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H1 receptor

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 262

Nomenclature: H1 receptor

Family: Histamine receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 487 3p25.3 HRH1 histamine receptor H1 17-18,26,49,69
Mouse 7 488 6 53.05 cM Hrh1 histamine receptor H1 38
Rat 7 486 4q42 Hrh1 histamine receptor H 1 24
Previous and Unofficial Names Click here for help
H1R | HH1R | Hisr
Database Links Click here for help
Specialist databases
GPCRDB hrh1_human (Hs), hrh1_mouse (Mm), hrh1_rat (Rn)
Other databases
ChEMBL Target CHEMBL231 (Hs), CHEMBL4322 (Mm), CHEMBL4701 (Rn)
DrugBank Target P35367 (Hs)
Ensembl Gene ENSG00000196639 (Hs), ENSMUSG00000053004 (Mm), ENSRNOG00000007420 (Rn)
Entrez Gene 3269 (Hs), 15465 (Mm), 24448 (Rn)
Human Protein Atlas ENSG00000196639 (Hs)
KEGG Gene hsa:3269 (Hs), mmu:15465 (Mm), rno:24448 (Rn)
OMIM 600167 (Hs)
Pharos P35367 (Hs)
RefSeq Nucleotide NM_000861 (Hs), NM_008285 (Mm), NM_017018 (Rn)
RefSeq Protein NP_000852 (Hs), NP_032311 (Mm), NP_058714 (Rn)
SynPHARM 2980 (in complex with doxepin)
9220 (in complex with [11C]doxepin)
UniProtKB P35367 (Hs), P70174 (Mm), P31390 (Rn)
Wikipedia HRH1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Histamine H1 receptor in complex with antagonist
PDB Id:  3RZE
Ligand:  doxepin
Resolution:  3.1Å
Species:  Human
References:  84
Natural/Endogenous Ligands Click here for help
histamine

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
dimethylhistaprodifen Small molecule or natural product Hs Full agonist 6.4 pKi 83
⤷ pKi 6.4 [83]
methylhistaprodifen Small molecule or natural product Hs Full agonist 6.4 pKi 83
⤷ pKi 6.4 (Ki 3.98x10-7 M) [83]
ST-1006 Small molecule or natural product Click here for species-specific activity table Hs Agonist <6.0 pKi 76
⤷ pKi <6.0 (Ki >1x10-6 M) [76]
2-(3-iodophenyl)histamine Small molecule or natural product Hs Full agonist 5.8 pKi 83
⤷ pKi 5.8 [83]
2-(3-bromophenyl)histamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.7 pKi 83
⤷ pKi 5.7 [83]
2-(3-chlorophenyl)histamine Small molecule or natural product Hs Full agonist 5.7 pKi 83
⤷ pKi 5.7 [83]
histaprodifen Small molecule or natural product Hs Full agonist 5.7 pKi 52
⤷ pKi 5.7 [52]
2-(2-thiazolyl)ethanamine Small molecule or natural product Hs Partial agonist 5.3 pKi 83
⤷ pKi 5.3 [83]
histamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 4.7 – 5.9 pKi 8,69,79,83,92
⤷ pKi 4.7 – 5.9 [8,69,79,83,92]
UR-PG55B Small molecule or natural product Hs Full agonist 5.2 pKi 92
⤷ pKi 5.2 [92]
UR-PG131A Small molecule or natural product Hs Full agonist 4.7 pKi 92
⤷ pKi 4.7 [92]
UR-PG153 Small molecule or natural product Hs Full agonist 4.7 pKi 92
⤷ pKi 4.7 [92]
oxo-arpromidine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.5 pKi 92
⤷ pKi 4.5 [92]
UR-PG146 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.4 pKi 92
⤷ pKi 4.4 [92]
2-pyridylethylamine Small molecule or natural product Immunopharmacology Ligand Hs Full agonist 3.7 pKi 79
⤷ pKi 3.7 [79]
vilazodone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist 6.5 pIC50 34
⤷ pIC50 6.5 (IC50 3.17x10-7 M) [34]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[11C]doxepin Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Antagonist 9.0 pKd 40
⤷ pKd 9.0 (Kd 1x10-9 M) [40]
[3H]pyrilamine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Inverse agonist 8.4 – 9.1 pKd 18,69,82-83
⤷ pKd 8.4 – 9.1 (Kd 4x10-9 – 7.9x10-10 M) [18,69,82-83]
tripelennamine Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Antagonist 8.0 pKd 33
⤷ pKd 8.0 (Kd 1x10-8 M) [33]
clemastine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 10.3 pKi 3
⤷ pKi 10.3 (Ki 4.9x10-11 M) [3]
cyproheptadine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 10.2 pKi 69
⤷ pKi 10.2 [69]
asenapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 9.8 pKi 82
⤷ pKi 9.8 [82]
doxepin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 9.5 – 10.0 pKi 8
⤷ pKi 9.5 – 10.0 [8]
promethazine Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 9.6 pKi 28
⤷ pKi 9.6 (Ki 2.4x10-10 M) [28]
amitriptyline Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 9.3 pKi 28
⤷ pKi 9.3 (Ki 5x10-10 M) [28]
Description: Antagonism of [3H]mepyramine binding
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.8 – 9.6 pKi 8,46,82
⤷ pKi 8.8 – 9.6 [8,46,82]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 9.2 pKi 82
⤷ pKi 9.2 [82]
alimemazine Small molecule or natural product Approved drug Immunopharmacology Ligand Bt Antagonist 9.1 pKi 47
⤷ pKi 9.1 (Ki 7.2x10-10 M) [47]
Description: Inhibition of [3H]mepyramine binding to bovine brain membrane preparations in vitro.
