Drug Information

Drug General Information
Drug ID
D00JVR
Former ID
DAP000332
Drug Name
Azelastine
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
Drug Type
Small molecular drug
Indication Allergic conjunctivitis [ICD9: 204.0, 372.0, 372.14, 995.3; ICD10:C91.0, H10, H10.45, T78.4] Approved [536119], [542129]
Therapeutic Class
Antiallergic Agents
Company
Meda Pharmaceuticals Inc
Structure
Download
2D MOL

3D MOL
Formula
C22H24ClN3O
InChI
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
InChIKey
MBUVEWMHONZEQD-UHFFFAOYSA-N
CAS Number
CAS 58581-89-8
PubChem Compound ID
2267
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
SuperDrug ATC ID
R01AC03; R06AX19; S01GX07
SuperDrug CAS ID
cas=058581898
Target and Pathway
Target(s) Histamine H1 receptor Target Info Antagonist [536700], [537714]
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
Ref 536119Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
Ref 542129(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 536700Intact 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. Epub 2008 Apr 29.
Ref 537714The 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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