Nomenclature: H3 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 7 445 20q13.33 HRH3 histamine receptor H3 15,31
Mouse 7 445 2 H4 Hrh3 histamine receptor H3 12,39
Rat 7 445 3q43 Hrh3 histamine receptor H3 30
Previous and Unofficial Names
GPCR97
MGC105370
H3R
HH3R
histamine H3 receptor
histamine receptor H3
AW049250
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
Natural/Endogenous Ligands
histamine
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H](R)-α-methylhistamine Hs Full agonist 9.2 pKd 29
pKd 9.2 (Kd 6x10-10 M) [29]
N-[3H]methylhistamine Hs Full agonist 9.1 pKd 29
pKd 9.1 [29]
N-[3H]methylhistamine Rn Full agonist 9.1 pKd 30
pKd 9.1 [30]
N-[3H]α-methylhistamine Mm Full agonist 9.0 pKd 12
pKd 9.0 (Kd 1x10-9 M) [12]
[3H]histamine Hs Full agonist 8.0 pKd 29,35
pKd 8.0 [29,35]
iodoproxyfan Hs Full agonist 10.0 pKi 46
pKi 10.0 [46]
immepip Mm Full agonist 9.8 pKi 12
pKi 9.8 [12]
iodoproxyfan Rn Full agonist 9.6 pKi 46
pKi 9.6 [46]
cipralisant Rn Full agonist 9.5 pKi 46
pKi 9.5 [46]
imetit Rn Full agonist 9.0 – 9.7 pKi 30,33,46
pKi 9.0 – 9.7 [30,33,46]
imetit Hs Full agonist 8.8 – 9.7 pKi 15,29-30,45-46
pKi 8.8 – 9.7 [15,29-30,45-46]
imetit Mm Full agonist 8.8 – 9.7 pKi 12,39
pKi 8.8 – 9.7 [12,39]
immepip Hs Full agonist 8.8 – 9.7 pKi 15,26,29-30,46
pKi 8.8 – 9.7 [15,26,29-30,46]
immethridine Hs Full agonist 9.1 pKi 25
pKi 9.1 [25]
N-α-methylhistamine Mm Full agonist 9.0 pKi 12
pKi 9.0 [12]
methimepip Hs Full agonist 9.0 pKi 24
pKi 9.0 [24]
N-methylhistamine Hs Full agonist 8.6 – 9.3 pKi 15,29-30
pKi 8.6 – 9.3 [15,29-30]
immepip Rn Full agonist 8.8 – 8.9 pKi 30,46
pKi 8.8 – 8.9 [30,46]
N-methylhistamine Rn Full agonist 8.8 pKi 30
pKi 8.8 [30]
(R)-α-methylhistamine Hs Full agonist 8.4 – 9.2 pKi 15,28-30,45-46
pKi 8.4 – 9.2 [15,28-30,45-46]
MK-0249 Hs Inverse agonist 8.77 pKi 34
pKi 8.77 (Ki 1.7x10-9 M) [34]
GR 175737 Hs Partial agonist 8.6 pKi 46
pKi 8.6 [46]
cipralisant Hs Full agonist 8.6 pKi 46
pKi 8.6 [46]
VUF 8328 Hs Partial agonist 8.5 pKi 45
pKi 8.5 [45]
imbutamine Hs Full agonist 8.4 pKi 26
pKi 8.4 [26]
(R)-α-methylhistamine Mm Full agonist 8.4 pKi 12
pKi 8.4 [12]
(R)-α-methylhistamine Rn Full agonist 8.0 – 8.7 pKi 28,30,46
pKi 8.0 – 8.7 [28,30,46]
proxyfan Mm Full agonist 8.2 – 8.5 pKi 39
pKi 8.2 – 8.5 [39]
GR 175737 Rn Partial agonist 8.3 pKi 46
pKi 8.3 [46]
proxyfan Hs Full agonist 8.3 pKi 46
pKi 8.3 [46]
impentamine Hs Full agonist 8.3 pKi 26
pKi 8.3 [26]
proxyfan Rn Full agonist 8.0 – 8.5 pKi 33,46
pKi 8.0 – 8.5 [33,46]
histamine Hs Full agonist 7.8 – 8.3 pKi 15,26,28-30,46
pKi 7.8 – 8.3 [15,26,28-30,46]
VUF 5207 Hs Full agonist 7.8 pKi 45
pKi 7.8 [45]
(S)-α-methylhistamine Hs Full agonist 7.6 pKi 46
pKi 7.6 [46]
histamine Rn Full agonist 7.2 – 7.9 pKi 28,30,33
pKi 7.2 – 7.9 [28,30,33]
histamine Mm Full agonist 7.1 – 7.8 pKi 12,39
pKi 7.1 – 7.8 [12,39]
impromidine Hs Partial agonist 7.2 pKi 29
pKi 7.2 [29]
(S)-α-methylhistamine Rn Full agonist 6.6 pKi 46
pKi 6.6 [46]
dimaprit Hs Full agonist 6.1 pKi 29
pKi 6.1 [29]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[123I]iodoproxyfan Rn Antagonist 10.3 pKd 28
pKd 10.3 [28]
[123I]iodoproxyfan Hs Antagonist 10.2 pKd 28
pKd 10.2 (Kd 6.3x10-11 M) [28]
[125I]iodophenpropit Rn Antagonist 9.2 pKd 23
pKd 9.2 (Kd 6x10-10 M) [23]
clobenpropit Mm Antagonist 9.5 pKi 12
pKi 9.5 [12]
A-349821 Hs Inverse agonist 9.4 pKi 17
pKi 9.4 [17]
ABT-239 Hs Inverse agonist 9.4 pKi 18
pKi 9.4 [18]
clobenpropit Rn Antagonist 8.9 – 9.8 pKi 19,28,30,33,45-46
pKi 8.9 – 9.8 [19,28,30,33,45-46]
ciproxifan Mm Antagonist 9.1 – 9.4 pKi 39
pKi 9.1 – 9.4 [39]
1-[4-(3-piperidin-1-ylpropoxy)benzyl]piperidine Hs Antagonist 9.2 pKi 1
pKi 9.2 [1]