desloratadine Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Antagonist 9.0 pKi 50
⤷ pKi 9.0 (Ki 9.7x10-10 M) [50]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.7 – 9.2 pKi 46,82
⤷ pKi 8.7 – 9.2 [46,82]
azelastine Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 8.9 pKi 78
⤷ pKi 8.9 (Ki 1.26x10-9 M) [78]
mepyramine Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Inverse agonist 8.7 – 9.0 pKi 8,79
⤷ pKi 8.7 – 9.0 [8,79]
triprolidine Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 8.5 – 9.0 pKi 8,69
⤷ pKi 8.5 – 9.0 (Ki 3.16x10-9 – 1x10-9 M) [8,69]
(-)-trans-H2-PAT Small molecule or natural product Hs Antagonist 8.6 – 8.8 pKi 8
⤷ pKi 8.6 – 8.8 [8]
hydroxyzine Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Antagonist 8.7 pKi 30
⤷ pKi 8.7 (Ki 1.99x10-9 M) [30]
ketotifen Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 8.6 pKi 48
⤷ pKi 8.6 (Ki 2.5x10-9 M) [48]
mizolastine Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Antagonist 8.6 pKi 13
⤷ pKi 8.6 (Ki 2.7x10-9 M) [13]
Description: Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer.
astemizole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.5 pKi 77
⤷ pKi 8.5 (Ki 3x10-9 M) [77]
(±)-trans-H2-PAT Small molecule or natural product Hs Antagonist 8.4 – 8.6 pKi 8
⤷ pKi 8.4 – 8.6 [8]
(R)-cetirizine Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inverse agonist 8.5 pKi 79
⤷ pKi 8.5 [79]
(+)-chlorpheniramine Small molecule or natural product Hs Antagonist 8.3 – 8.6 pKi 8,69
⤷ pKi 8.3 – 8.6 [8,69]
thiothixene Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.4 pKi 46
⤷ pKi 8.4 [46]
dosulepin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.4 pKi 86
⤷ pKi 8.4 (Ki 4x10-9 M) [86]
quetiapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.0 – 8.7 pKi 46,82
⤷ pKi 8.0 – 8.7 [46,82]
cyclizine Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 8.4 pKi 3
⤷ pKi 8.4 (Ki 4.44x10-9 M) [3]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.2 pKi 46
⤷ pKi 8.2 [46]
loxapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.2 pKi 46
⤷ pKi 8.2 [46]
cetirizine Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Inverse agonist 8.2 pKi 69
⤷ pKi 8.2 [69]
chlorpheniramine Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 8.1 pKi 78
⤷ pKi 8.1 (Ki 7x10-9 M) [78]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.1 pKi 46
⤷ pKi 8.1 [46]
(±)-cis-H2-PAT Small molecule or natural product Hs Antagonist 7.8 – 8.2 pKi 8
⤷ pKi 8.1 – 8.2 [8]
pKi 7.8 – 7.9 [8]
fluspirilene Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.9 pKi 82
⤷ pKi 7.9 [82]
diphenhydramine Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Antagonist 7.9 pKi 8
⤷ pKi 7.9 [8]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.6 – 7.8 pKi 46,82
⤷ pKi 7.6 – 7.8 [46,82]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.7 pKi 46
⤷ pKi 7.7 [46]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.7 pKi 46
⤷ pKi 7.7 [46]
ziprasidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.4 – 7.8 pKi 46,82
⤷ pKi 7.4 – 7.8 [46,82]
fexofenadine Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Antagonist 7.6 pKi 2
⤷ pKi 7.6 (Ki 2.7x10-8 M) [2]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.5 pKi 46
⤷ pKi 7.5 [46]
9-OH-risperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 82
⤷ pKi 7.5 [82]
AZD3778 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 5
⤷ pKi 7.5 (Ki 3.16x10-8 M) [5]
Description: Assayed using the sodium salt of the compound
(+)-trans-H2-PAT Small molecule or natural product Hs Antagonist 7.4 – 7.5 pKi 8
⤷ pKi 7.4 – 7.5 [8]
loratadine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 7.4 pKi 43
⤷ pKi 7.4 (Ki 3.7x10-8 M) [43]
terfenadine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 7.4 pKi 2
⤷ pKi 7.4 (Ki 4x10-8 M) [2]
trifluoperazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.2 pKi 46
⤷ pKi 7.2 [46]
(S)-dimetindene Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 7.2 pKi 11
⤷ pKi 7.2 (Ki 6.9x10-8 M) [11]
rupatadine Small molecule or natural product Approved drug Immunopharmacology Ligand Cp Antagonist 7.0 pKi 63
⤷ pKi 7.0 (Ki 1x10-7 M) [63]
Description: [3H]-pyrilamine binding to guinea pig cerebellum membranes.
