Drug Information

Drug General Information
Drug ID
D0Y2HR
Former ID
DAP000326
Drug Name
Astemizole
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; R 43 512; R43512; [3H]Astemizole; Alonga, Astemizol; Astemizol [INN-Spanish]; Astemizolum [INN-Latin]; HISMANAL (TN); Hismanal (TN); MJD-30; Nono-Nastizol A; Novo-mastizol A; R-43512; Ratiopharm, Astemizol; Astemizole [USAN:BAN:INN]; GNF-PF-2461; R-43-512; Astemizole (JAN/USP/INN); Hestazol, Kelp, Laridal, Retolen, Wareezol, HSBD 6799, BRN 4830190; 1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole
Drug Type
Small molecular drug
Indication Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10:J00, J30, J31.0, T78.4] Withdrawn from market [534869], [539680]
Therapeutic Class
Antiallergic Agents
Company
Janssen Pharmaceutica
Structure
Download
2D MOL

3D MOL
Formula
C28H31FN4O
InChI
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)
InChIKey
GXDALQBWZGODGZ-UHFFFAOYSA-N
CAS Number
CAS 68844-77-9
PubChem Compound ID
2247
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
SuperDrug ATC ID
R06AX11
SuperDrug CAS ID
cas=068844779
Target and Pathway
Target(s) Histamine H1 receptor Target Info Antagonist [537070], [537328]
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 534869Comparative tolerability of second generation antihistamines. Drug Saf. 1999 May;20(5):385-401.
Ref 539680(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 537070Histamine and the convulsive threshold or effectiveness of antiepileptic drugs. Przegl Lek. 2008;65(11):803-6.
Ref 537328Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells. J Pharmacol Exp Ther. 2009 Aug;330(2):403-12. Epub 2009 May 14.

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