A-317920 Rn Antagonist 9.2 pKi 17,19
pKi 9.2 [17,19]
iodophenpropit Rn Antagonist 8.8 – 9.1 pKi 45-46
pKi 8.8 – 9.1 [45-46]
clobenpropit Hs Antagonist 8.4 – 9.4 pKi 15,19,28-30,45-46
pKi 8.4 – 9.4 [15,19,28-30,45-46]
ABT-239 Rn Inverse agonist 8.9 pKi 18
pKi 8.9 [18]
ciproxifan Rn Antagonist 8.4 – 9.3 pKi 17,19,28,33,46
pKi 8.4 – 9.3 [17,19,28,33,46]
A-349821 Rn Inverse agonist 8.8 pKi 17
pKi 8.8 [17]
thioperamide Mm Antagonist 8.6 – 8.8 pKi 39
pKi 8.6 – 8.8 [39]
FUB 349 Hs Antagonist 8.7 pKi 28
pKi 8.7 [28]
A-304121 Rn Antagonist 8.6 pKi 17,19
pKi 8.6 [17,19]
proxyfan Hs Antagonist 8.6 pKi 28
pKi 8.6 [28]
A331440 Hs Antagonist 8.5 pKi 20
pKi 8.5 [20]
proxyfan Rn Antagonist 8.5 pKi 28
pKi 8.5 [28]
iodophenpropit Hs Antagonist 8.2 – 8.7 pKi 45-46
pKi 8.2 – 8.7 [45-46]
impentamine Hs Antagonist 8.3 pKi 45
pKi 8.3 [45]
impentamine Rn Antagonist 8.3 pKi 45
pKi 8.3 [45]
thioperamide Rn Antagonist 7.7 – 8.8 pKi 17,19,28,30,33,45-46
pKi 7.7 – 8.8 [17,19,28,30,33,45-46]
FUB 349 Rn Antagonist 7.9 pKi 28
pKi 7.9 [28]
VUF 4904 Hs Antagonist 7.9 pKi 45
pKi 7.9 [45]
FUB 349 Mm Antagonist 7.6 – 7.8 pKi 39
pKi 7.6 – 7.8 [39]
GT2394 Rn Antagonist 7.7 pKi 46
pKi 7.7 [46]
4-(3-piperdin-1-yl-propoxy)benzonitrile Hs Antagonist 7.6 pKi 29
pKi 7.6 [29]
thioperamide Hs Antagonist 7.1 – 7.7 pKi 15,17,19,28,30,45-46
pKi 7.1 – 7.7 [15,17,19,28,30,45-46]
burimamide Rn Antagonist 7.3 pKi 45
pKi 7.3 [45]
JB 98064 Hs Antagonist 7.3 pKi 46
pKi 7.3 [46]
burimamide Hs Antagonist 7.1 pKi 29,45
pKi 7.1 [29,45]
JB 98064 Rn Antagonist 7.0 pKi 46
pKi 7.0 [46]
A-317920 Hs Antagonist 7.0 pKi 17,19
pKi 7.0 [17,19]
ciproxifan Hs Antagonist 6.7 – 7.3 pKi 15,17,19,28,46
pKi 6.7 – 7.3 [15,17,19,28,46]
FUB 465 Rn Antagonist 6.4 – 6.9 pKi 33
pKi 6.4 – 6.9 [33]
GT2394 Hs Antagonist 6.4 pKi 46
pKi 6.4 [46]
A-304121 Hs Antagonist 6.1 pKi 17,19
pKi 6.1 [17,19]
clozapine Rn Antagonist 5.8 pKi 30
pKi 5.8 [30]
View species-specific antagonist tables
Antagonist Comments
VUF 4904 is a neutral antagonist [45].
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  13-14
Tissue Distribution
Brain: thalamus, caudate nucleus, putamen, cerebellum, amygdala, substantia nigra, hippocampus, hypothalamus, cerebral cortex.
Species:  Human
Technique:  Northern blotting and RT-PCR.
References:  15
Brain: thalamus, hypothalamus, hippocampus > cerebellum, brainstem.
Species:  Mouse
Technique:  Radioligand binding.
References:  22
Brain: cerebral cortex, basal ganglia, caudate putamen, nucleus accumbens, subthalamic nucleus, hypothalamus, thalamus, hippocampus, dentate gyrus, cerebellum.
Species:  Mouse
Technique:  in situ hybridisation.
References:  39
Brain: cerebral cortex, hippocampus, cerebellum, striatum, olfactory tubercle, substantia nigra, thalamus.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  11
Brain: cerebral cortex, striatum, hypothalamus.
Species:  Mouse
Technique:  Southern blotting and RT-PCR.
References:  39
Embryo: lipoblasts of adipose tissue, tongue.
Adult: epithelial layer of the tongue, epithelial cells of hair follicles and epidermis, gastric mucosa of the stomach.
Species:  Rat
Technique:  in situ hybridisation.
References:  21
Skin, dorsal root ganglia, superior cervical ganglia, spinal cord.
Species:  Rat
Technique:  Immunohistochemistry.
References:  8
Brain: cerebral cortex, hippocampus, midbrain, hypothalamus, striatum, brainstem, cerebellum, olfactory tuberculum.
Species:  Rat
Technique:  Southern blotting and RT-PCR.
References:  33
Brain: cerebral cortex, thalamic nuclei, hippocampus, dentate gyrus, basal ganglia, substantia nigra, caudate putamen, nucleus accumbens, amygdala, thalamus, hypothalamus, brainstem, cerebellum.
Species:  Rat
