Nomenclature: H1 receptor

Family: Histamine receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates. 

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 487 3p25 HRH1 histamine receptor H1 11-12,20,33,51
Mouse 7 488 6 E3 Hrh1 histamine receptor H1 25
Rat 7 486 4q42 Hrh1 histamine receptor H 1 18
Previous and Unofficial Names
Hisr
H1R
HH1R
Histamine receptor H1
histamine H1 receptor
histamine receptor H 1
Bphs
Hir
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Selected 3D Structures
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:  63
Natural/Endogenous Ligand(s)
histamine
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
dimethylhistaprodifen Hs Full agonist 6.4 pKi 62
pKi 6.4 [62]
methylhistaprodifen Hs Full agonist 6.4 pKi 62
pKi 6.4 [62]
2-(3-iodophenyl)histamine Hs Full agonist 5.8 pKi 62
pKi 5.8 [62]
2-(3-bromophenyl)histamine Hs Full agonist 5.7 pKi 62
pKi 5.7 [62]
2-(3-chlorophenyl)histamine Hs Full agonist 5.7 pKi 62
pKi 5.7 [62]
histaprodifen Hs Full agonist 5.7 pKi 36
pKi 5.7 [36]
2-(2-thiazolyl)ethanamine Hs Partial agonist 5.34 pKi 62
pKi 5.34 [62]
histamine Hs Full agonist 4.7 – 5.9 pKi 4,51,58,62,70
pKi 4.7 – 5.9 [4,51,58,62,70]
UR-PG55B Hs Full agonist 5.2 pKi 70
pKi 5.2 [70]
UR-PG131A Hs Full agonist 4.7 pKi 70
pKi 4.7 [70]
UR-PG153 Hs Full agonist 4.7 pKi 70
pKi 4.7 [70]
UR-PG136 Hs Full agonist 4.5 pKi 70
pKi 4.5 [70]
UR-PG146 Hs Full agonist 4.4 pKi 70
pKi 4.4 [70]
2-pyridylethylamine Hs Full agonist 3.7 pKi 58
pKi 3.7 [58]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[11C]doxepin Hs Antagonist 9.0 pKd 27
pKd 9.0 (Kd 1x10-9 M) [27]
[3H]pyrilamine Hs Inverse agonist 8.4 – 9.1 pKd 12,51,61-62
pKd 8.4 – 9.1 (Kd 7.9x10-10 – 4x10-9 M) [12,51,61-62]
cyproheptadine Hs Antagonist 10.2 pKi 51
pKi 10.2 [51]
asenapine Hs Antagonist 9.8 pKi 61
pKi 9.8 [61]
doxepin Hs Antagonist 9.5 – 10.0 pKi 4
pKi 9.5 – 10.0 [4]
clozapine Hs Antagonist 8.8 – 9.6 pKi 4,32,61
pKi 8.8 – 9.6 [4,32,61]
zotepine Hs Antagonist 9.2 pKi 61
pKi 9.2 [61]
desloratadine Hs Antagonist 9.01 pKi 34
pKi 9.01 (Ki 9.7x10-10 M) [34]
olanzapine Hs Antagonist 8.7 – 9.2 pKi 32,61
pKi 8.7 – 9.2 [32,61]
azelastine Hs Antagonist 8.9 pKi 57
pKi 8.9 (Ki 1.26x10-9 M) [57]
pyrilamine Hs Inverse agonist 8.7 – 9.0 pKi 4,58
pKi 8.7 – 9.0 [4,58]
triprolidine Hs Antagonist 8.5 – 9.0 pKi 4,51
pKi 8.5 – 9.0 [4,51]
(-)-trans-H2-PAT Hs Antagonist 8.6 – 8.8 pKi 4
pKi 8.6 – 8.8 [4]
(±)-trans-H2-PAT Hs Antagonist 8.4 – 8.6 pKi 4
pKi 8.4 – 8.6 [4]
(R)-cetirizine Hs Inverse agonist 8.5 pKi 58
pKi 8.5 [58]
(+)-chlorpheniramine Hs Antagonist 8.3 – 8.6 pKi 4,51
pKi 8.3 – 8.6 [4,51]
thiothixene Hs Antagonist 8.4 pKi 32
pKi 8.4 [32]
quetiapine Hs Antagonist 8.0 – 8.7 pKi 32,61
pKi 8.0 – 8.7 [32,61]
cetirizine Hs Inverse agonist 8.2 pKi 51
pKi 8.2 [51]
chlorpromazine Hs Antagonist 8.2 pKi 32
pKi 8.2 [32]
loxapine Hs Antagonist 8.2 pKi 32