sertindole Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.9 pKi 46,82
⤷ pKi 6.9 [46,82]
(+)-cis-H2-PAT Small molecule or natural product Hs Antagonist 6.9 pKi 8
⤷ pKi 6.9 [8]
(S)-cetirizine Small molecule or natural product Ligand has a PDB structure Hs Inverse agonist 6.7 pKi 79
⤷ pKi 6.7 [79]
BU-E 47 Small molecule or natural product Hs Antagonist 6.6 pKi 83
⤷ pKi 6.6 [83]
(-)-chlorpheniramine Small molecule or natural product Hs Antagonist 6.4 – 6.7 pKi 8
⤷ pKi 6.4 – 6.7 [8]
arpromidine Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.5 pKi 83,92
⤷ pKi 6.5 [83,92]
pimozide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.2 pKi 46
⤷ pKi 6.2 [46]
JNJ-39758979 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist <6.0 pKi 76
⤷ pKi <6.0 (Ki >1x10-6 M) [76]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.7 – 6.1 pKi 46,82
⤷ pKi 5.7 – 6.1 [46,82]
ABT-239 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 5.8 pKi 22
⤷ pKi 5.8 [22]
pitolisant Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.8 pKi 76
⤷ pKi 5.8 [76]
molindone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.7 pKi 46
⤷ pKi 5.7 [46]
pipamperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 pKi 82
⤷ pKi 5.6 [82]
A-349821 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 5.6 pKi 21
⤷ pKi 5.6 [21]
clobenpropit Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 5.6 pKi 23
⤷ pKi 5.6 [23]
A-317920 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 pKi 21,23
⤷ pKi 5.4 [21,23]
impromidine Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 5.2 pKi 92
⤷ pKi 5.2 [92]
ciproxifan Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 76
⤷ pKi <5.0 (Ki >1x10-5 M) [76]
MK-0249 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 76
⤷ pKi <5.0 (Ki >1x10-5 M) [76]
conessine Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 76
⤷ pKi <5.0 (Ki >1x10-5 M) [76]
INCB-38579 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <5.0 pKi 76
⤷ pKi <5.0 (Ki >1x10-5 M) [76]
rupatadine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 8.4 pIC50 72
⤷ pIC50 8.4 (IC50 3.9x10-9 M) [72]
epinastine Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Antagonist 7.6 pIC50 36
⤷ pIC50 7.6 (IC50 2.5x10-8 M) [36]
Description: Antagonism of 5 nM [3H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells.
tripelennamine Small molecule or natural product Approved drug Primary target of this compound Immunopharmacology Ligand Hs Antagonist 7.4 pIC50 33
⤷ pIC50 7.4 (IC50 3.98x10-8 M) [33]
mizolastine Small molecule or natural product Approved drug Immunopharmacology Ligand Cp Antagonist 7.3 pIC50 6
⤷ pIC50 7.3 (IC50 4.7x10-8 M) [6]
Description: Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections.
[11C]pyrilamine Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Inverse agonist - -
⤷
View species-specific antagonist tables
Antagonist Comments
Astemizole is highly selective for the histamine H1 receptor over the H2 receptor.
Immunopharmacology Comments
The H1 receptor was the first of the family to be targeted for clinical use, with antagonists (anti-histamines) developed that are still used widely to treat allergic inflammation such as rhinitis, allergic conjunctivitis, urticaria and even anaphylaxis.