Technique:  in situ hybridisation.
References:  37
Embryo: brain, spinal cord, spinal ganglia, tongue epithelium, salivary glands, respiratory epithelium, lung, stomach, intestine, skin, thymus, liver, adipose tissue.
Adult: brain, spinal cord, spinal ganglia, tongue epithelium, stomach, intestine, skin, thymus.
Species:  Rat
Technique:  in situ hybridisation.
References:  21
Cochlea.
Species:  Rat
Technique:  RT-PCR.
References:  3
Embryo: adipose tissue, liver.
Adult: brain.
Species:  Rat
Technique:  RT-PCR and Southern blotting.
References:  21
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 Ca2+ levels in CHO cells transfected with the human H3 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Ca2+ mobilisation.
References:  15
Measurement of cAMP levels in SK-N-MC cells transfected with the rat H3 receptor.
Species:  Rat
Tissue:  SK-N-MC cells.
Response measured:  Inhibition of cAMP accumulation.
References:  30,45
Measurement of Ca2+ levels in HEK 293 cells transfected with the mouse H3 receptor.
Species:  Mouse
Tissue:  HEK 293 cells.
Response measured:  Ca2+ mobilisation.
References:  12
Measurement of cAMP levels in SK-N-MC cells transfected with the human H3 receptor.
Species:  Human
Tissue:  SK-N-MC cells.
Response measured:  Inhibition of cAMP accumulation.
References:  45
Measurement of MAP kinase activation in COS-7 cells transfected with the rat H3 receptor.
Species:  Rat
Tissue:  COS-7 cells.
Response measured:  Activation of p44/p42 MAPK.
References:  16
Physiological Functions
Inhibition of substantia nigra pars reticulata (SNr) inhibitory projection neuron firing frequency (via cell hyperpolarisation).
The balance between this effect and the opposing effect of H1 and H2 receptors may contribute to movement control.
Species:  Mouse
Tissue:  Coronal midbrain slices.
References:  48
Inhibition of gastric acid secretion.
Species:  Rat
Tissue:  In vivo.
References:  5
Inhibition of serotonin release in the substantia nigra pars reticulata (SNr).
Species:  Rat
Tissue:  Midbrain slices.
References:  41
Inhibition of acetylcholine release.
Species:  Rat
Tissue:  Isolated stomach.
References:  47
Inhibition of glutamate release.
Species:  Rat
Tissue:  Dentate gyrus.
References:  6
Inhibition of cholinergic transmission.
Role in consolidation of fear conditioning.
Species:  Rat
Tissue:  In vivo.
References:  7,36
Vasoconstriction.
Species:  Human
Tissue:  Turbinate mucosa strips.
References:  44
Regulation of food intake and body weight.
Species:  Rat
Tissue:  In vivo.
References:  32
Activation of spinal H3 receptors inhibits mechanical nociception.
Species:  Human
Tissue:  In vivo.
References:  10
Autoreceptor: inhibition of histamine release.
Species:  Rat
Tissue:  Cerebral cortex.
References:  2
Inhibition of chemical and mechanical nociception.
Species:  Rat
Tissue:  In vivo.
References:  9
Physiological Consequences of Altering Gene Expression
H3 receptor knockout mice exhibit normal circadian rhythmicity, but a decrease in locomotion, wheel-running behaviour and body temperature during the dark phase.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  43
H3 receptor knockout mice exhibit a mild obese phenotype, suggesting the H3 receptor may have a role in energy homeostasis.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  40
Sympathetic nerve endings from hearts from H3 receptor knockout mice exhibit an increase in basal noradrenaline release compared to hearts from wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  27
H3 receptor knockout mice exhibit increased spatial learning and memory as well as reduced levels of anxiety.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  38
