sapiens (human)1.959
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)0.767
Muscarinic acetylcholine receptor M3Homo sapiens (human)0.84
ATP-dependent translocase ABCB1Mus musculus (house mouse)1.3
Substance-K receptorHomo sapiens (human)2.986
D(1A) dopamine receptorHomo sapiens (human)4.01
D(4) dopamine receptorHomo sapiens (human)6.087
Sodium-dependent noradrenaline transporter Homo sapiens (human)1.375
Histamine H2 receptorHomo sapiens (human)1.682
Alpha-1D adrenergic receptorHomo sapiens (human)0.769
5-hydroxytryptamine receptor 2AHomo sapiens (human)0.02
5-hydroxytryptamine receptor 2CHomo sapiens (human)0.179
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)0.767
Sodium-dependent serotonin transporterHomo sapiens (human)1.318
Melanocortin receptor 5Homo sapiens (human)2.263
Histamine H1 receptorHomo sapiens (human)0.014
Mu-type opioid receptorHomo sapiens (human)1.492
D(3) dopamine receptorHomo sapiens (human)0.436
Kappa-type opioid receptorHomo sapiens (human)6.616
5-hydroxytryptamine receptor 2BHomo sapiens (human)0.012
5-hydroxytryptamine receptor 6Homo sapiens (human)3.266
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)1.1
Sodium-dependent dopamine transporter Homo sapiens (human)0.998
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)0.2857
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)1.1
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)1.1
Sigma non-opioid intracellular receptor 1Homo sapiens (human)2.246

Research

Studies (14)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's2 (14.29)18.2507
2000's10 (71.43)29.6817
2010's2 (14.29)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Cavalli, A; De Ponti, F; Poluzzi, E; Recanatini, M1
Keserü, GM1
Li, J; Rajamani, R; Reynolds, CH; Tounge, BA1
Chen, X; Chong, CR; Liu, JO; Shi, L; Sullivan, DJ1
Bianucci, AM; Calderone, V; Coi, A; Massarelli, I; Testai, L1
Jia, L; Sun, H1
Caron, G; Ermondi, G; Visentin, S1
De Jonghe, S; Herdewijn, P; Moreels, L; Peigneur, S; Rozenski, J; Tian, J; Tytgat, J; Van den Steen, PE; Vandermosten, L1
De Mol, NJ; Fischer, MJ; Janssen, LH; Kok-Van Esterik, JA; Paulussen, JJ; Van der Heijden, VS1
Gong, Q; January, CT; Vorperian, VR; Zhang, S; Zhou, Z1
Brown, AM; Ficker, E; Obejero-Paz, CA; Zhao, S1
Paakkari, I1
Hefni, A; Lever, R; Moffatt, JD; Page, CP; Paul, W1
Cioc, RC; Maes, BU; Mampuys, P; Orru, RV; Ruijter, E; Vlaar, T1

Reviews

1 review(s) available for tecastemizole and astemizole

ArticleYear
Cardiotoxicity of new antihistamines and cisapride.
    Toxicology letters, 2002, Feb-28, Volume: 127, Issue:1-3

    Topics: Arrhythmias, Cardiac; Astemizole; Benzimidazoles; Butyrophenones; Cetirizine; Cisapride; Heart Diseases; Histamine H1 Antagonists; Humans; Loratadine; Piperidines; Serotonin Receptor Agonists; Terfenadine; Triprolidine

2002

Other Studies

13 other study(ies) available for tecastemizole and astemizole

ArticleYear
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
    Journal of medicinal chemistry, 2002, Aug-29, Volume: 45, Issue:18

    Topics: Anti-Arrhythmia Agents; Cation Transport Proteins; Cluster Analysis; Databases, Factual; Ether-A-Go-Go Potassium Channels; Long QT Syndrome; Models, Molecular; Molecular Conformation; Potassium Channel Blockers; Potassium Channels; Potassium Channels, Voltage-Gated; Quantitative Structure-Activity Relationship

2002
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
    Bioorganic & medicinal chemistry letters, 2003, Aug-18, Volume: 13, Issue:16

    Topics: Cation Transport Proteins; Databases, Factual; Discriminant Analysis; Ether-A-Go-Go Potassium Channels; Holography; Linear Models; Potassium Channel Blockers; Potassium Channels; Potassium Channels, Voltage-Gated; Quantitative Structure-Activity Relationship

2003
A two-state homology model of the hERG K+ channel: application to ligand binding.
    Bioorganic & medicinal chemistry letters, 2005, Mar-15, Volume: 15, Issue:6

    Topics: ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Ligands; Models, Biological; Models, Molecular; Potassium Channels, Voltage-Gated; Protein Binding; Protein Conformation

2005
A clinical drug library screen identifies astemizole as an antimalarial agent.
    Nature chemical biology, 2006, Volume: 2, Issue:8