Cell Type Associations
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   eosinophil (CL:0000771)
Comment:  Eosinophils express all four histamine receptor subtypes.
References:  29,64
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  In humans, mast cells express H1R, H2R and H4R.
References:  27
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0006954 inflammatory response TAS
click arrow to show/hide IEA associations
GO:0048245 eosinophil chemotaxis IEA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0048245 eosinophil chemotaxis IEA
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Adenylyl cyclase stimulation
Comments:  Stimulation of cAMP accumulation is via Gβγ subunits of Gq [58].
References:  58
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  51
Tissue Distribution Click here for help
Brain: cerebrum.
Heart: myocardium (ventricle > atrium).
Species:  Human
Technique:  Northern and Western blotting.
References:  62
Brain.
Species:  Human
Technique:  Positron emission tomography (PET).
References:  68
Cranial arteries.
Species:  Human
Technique:  RT-PCR.
References:  42
Myometrium.
Species:  Human
Technique:  Radioligand binding.
References:  31
Gastrointestinal tract.
Species:  Human
Technique:  qRT-PCR and immunohistochemistry.
References:  80
Uterine horns.
Species:  Mouse
Technique:  Radioligand binding.
References:  32
Mast cells.
Species:  Mouse
Technique:  RT-PCR.
References:  37
Sympathetic preganglionic neurons in the spinal cord.
Species:  Rat
Technique:  RT-PCR.
References:  90
Embryonic brain and spinal cord.
Species:  Rat
Technique:  in situ hybridization, RT-PCR and Northern blotting.
References:  45
Brain: cerebrum.
Heart: myocardium (atrium and ventricle).
Species:  Rat
Technique:  Northern and Western blotting.
References:  62
Cochlea.
Species:  Rat
Technique:  RT-PCR.
References:  4
Expression Datasets Click here for help

Show »

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of IP levels in COS-7 cells transfected with the human H1 receptor.
Species:  Human
Tissue:  COS-7 cells.
Response measured:  Stimulation of IP formation.
References:  17
Measurement of IP levels in CHO cells transfected with the human H1 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of IP formation.
References:  8
Measurement of AC activity in baculovirus-infected Sf9 insect cells expressing the human H1 receptor.
Species:  Human
Tissue:  Sf9 cells.
Response measured:  Stimulation of AC activity.
References:  92
Measurement of cAMP levels in CHO cells transfected with the human H1 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of cAMP accumulation.
References:  58
Measurement of PLC activity and Ca2+ mobilisation in cultured ciliary muscle cells endogenously expressing the H1 receptor.
Species:  Human
Tissue:  Cultured ciliary muscle cells.
Response measured:  Activation of PLC and mobilisation of both intracellular and extracellular Ca2+.
References:  56
Measurement of IP levels in cultured human endothelial cells endogenously expressing the H1 receptor.
Species:  Human
Tissue:  Cultured umbilical vein endothelial cells.
Response measured:  Stimulation of IP formation.
References:  53
Measurement of mitogenesis in human astrocytoma U373 MG cells endogenously expressing the H1 receptor.
Species:  Human
Tissue:  Astrocytoma U373 MG cells.
Response measured:  Cell proliferation via PKC and MAPK.
References:  35
Measurement of Ca2+ levels as well as ERK1/2 and PKC activity in human primary epithelial cells and the NCI-H292 cell line, both endogenously expressing the H1 receptor.
Species:  Human
Tissue:  Primary epithelial cells and the NCI-H292 cell line.
Response measured:  Elevation of Ca2+ levels and activation of PKC and ERK1/2.
References:  61
Measurement of IP, DAG and Ca2+ levels in human HeLa carcinoma cells endogenously expressing the H1 receptor.
Species:  Human
Tissue:  HeLa carcinoma cells.
Response measured:  Formation of IP and DAG and a rise in Ca2+ levels.
References:  88
Physiological Functions Click here for help
Relaxation of smooth muscle (via an endothelial H1 receptor).
Species:  Human
Tissue:  Cranial arteries.
References:  42
Contraction of smooth muscle.
Species:  Human
Tissue:  Arterial rings.
References:  16
Modulation of adrenergic neurotransmission.
Species:  Rat
Tissue:  Vas deferens.
References:  89
Bronchoconstriction.
Species:  Human
Tissue:  In vivo.
References:  12,14,19,54,73,87
Inhibition of locomotor behaviour.
Species:  Rat
Tissue:  In vivo.
References:  1
Modulation of feeding behaviour.
Species:  Rat
Tissue:  In vivo.