H3 receptor knockout mice exhibit hyperphagia and late-onset obesity.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  42
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ * C57BL/6J
MGI:2139279  MP:0001362 abnormal anxiety-related response PMID: 12130692 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
B6.129X1-Hrh3
MGI:2139279  MP:0005167 abnormal blood-brain barrier function PMID: 17548817 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ * C57BL/6J
MGI:2139279  MP:0001777 abnormal body temperature regulation PMID: 12130692 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ
MGI:2139279  MP:0001544 abnormal cardiovascular system physiology PMID: 12527809 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0005450 abnormal energy expenditure PMID: 12488429 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ * C57BL/6J
MGI:2139279  MP:0003953 abnormal hormone level PMID: 15078574 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ * C57BL/6J
MGI:2139279  MP:0003313 abnormal locomotor activation PMID: 12130692 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ * C57BL/6J
MGI:2139279  MP:0003633 abnormal nervous system physiology PMID: 12130692 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ * C57BL/6J
MGI:2139279  MP:0001463 abnormal spatial learning PMID: 15078574 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ
MGI:2139279  MP:0005447 abnormal synaptic norepinephrine release PMID: 12527809 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ * C57BL/6J
MGI:2139279  MP:0001364 decreased anxiety-related response PMID: 15078574 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0005534 decreased body temperature PMID: 12488429 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0005290 decreased oxygen consumption PMID: 12488429 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0001402 hypoactivity PMID: 12488429 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
involves: 129X1/SvJ * C57BL/6J
MGI:2139279  MP:0001363 increased anxiety-related response PMID: 15078574 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0002079 increased circulating insulin level PMID: 12488429 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0005669 increased circulating leptin level PMID: 12488429 
Hrh3tm1Twl Hrh3tm1Twl/Hrh3tm1Twl
B6.129X1-Hrh3
MGI:2139279  MP:0004799 increased susceptibility to experimental autoimmune encephalomyelitis PMID: 17548817 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0005455 increased susceptibility to weight gain PMID: 12488429 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0010024 increased total body fat amount PMID: 12488429 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0005331 insulin resistance PMID: 12488429 
Hrh3tm1Kot Hrh3tm1Kot/Hrh3tm1Kot
involves: 129X1/SvJ * C57BL/6N
MGI:2139279  MP:0001433 polyphagia PMID: 12488429 
Biologically Significant Variants
Type:  Splice variants.
Species:  Human
Description:  Expression of human H3 receptor splice variants in CHO cells show that a deletion in the 2nd transmembrane domain alters ligand binding and deletions in the 3rd intracellular loop result in signal transduction being abolished.
References:  15
Type:  Splice variants.
Species:  Rat
Description:  Various H3 receptor splice variants have been reported to exist rat tissues. When expressed in in CHO and COS-7 cells, some have altered pharmacological properties or cell surface trafficking.
References:  4,33
Available Assays
DiscoveRx PathHunter® CHO-K1 HRH3 β-Arrestin Cell Line (Cat no. 93-0509C2)
PathHunter® eXpress HRH3 CHO-K1 β-Arrestin GPCR Assay (Cat no. 93-0509E2CP2M)
more info