pKi 8.2 [32]
perphenazine Hs Antagonist 8.1 pKi 32
pKi 8.1 [32]
(±)-cis-H2-PAT Hs Antagonist 7.8 – 8.2 pKi 4
pKi 8.1 – 8.2 [4]
pKi 7.8 – 7.9 [4]
fluspirilene Hs Antagonist 7.9 pKi 61
pKi 7.9 [61]
diphenhydramine Hs Antagonist 7.9 pKi 4
pKi 7.9 [4]
thioridazine Hs Antagonist 7.7 pKi 32
pKi 7.7 [32]
risperidone Hs Antagonist 7.6 – 7.8 pKi 32,61
pKi 7.6 – 7.8 [32,61]
fluphenazine Hs Antagonist 7.7 pKi 32
pKi 7.7 [32]
ziprasidone Hs Antagonist 7.4 – 7.8 pKi 32,61
pKi 7.4 – 7.8 [32,61]
aripiprazole Hs Antagonist 7.5 pKi 32
pKi 7.5 [32]
9-OH-risperidone Hs Antagonist 7.5 pKi 61
pKi 7.5 [61]
(+)-trans-H2-PAT Hs Antagonist 7.4 – 7.5 pKi 4
pKi 7.4 – 7.5 [4]
trifluoperazine Hs Antagonist 7.2 pKi 32
pKi 7.2 [32]
sertindole Hs Antagonist 6.9 pKi 32,61
pKi 6.9 [32,61]
(+)-cis-H2-PAT Hs Antagonist 6.9 pKi 4
pKi 6.9 [4]
(S)-cetirizine Hs Inverse agonist 6.7 pKi 58
pKi 6.7 [58]
BU-E 47 Hs Antagonist 6.6 pKi 62
pKi 6.6 [62]
(-)-chlorpheniramine Hs Antagonist 6.4 – 6.7 pKi 4
pKi 6.4 – 6.7 [4]
arpromidine Hs Antagonist 6.5 pKi 62,70
pKi 6.5 [62,70]
pimozide Hs Antagonist 6.2 pKi 32
pKi 6.2 [32]
haloperidol Hs Antagonist 5.7 – 6.1 pKi 32,61
pKi 5.7 – 6.1 [32,61]
ABT-239 Hs Inverse agonist 5.8 pKi 16
pKi 5.8 [16]
molindone Hs Antagonist 5.7 pKi 32
pKi 5.7 [32]
clobenpropit Hs Antagonist 5.6 pKi 17
pKi 5.6 [17]
A-349821 Hs Inverse agonist 5.6 pKi 15
pKi 5.6 [15]
pipamperone Hs Antagonist 5.6 pKi 61
pKi 5.6 [61]
A-317920 Hs Antagonist 5.4 pKi 15,17
pKi 5.4 [15,17]
impromidine Hs Antagonist 5.2 pKi 70
pKi 5.2 [70]
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Adenylate cyclase stimulation
Comments:  Stimulation of cAMP accumulation is via Gβγ subunits of Gq [42].
References:  42
Secondary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  35
Tissue Distribution
Brain: cerebrum.
Heart: myocardium (ventricle > atrium).
Species:  Human
Technique:  Northern and Western blotting.
References:  46
Brain.
Species:  Human
Technique:  Positron emission tomography (PET).
References:  50
Cranial arteries.
Species:  Human
Technique:  RT-PCR.
References:  29
Myometrium.
Species:  Human
Technique:  Radioligand binding.
References:  21
Gastrointestinal tract.
Species:  Human
Technique:  qRT-PCR and immunohistochemistry.
References:  59
Uterine horns.
Species:  Mouse
Technique:  Radioligand binding.
References:  22
Mast cells.
Species:  Mouse
Technique:  RT-PCR.
References:  24
Sympathetic preganglionic neurons in the spinal cord.
Species:  Rat
Technique:  RT-PCR.
References:  68
Embryonic brain and spinal cord.
Species:  Rat
Technique:  in situ hybridization, RT-PCR and Northern blotting.
References:  31
Brain: cerebrum.
Heart: myocardium (atrium and ventricle).
Species:  Rat
Technique:  Northern and Western blotting.
References:  46
Cochlea.
Species:  Rat
Technique:  RT-PCR.
References:  2
Expression Datasets