References:  25
Modulation of feeding behaviour.
Species:  Mouse
Tissue:  In vivo.
References:  59-60,70-71
Hypernociception.
Species:  Rat
Tissue:  In vivo.
References:  55
Endothelium-dependent vasodilation.
Species:  Rat
Tissue:  Mesenteric vascular beds.
References:  44
Role in the stimulation of skin blood flow during whole body heating.
Species:  Human
Tissue:  In vivo.
References:  91
Stimulation of the nitric oxide signalling system.
Species:  Rat
Tissue:  Submandibular gland.
References:  9
Increased vascular permeability.
Species:  Mouse
Tissue:  In vivo.
References:  7,74
Modulation of neuronal firing.
Species:  Rat
Tissue:  Dorsal raphe nucleus.
References:  10
Contraction of smooth muscle.
Species:  Human
Tissue:  Isolated uterine strips.
References:  57
Contraction of smooth muscle.
Species:  Rat
Tissue:  Isolated stomach fundus.
References:  20
Increase in substantia nigra pars reticulata (SNr) inhibitory projection neuron firing frequency (via cell depolarisation).
The balance between the effect of H1 and H2 receptors and the opposing effect of H3 receptors may contribute to movement control.
Species:  Mouse
Tissue:  Coronal midbrain slices.
References:  95
Depolarisation.
Species:  Rat
Tissue:  Sympathetic preganglionic neurons.
References:  90
Regulation of cytokine production.
Species:  Mouse
Tissue:  CD4+ and CD8+ T cells.
References:  85
Prostacyclin formation.
Species:  Human
Tissue:  Pulmonary artery.
References:  81
Physiological Consequences of Altering Gene Expression Click here for help
H1 receptor knockout mice develop normally, but exhibit impaired locomotor activity and exploratory behavior.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  39,94
H1 receptor knockout mice subjected to social isolation after weaning exhibit similar levels of locomotor activity to socially reared H1 receptor knockout mice. This is in contrast to wild-type mice, where there is a significant decrease in locomotor activity in socially isolated WT mice compared with socially reared WT mice. It is suggested that blockade of H1 receptors by atypical antipsychotics attenuates social isolation-induced behavioral changes.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  15
H1 receptor knockout mice exhibit decreased exploratory activity, reduced levels of anxiety and aggression, a decrease in nociceptive response and an increased 5-HT turnover rate in the cerebral cortex and hippocampus.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  93
H1 receptor knockout mice exhibit a significant decrease in nociception compared to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  66
H1 knockout mice exhibit enhancement of morphine-induced antinociception.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  65
H1 receptor knockout mice do not exhibit an increase in respiratory frequency upon elevation of body temperature, as observed in wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  41
H1 receptor knockout mice exhibit a reduction in the effect of neurotensin on the supression of food intake.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  75
H1 receptor knockout mice do not exhibit an increase in vascular permeability of the conjunctiva, as observed in wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  74
CD4+ T cells from H1 receptor knockout mice exhibit a decrease in the release of Il-2 and Il-10, and an increase in the release of IL-4. CD8+ T cells from H1 receptor knockout mice also exhibit a decrease in the release of Il-2 and Il-10, as well as an increase in the release of IFN-γ.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  85
H1 receptor knockout mice exhibit enhanced antinociception by administration of orexin-A, compared to wild-type mice following administration of orexin-A.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  67
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6		 MGI:107619  MP:0004924 abnormal behavior PMID: 8917588 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6		 MGI:107619  MP:0001502 abnormal circadian rhythm PMID: 8917588 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1		 MGI:107619  MP:0003638 abnormal response/metabolism to endogenous compounds PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6		 MGI:107619  MP:0005093 decreased B cell proliferation PMID: 9989982 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1		 MGI:107619  MP:0001262 decreased body weight PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1		 MGI:107619  MP:0002727 decreased circulating insulin level PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1		 MGI:107619  MP:0003910 decreased eating behavior PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6		 MGI:107619  MP:0001417 decreased exploration in new environment PMID: 8917588 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6		 MGI:107619  MP:0008498 decreased IgG3 level PMID: 9989982 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6		 MGI:107619  MP:0001806 decreased IgM level PMID: 9989982 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1		 MGI:107619  MP:0001876 decreased inflammatory response PMID: 16680192 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6		 MGI:107619  MP:0008567 decreased interferon-gamma secretion PMID: 9989982 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1		 MGI:107619  MP:0008567 decreased interferon-gamma secretion PMID: 16680192 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1		 MGI:107619  MP:0008673 decreased interleukin-13 secretion PMID: 16680192 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6		 MGI:107619