Page last updated: 2024-09-04

desmethylastemizole and astemizole

desmethylastemizole has been researched along with astemizole in 10 studies

Compound Research Comparison

Studies
(desmethylastemizole)
Trials
(desmethylastemizole)
Recent Studies (post-2010)
(desmethylastemizole)
Studies
(astemizole)
Trials
(astemizole)
Recent Studies (post-2010) (astemizole)
12121,130117578

Protein Interaction Comparison

ProteinTaxonomydesmethylastemizole (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 (10)

TimeframeStudies, this research(%)All Research%
pre-19902 (20.00)18.7374
1990's2 (20.00)18.2507
2000's5 (50.00)29.6817
2010's0 (0.00)24.3611
2020's1 (10.00)2.80

Authors

AuthorsStudies
Janssen, M; Janssen, PA; Janssens, F; Luyckx, M; Stokbroekx, RA; Torremans, J1
Keserü, GM1
Chen, X; Chong, CR; Liu, JO; Shi, L; Sullivan, DJ1
Bianucci, AM; Calderone, V; Coi, A; Massarelli, I; Testai, L1
Jia, L; Sun, H1
Chen, K; Ding, Y; Du, D; Duan, W; Fan, S; Jiang, H; Kong, X; Li, Y; Liu, J; Liu, Y; Luo, C; Luo, Z; Min, J; Stazi, G; Valente, S; Xu, D; Zhang, N; Zhang, Y; Zhao, K; Zhu, K; Zhu, L; Zwergel, C1
Embrechts, L; Heykants, J; Woestenborghs, R1
Hoon, TJ; January, CT; Mohammad, S; Studenik, C; Vorperian, VR; Zhou, Z1
Gong, Q; January, CT; Vorperian, VR; Zhang, S; Zhou, Z1
Hsieh, Y; Kang, L; Korfmacher, WA; Lachowicz, J; Li, F; Sondey, C1

Other Studies

10 other study(ies) available for desmethylastemizole and astemizole

ArticleYear
New antihistaminic N-heterocyclic 4-piperidinamines. 2. Synthesis and antihistaminic activity of 1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-a mines.
    Journal of medicinal chemistry, 1985, Volume: 28, Issue:12

    Topics: Administration, Oral; Animals; Astemizole; Benzimidazoles; Chemical Phenomena; Chemistry; Guinea Pigs; Histamine; Histamine Antagonists; Male; p-Methoxy-N-methylphenethylamine; Piperidines; Pupil; Rats; Rats, Inbred Strains; Serotonin; Skin Tests; Structure-Activity Relationship

1985
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 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
Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction.
    Journal of medicinal chemistry, 2021, 06-24, Volume: 64, Issue:12

    Topics: Astemizole; Cell Line, Tumor; Cell Proliferation; Drug Repositioning; Enhancer of Zeste Homolog 2 Protein; Enzyme Inhibitors; Humans; Molecular Docking Simulation; Molecular Structure; Polycomb Repressive Complex 2; Protein Binding; Structure-Activity Relationship

2021
Simultaneous determination of astemizole and its demethylated metabolite in animal plasma and tissues by high-performance liquid chromatography.
    Journal of chromatography, 1983, Dec-09, Volume: 278, Issue:2

    Topics: Animals; Astemizole; Benzimidazoles; Chromatography, High Pressure Liquid; Dealkylation; Dogs; Humans; Kinetics; Male

1983
Torsade de pointes with an antihistamine metabolite: potassium channel blockade with desmethylastemizole.
    Journal of the American College of Cardiology, 1996, Nov-15, Volume: 28, Issue:6

    Topics: Aged; Aged, 80 and over; Animals; Astemizole; Electrocardiography; Female; Heart; Heart Arrest; Histamine H1 Antagonists; Humans; Potassium Channels; Rabbits; Torsades de Pointes

1996
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
MALDI-tandem mass spectrometry imaging of astemizole and its primary metabolite in rat brain sections.
    Bioanalysis, 2009, Volume: 1, Issue:2

    Topics: Animals; Astemizole; Brain Chemistry; Cerebral Ventricles; Chromatography, High Pressure Liquid; Diagnostic Imaging; Histamine H1 Antagonists, Non-Sedating; Rats; Spectrometry, Mass, Electrospray Ionization; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization

2009