Drug Information
| Drug General Information | Top | |||
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| Drug ID |
D00JVR
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| Former ID |
DAP000332
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| Drug Name |
Azelastine
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| Synonyms |
Azelastina; Azelastinum; Optivar; Astelin (TN); Astepro (TN); Azelastina [INN-Spanish]; Azelastine (INN); Azelastine [INN:BAN]; Azelastinum [INN-Latin]; Optivar (TN); 4-((4-Chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone hydrochloride; 4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone HCl; 4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one; 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)-phthalazinone; 4-(p-chlorobenzyl)-2-(N-methylperhydroazepinyl-(4))-1-(2H)-phthalazinone; 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one; 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one
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| Drug Type |
Small molecular drug
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| Indication | Allergic conjunctivitis [ICD-11: 9A60.02; ICD-10: H10.1] | Approved | [1], [2] | |
| Therapeutic Class |
Antiallergic Agents
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| Company |
Meda Pharmaceuticals Inc
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| Structure |
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Download2D MOL |
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| Formula |
C22H24ClN3O
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| Canonical SMILES |
CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl
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| InChI |
1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3
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| InChIKey |
MBUVEWMHONZEQD-UHFFFAOYSA-N
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| CAS Number |
CAS 58581-89-8
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| PubChem Compound ID | ||||
| PubChem Substance ID |
9970, 4503340, 7978748, 8151525, 11373087, 11484393, 11488465, 11491799, 14829436, 29221440, 46507582, 47953967, 48415598, 50010207, 50122563, 50854757, 51091808, 57321230, 81040982, 85209838, 85788529, 87245030, 87350406, 103188977, 104300096, 124893571, 125353726, 126686074, 128573214, 131344384, 134337644, 135027355, 137175390, 139157643, 152034299, 160964310, 162173200, 162876873, 163414086, 164788079, 164833138, 172912872, 174007265, 176485063, 178103698, 179116569, 179499903, 184643901, 210279616, 210281939
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| ChEBI ID |
CHEBI:2950
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| ADReCS Drug ID | BADD_D00198 ; BADD_D00199 | |||
| SuperDrug ATC ID |
R01AC03; R06AX19; S01GX07
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| SuperDrug CAS ID |
cas=058581898
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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): Eubacteriales | ||||
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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 Azelastine HCl (adjusted p-values: 7.90E-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 Azelastine HCl (adjusted p-values: 4.10E-03). | |||
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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 Azelastine HCl (adjusted p-values: 6.53E-03). | |||
| 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 Azelastine HCl (adjusted p-values: 8.44E-05). | |||
| 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: 7121). | |||
| REF 2 | Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20. | |||
| REF 3 | Extensive impact of non-antibiotic drugs on human gut bacteria. Nature. 2018 Mar 29;555(7698):623-628. | |||
| REF 4 | Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79. | |||
| REF 5 | The in vivo potency and selectivity of azelastine as an H1 histamine-receptor antagonist in human airways and skin. J Allergy Clin Immunol. 1988 Dec;82(6):1113-8. | |||
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