    Topics: Animals; Antimalarials; Astemizole; Chloroquine; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Drug Resistance; Drug Resistance, Multiple; Humans; Mice; Plasmodium falciparum; Plasmodium yoelii

2006
Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation.
    European journal of medicinal chemistry, 2008, Volume: 43, Issue:11

    Topics: Amino Acid Sequence; Heart; Humans; Models, Molecular; Molecular Sequence Data; Molecular Structure; Protein Subunits; Sequence Alignment; Structure-Activity Relationship; Trans-Activators; Transcriptional Regulator ERG

2008
Support vector machines classification of hERG liabilities based on atom types.
    Bioorganic & medicinal chemistry, 2008, Jun-01, Volume: 16, Issue:11

    Topics: Animals; Arrhythmias, Cardiac; CHO Cells; Computer Simulation; Cricetinae; Cricetulus; Discriminant Analysis; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Humans; Models, Chemical; Patch-Clamp Techniques; Potassium Channel Blockers; Potassium Channels, Voltage-Gated; Predictive Value of Tests; ROC Curve

2008
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
    European journal of medicinal chemistry, 2009, Volume: 44, Issue:5

    Topics: Ether-A-Go-Go Potassium Channels; Humans; Hydrophobic and Hydrophilic Interactions; Models, Molecular; Potassium Channel Blockers; Quantitative Structure-Activity Relationship

2009
Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.
    Bioorganic & medicinal chemistry, 2017, 12-15, Volume: 25, Issue:24

    Topics: Antimalarials; Astemizole; Dose-Response Relationship, Drug; Humans; Molecular Structure; Parasitic Sensitivity Tests; Plasmodium falciparum; Structure-Activity Relationship; Transcriptional Regulator ERG

2017
Effects of the anti-allergics astemizole and norastemizole on Fc epsilon RI receptor-mediated signal transduction processes.
    European journal of pharmacology, 1997, Mar-12, Volume: 322, Issue:1

    Topics: Animals; Anti-Allergic Agents; Astemizole; Benzimidazoles; Calcium; Cell Adhesion; Cell Line; Erythrocyte Membrane; Exocytosis; Fibronectins; Hemolysis; Hypotonic Solutions; Inosine Triphosphate; Piperidines; Protein Tyrosine Phosphatases; Rats; Receptors, IgE; Signal Transduction

1997
Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole.
    Journal of cardiovascular electrophysiology, 1999, Volume: 10, Issue:6

    Topics: Astemizole; Benzimidazoles; Cation Transport Proteins; Cell Line; DNA-Binding Proteins; Dose-Response Relationship, Drug; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Histamine H1 Antagonists; Humans; Piperidines; Potassium Channel Blockers; Potassium Channels; Potassium Channels, Voltage-Gated; Terfenadine; Trans-Activators; Transcriptional Regulator ERG

1999
The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations.
    The Journal of biological chemistry, 2002, Feb-15, Volume: 277, Issue:7

    Topics: Anti-Arrhythmia Agents; Astemizole; Benzimidazoles; Binding Sites; Blotting, Western; Cation Transport Proteins; Cell Line; Cell Membrane; Cisapride; DNA-Binding Proteins; Dose-Response Relationship, Drug; Electrophysiology; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Gastrointestinal Agents; Histamine H1 Antagonists; Humans; Inhibitory Concentration 50; Ions; Long QT Syndrome; Models, Chemical; Mutagenesis, Site-Directed; Mutation; Patch-Clamp Techniques; Piperidines; Potassium Channels; Potassium Channels, Voltage-Gated; Protein Folding; Pyridines; Quaternary Ammonium Compounds; Quinidine; Structure-Activity Relationship; Trans-Activators; Transcriptional Regulator ERG

2002
Effect of tecastemizole on pulmonary and cutaneous allergic inflammatory responses.
    Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology, 2007, Volume: 37, Issue:6

    Topics: Anaphylaxis; Animals; Anti-Inflammatory Agents; Astemizole; Benzimidazoles; Cell Adhesion; Cell Adhesion Molecules; Cell Movement; Dermatitis, Atopic; Dexamethasone; Disease Models, Animal; Endothelium, Vascular; Eosinophils; Guinea Pigs; Histamine H1 Antagonists; Humans; Inflammation; Intercellular Adhesion Molecule-1; Male; Mice; Mice, Inbred BALB C; Piperidines; Receptors, Histamine H1; Respiratory Hypersensitivity; Umbilical Veins; Vascular Cell Adhesion Molecule-1

2007
Sustainable synthesis of diverse privileged heterocycles by palladium-catalyzed aerobic oxidative isocyanide insertion.
    Angewandte Chemie (International ed. in English), 2012, Dec-21, Volume: 51, Issue:52

    Topics: Astemizole; Benzimidazoles; Catalysis; Cyanides; Diamines; Guanidines; Heterocyclic Compounds; Oxidation-Reduction; Palladium; Piperidines

2012