Therapeutic Targets Database
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TTD Target ID: TTDS00086

Target Information
NameHistamine H1 receptor    
Type of targetSuccessful target    
SynonymsH1 Histamine receptor    
Histamine receptor 1    
DiseaseAcute lymphoblastic leukaemia (therapy-refractory)    [1]
Allergic diseases    [2]
Allergic rhinitis, unspecified    [3]
Anxiety disorder, unspecified    [4]
Chronic rhinitis    [5]
Chronic urticaria    [5]
Epidermal hyperplasia    [6]
Epilepsy    [7]
Hypotension    [8]
Intimal hyperplasia    [9]
Ischemia    [10]
Motion sickness    [11]
Nausea and vomiting    [12]
Seasonal allergic rhinitis    [5]
Systemic arterial vasodilation    [13]
Drug(s)(S)-(+)-Dimethindene maleateApprovedPruritus[14][15][16][10]
AceprometazineApprovedSleep disorders[17]
AcrivastineApprovedAllergic rhinitis[18][5]
AlcaftadineApprovedAllergic conjunctivitis[19]
AntazolineApprovedNasal congestion[20][21][22][5]
Antazoline hydrochlorideApprovedOcular allergies[20][21][22]
Antazoline phosphateApprovedOcular allergies[20][21][22]
AstemizoleApprovedAllergic rhinitis[23][20]
AzatadineApprovedAllergic rhinitis[24]
AzelastineApprovedAllergic conjunctivitis[25][26]
BepotastineApprovedAllergic rhinitis and uriticaria/puritus[27]
Bepotastine besilateApprovedAllergic conjunctivitis[28][29]
BromodiphenhydramineApprovedHay fever[30]
BrompheniramineApprovedAllergic rhinitis[31]
BuclizineApprovedNausea and vomiting[32]
CarbinoxamineApprovedAllergic rhinitis[33]
CetirizineApprovedAllergic rhinitis[34][35]
ChlorpheniramineApprovedAllergic rhinitis and uriticaria[25][3][10]
CinnarizineApprovedVertigo/meniere's disease[11][37]
ClemastineApprovedAllergic rhinitis[38][39]
CyclizineApprovedNausea and vomiting[40][12][41]
DesloratadineApprovedAllergic rhinitis[44][45]
DexbrompheniramineApprovedHay fever[46]
DimenhydrinateApprovedNausea and vomiting[47][4]
DimethindeneApprovedRespiratory allergies[14][15][16][10]
Dimethindene maleateApprovedRespiratory allergies[14][15][16][10]
DiphenhydramineApprovedVertigo/Meniere's disease[25][1]
DiphenylpyralineApprovedAllergic rhinitis[48]
DoxylamineApprovedAnxiety and morning sickness[50][51]
EmedastineApprovedAllergic conjunctivitis[52]
EpinastineApprovedAllergic conjunctivitis[53]
ErgotidineApprovedRespiratory allergies[54]
FexofenadineApprovedAllergic rhinitis[45][35]
HydroxyzineApprovedAnxiety disorder[55][56]
KetotifenApprovedAllergic conjunctivitis[25][7]
LevocabastineApprovedAllergic conjunctivitis[57][58]
Levocetirizine dihydrochlorideApprovedAllergic rhinitis[45][25][7]
Mepyramine maleateApprovedAllergies[62][63][34]
MequitazineApprovedAllergic rhinitis[64]
MethdilazineApprovedAllergic rhinitis[65]
MizolastineApprovedAllergic rhinitis[66]
OlopatadineApprovedAllergic conjunctivitis[67]
OxatomideApprovedHay fever[25][58]
PemirolastApprovedAllergic conjunctivitis[68]
PhenindamineApprovedCommon Cold and Allergies[69]
PheniramineApprovedHay fever[70]
PromethazineApprovedAllergic disorders, itching, nausea and vomiting[25][10]
TrimeprazineApprovedAllergic rhinitis[73]
TriprolidineApprovedHay fever[77]
TranilastMarketedOcular allergy[29]
Bepotastine besilatePhase IIIOcular allergy[28][29]
CarebastinePhase IIIOcular allergy[29]
OlopatadinePhase IIIOcular allergy[29]
GSK1004723Suspended in Phase II in GSK 2009 ReportAllergic rhinitis[78]
GSK835726Suspended in Phase II in GSK 2009 ReportAllergic rhinitis[78]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
UniProt IDP35367
FunctionIn peripheral tissues, the h1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neuro.    
Related US Patent6,506,756
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Antagonist (S)-[14][15][16][10]
Antazoline hydrochloride[20][21][22]
Antazoline phosphate[20][21][22]
Bepotastine besilate[28][29]
Dimethindene maleate[14][15][16][10]
Levocetirizine dihydrochloride[45][25][7]
Mepyramine maleate[62][63][34]
Pyrilamine Maleate[25][10]
Sch 37370[88]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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