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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
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:  11
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:  4
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:  70
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:  42
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:  40
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:  37
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:  23
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:  45
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:  66
Physiological Functions
Contraction of smooth muscle.
Species:  Human
Tissue:  Arterial rings.
References:  10
Relaxation of smooth muscle (via an endothelial H1 receptor).
Species:  Human
Tissue:  Cranial arteries.
References:  29
Modulation of adrenergic neurotransmission.
Species:  Rat
Tissue:  Vas deferens.
References:  67
Bronchoconstriction.
Species:  Human
Tissue:  In vivo.
References:  7-8,13,38,54,65
Inhibition of locomotor behaviour.
Species:  Rat
Tissue:  In vivo.
References:  1
Modulation of feeding behaviour.
Species:  Rat
Tissue:  In vivo.
References:  19
Modulation of feeding behaviour.
Species:  Mouse
Tissue:  In vivo.
References:  43-44,52-53
Hypernociception.
Species:  Rat
Tissue:  In vivo.
References:  39
Endothelium-dependent vasodilation.
Species:  Rat
Tissue:  Mesenteric vascular beds.
References:  30
Role in the stimulation of skin blood flow during whole body heating.
Species:  Human
Tissue:  In vivo.
References:  69
Stimulation of the nitric oxide signalling system.
Species:  Rat
Tissue:  Submandibular gland.
References:  5
Increased vascular permeability.
Species:  Mouse
Tissue:  In vivo.
References:  3,55
Modulation of neuronal firing.
Species:  Rat
Tissue:  Dorsal raphe nucleus.
References:  6
Contraction of smooth muscle.
Species:  Human
Tissue:  Isolated uterine strips.
References:  41
Contraction of smooth muscle.
Species:  Rat
Tissue:  Isolated stomach fundus.
References:  14
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:  73
Depolarisation.
Species:  Rat
Tissue:  Sympathetic preganglionic neurons.
References:  68
Regulation of cytokine production.
Species:  Mouse
Tissue:  CD4+ and CD8+ T cells.
References:  64
Prostacyclin formation.
Species:  Human
Tissue:  Pulmonary artery.
References:  60
Physiological Consequences of Altering Gene Expression
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:  48
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:  26,72
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:  9
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:  71
H1 knockout mice exhibit enhancement of morphine-induced antinociception.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  47
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:  28
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:  56
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:  55
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:  64
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:  49
Phenotypes, Alleles and Disease Models 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  MP:0008688 decreased interleukin-2 secretion PMID: 9989982 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0008703 decreased interleukin-5 secretion PMID: 16680192 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6
MGI:107619  MP:0005018 decreased T cell number PMID: 9989982 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6
MGI:107619  MP:0005095 decreased T cell proliferation PMID: 9989982 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0010025 decreased total body fat amount PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6
MGI:107619  MP:0002757 decreased vertical activity PMID: 8917588 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0001260 increased body weight PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0000005 increased brown adipose tissue amount PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0001554 increased circulating free fatty acid level PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0005669 increased circulating leptin level PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0003909 increased eating behavior PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0006094 increased fat cell size PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0002493 increased IgG level PMID: 16680192 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0002494 increased IgM level PMID: 16680192 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
involves: 129P2/OlaHsd * C57BL/6
MGI:107619  MP:0008699 increased interleukin-4 secretion PMID: 9989982 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0009355 increased liver triglyceride level PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0005317 increased triglyceride level PMID: 15331534 
Hrh1tm1Wtn Hrh1tm1Wtn/Hrh1tm1Wtn
B6.129P2-Hrh1
MGI:107619  MP:0000008 increased white adipose tissue amount PMID: 15331534 
Available Assays
DiscoveRx PathHunter® CHO-K1 HRH1 β-Arrestin Cell Line (Cat no. 93-0503C2)
PathHunter® eXpress HRH1 CHO-K1 β-Arrestin GPCR Assay (Cat no. 93-0503E2CP2M)
more info

