Drug Information
| Drug General Information | Top | |||
|---|---|---|---|---|
| Drug ID |
D0Y2HR
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| Former ID |
DAP000326
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| Drug Name |
Astemizole
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| Synonyms |
Alermizol; Astemina; Astemisan; Astemisol; Astemison; Astemizol; Astemizolum; Astesen; Emdar; Esmacen; Fustermizol; Hestazol; Hismanal; Histamen; Histaminos; Histazol; Hubermizol; Kelp; Laridal; Metodih; Metodik; Paralergin; Retolen; Rifedot; Rimbol; Romadin; Simprox; Urdrim; Wareezol; Waruzol; AlacanBrand of Astemizole; Alonga Brand of Astemizole; Astemizol Alonga; Astemizol [German]; Astemizol ratiopharm; Astemizole Alacan Brand; Astemizole Alonga Brand; Astemizole Byk Brand; Astemizole Diba Brand; Astemizole Elfar Brand; Astemizole Esteve Brand; Astemizole Fustery Brand; Astemizole ICN Brand; Astemizole Janssen Brand; Astemizole Lesvi Brand; Astemizole McNeil Brand; Astemizole Medinsa Brand; Astemizole Merck Brand; Astemizole Senosiain Brand; Astemizole Septa Brand; Astemizole Smaller Brand; Astemizole Urbion Brand; Astemizole Vita Brand; Astemizole ratiopharm Brand; Byk Brand of Astemizole; Diba Brand of Astemizole; Elfar Brand of Astemizole; Esteve Brand of Astemizole; Fustery Brand of Astemizole; ICN Brand of Astemizole; Janssen Brand of Astemizole; Lesvi Brand of Astemizole; McNeil Brand of Astemizole; Medinsa Brand of Astemizole; Merck Brand of Astemizole; Ratiopharm Brand of Astemizole; Reig Jofre Brand of Astemizole; Senosiain Brand of Astemizole; Septa Brand of Astemizole; Smaller Brand of Astemizole; Urbion Brand of Astemizole; Vita Brand of Astemizole; R 42512; [3H]Astemizole; Alonga, Astemizol; Astemizol [INN-Spanish]; Astemizolum [INN-Latin]; HISMANAL (TN); Hismanal (TN); MJD-30; Nono-Nastizol A; Novo-mastizol A; Ratiopharm, Astemizol; Astemizole [USAN:BAN:INN]; GNF-PF-2461; Astemizole (JAN/USP/INN); Hestazol, Kelp, Laridal, Retolen, Wareezol, HSBD 6799, BRN 4830190; 1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole
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| Drug Type |
Small molecular drug
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| Indication | Allergic rhinitis [ICD-11: CA08.0] | Withdrawn from market | [1], [2] | |
| Therapeutic Class |
Antiallergic Agents
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| Company |
Janssen Pharmaceutica
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| Structure |
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Download2D MOL |
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| Formula |
C28H31FN4O
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| Canonical SMILES |
COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
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| InChI |
1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)
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| InChIKey |
GXDALQBWZGODGZ-UHFFFAOYSA-N
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| CAS Number |
CAS 68844-77-9
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| PubChem Compound ID | ||||
| PubChem Substance ID |
9050, 459037, 855746, 4266413, 5313663, 7847301, 7978732, 8150150, 8151518, 10321136, 11112828, 11335214, 11360453, 11363342, 11365904, 11368466, 11372003, 11374824, 11376628, 11461425, 11466164, 11467284, 11485540, 11485887, 11489548, 11490887, 11493037, 11494262, 11528621, 11538010, 12013338, 14760289, 22391432, 26613163, 26680817, 26746979, 26746980, 26751496, 26751497, 29221421, 46487928, 46508569, 47216611, 47440072, 47515146, 47736292, 47810587, 47885241, 48034934, 48259050
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| ChEBI ID |
CHEBI:2896
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| SuperDrug ATC ID |
R06AX11
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| SuperDrug CAS ID |
cas=068844779
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| Interaction between the Drug and Microbe | Top | |||
|---|---|---|---|---|
| The Abundace of Studied Microbe(s) Regulated by Drug | ||||
| The Order in the Taxonomic Hierarchy of the following Microbe(s): Bacteroidales | ||||
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Studied Microbe: Prevotella copri
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[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Prevotella copri was decreased by Astemizole (adjusted p-values: 7.61E-03). | |||
| The Order in the Taxonomic Hierarchy of the following Microbe(s): Eubacteriales | ||||
|
Studied Microbe: Blautia obeum
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|
[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Blautia obeum was decreased by Astemizole (adjusted p-values: 6.39E-05). | |||
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Studied Microbe: Coprococcus comes
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|
[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Coprococcus comes was decreased by Astemizole (adjusted p-values: 5.02E-03). | |||
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Studied Microbe: Dorea formicigenerans
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|
[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Dorea formicigenerans was decreased by Astemizole (adjusted p-values: 3.58E-04). | |||
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Studied Microbe: Eubacterium eligens
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|
[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Eubacterium eligens was decreased by Astemizole (adjusted p-values: 2.06E-03). | |||
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Studied Microbe: Eubacterium rectale
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|
[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Eubacterium rectale was decreased by Astemizole (adjusted p-values: 9.66E-04). | |||
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Studied Microbe: Roseburia intestinalis
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|
[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Roseburia intestinalis was decreased by Astemizole (adjusted p-values: 9.30E-04). | |||
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Studied Microbe: Ruminococcus gnavus
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|
[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Ruminococcus gnavus was decreased by Astemizole (adjusted p-values: 9.20E-04). | |||
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Studied Microbe: Ruminococcus torques
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|
[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Ruminococcus torques was decreased by Astemizole (adjusted p-values: 5.37E-04). | |||
| The Order in the Taxonomic Hierarchy of the following Microbe(s): Verrucomicrobiales | ||||
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Studied Microbe: Akkermansia muciniphila
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|
[3] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Akkermansia muciniphila was decreased by Astemizole (adjusted p-values: 5.39E-04). | |||
| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Histamine H1 receptor (H1R) | Target Info | Antagonist | [4], [5] |
| KEGG Pathway | Calcium signaling pathway | |||
| Neuroactive ligand-receptor interaction | ||||
| Inflammatory mediator regulation of TRP channels | ||||
| Panther Pathway | Histamine H1 receptor mediated signaling pathway | |||
| Reactome | Histamine receptors | |||
| G alpha (q) signalling events | ||||
| WikiPathways | Monoamine GPCRs | |||
| GPCRs, Class A Rhodopsin-like | ||||
| IL-4 Signaling Pathway | ||||
| Gastrin-CREB signalling pathway via PKC and MAPK | ||||
| GPCR ligand binding | ||||
| GPCR downstream signaling | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2603). | |||
| REF 2 | Comparative tolerability of second generation antihistamines. Drug Saf. 1999 May;20(5):385-401. | |||
| REF 3 | Extensive impact of non-antibiotic drugs on human gut bacteria. Nature. 2018 Mar 29;555(7698):623-628. | |||
| REF 4 | Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells. J Pharmacol Exp Ther. 2009 Aug;330(2):403-12. | |||
| REF 5 | Histamine and the convulsive threshold or effectiveness of antiepileptic drugs. Przegl Lek. 2008;65(11):803-6. | |||
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