REFERENCES

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2. Azuma H, Sawada S, Takeuchi S, Higashiyama K, Kakigi A, Takeda T. (2003) Expression of mRNA encoding the H1, H2, and H3 histamine receptors in the rat cochlea. Neuroreport14: 423-425. [PMID:12634496]

3. Bhargava KP, Nath R, Palit G. (1977) Nature of histamine receptors concerned in capillary permeability. Br J Pharmacol59: 349-351. [PMID:837022]

4. Booth RG, Moniri NH, Bakker RA, Choksi NY, Nix WB, Timmerman H, Leurs R. (2002) A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors. J Pharmacol Exp Ther302: 328-336. [PMID:12065734]

5. Borda E, Stranieri G, Sterin-Borda L. (2002) H(1)-Receptor activation triggers the endogenous nitric oxide signalling system in the rat submandibular gland. Mediators Inflamm11: 337-343. [PMID:12581497]

6. Bárbara A, Aceves J, Arias-Montaño JA. (2002) Histamine H1 receptors in rat dorsal raphe nucleus: pharmacological characterisation and linking to increased neuronal activity. Brain Res954: 247-255. [PMID:12414108]

7. Casterline CL, Evans R. (1977) Further studies on the mechanism of human histamine-induced asthma: the effect of an aerosolized H1 receptor antagonist (diphenhydramine). J Allergy Clin Immunol59: 420-424. [PMID:16944]

8. Crimi N, Polosa R, Magrì S, Prosperini G, Paolino G, Mastruzzo C, Mistretta A. (1996) Inhaled lysine acetylsalicylate (L-ASA) attenuates histamine-induced bronchoconstriction in asthma. Allergy51: 157-163. [PMID:8781669]

9. Dai H, Okuda T, Sakurai E, Kuramasu A, Kato M, Jia F, Xu AJ, Iinuma K, Sato I, Yanai K. (2005) Blockage of histamine H1 receptor attenuates social isolation-induced disruption of prepulse inhibition: a study in H1 receptor gene knockout mice. Psychopharmacology (Berl)183: 285-293. [PMID:16237577]

10. Daneshmand MA, Keller RS, Canver MC, Canver AC, Canver CC. (2004) Histamine H1 and H2 receptor-mediated vasoreactivity of human internal thoracic and radial arteries. Surgery136: 458-463. [PMID:15300215]

11. De Backer MD, Gommeren W, Moereels H, Nobels G, Van Gompel P, Leysen JE, Luyten WH. (1993) Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor. Biochem Biophys Res Commun197: 1601-1608. [PMID:8280179]

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Paul Chazot, Hiroyuki Fukui, C. Robin Ganellin, Helmut L. Haas, Stephen J. Hill, Rebecca Hills, Roberto Levi, Walter Schunack, Jean-Charles Schwartz, Nigel P. Shankley, Henk Timmerman, J. Michael Young.
Histamine receptors: H1 receptor. Last modified on 31/03/2014. Accessed on 17/04/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=262.

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