REFERENCES

1. Apodaca R, Dvorak CA, Xiao W, Barbier AJ, Boggs JD, Wilson SJ, Lovenberg TW, Carruthers NI. (2003) A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines. J Med Chem46: 3938-3944. [PMID:12930154]

2. Arrang JM, Garbarg M, Schwartz J-C. (1983) Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature302: 1-5. [PMID:6188956]

3. 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]

4. Bakker RA, Lozada AF, van Marle A, Shenton FC, Drutel G, Karlstedt K, Hoffmann M, Lintunen M, Yamamoto Y, van Rijn RM, Chazot PL, Panula P, Leurs R. (2006) Discovery of naturally occurring splice variants of the rat histamine H3 receptor that act as dominant-negative isoforms. Mol Pharmacol69: 1194-1206. [PMID:16415177]

5. Barocelli E, Ballabeni V, Chiavarini M, Impicciatore M. (1995) R-alpha-methylhistamine-induced inhibition of gastric acid secretion in pylorus-ligated rats via central histamine H3 receptors. Br J Pharmacol115: 1326-1330. [PMID:7582564]

6. Brown RE, Haas HL. (1999) On the mechanism of histaminergic inhibition of glutamate release in the rat dentate gyrus. J Physiol515: 777-786. [PMID:10066904]

7. Cangioli I, Baldi E, Mannaioni PF, Bucherelli C, Blandina P, Passani MB. (2002) Activation of histaminergic H3 receptors in the rat basolateral amygdala improves expression of fear memory and enhances acetylcholine release. Eur J Neurosci16: 521-528. [PMID:12193196]

8. Cannon KE, Chazot PL, Hann V, Shenton F, Hough LB, Rice FL. (2007) Immunohistochemical localization of histamine H3 receptors in rodent skin, dorsal root ganglia, superior cervical ganglia, and spinal cord: potential antinociceptive targets. Pain129: 76-92. [PMID:17134835]

9. Cannon KE, Hough LB. (2005) Inhibition of chemical and low-intensity mechanical nociception by activation of histamine H3 receptors. J Pain6: 193-200. [PMID:15772913]

10. Cannon KE, Nalwalk JW, Stadel R, Ge P, Lawson D, Silos-Santiago I, Hough LB. (2003) Activation of spinal histamine H3 receptors inhibits mechanical nociception. Eur J Pharmacol470: 139-147. [PMID:12798951]

11. Chazot PL, Hann V, Wilson C, Lees G, Thompson CL. (2001) Immunological identification of the mammalian H3 histamine receptor in the mouse brain. Neuroreport12: 259-262. [PMID:11209931]

12. Chen J, Liu C, Lovenberg TW. (2003) Molecular and pharmacological characterization of the mouse histamine H3 receptor. Eur J Pharmacol467: 57-65. [PMID:12706455]

13. Clark EA, Hill SJ. (1996) Sensitivity of histamine H3-receptor agonist-stimulated [35S]-GTP-γS binding to pertussis toxin. Eur. J. Pharmacol.296: 223-225. [PMID:8838460]

14. Clark MA, Korte A, Egan RW. (1993) Guanine nucleotides and pertussis toxin reduce the affinity of histamine H3 receptors on AtT-20 cells. Agents Actions40: 129-134. [PMID:8023737]

15. Cogé F, Guénin SP, Audinot V, Renouard-Try A, Beauverger P, Macia C, Ouvry C, Nagel N, Rique H, Boutin JA, Galizzi JP. (2001) Genomic organization and characterization of splice variants of the human histamine H3 receptor. Biochem J355: 279-288. [PMID:11284713]

16. Drutel G, Peitsaro N, Karlstedt K, Wieland K, Smit MJ, Timmerman H, Panula P, Leurs R. (2001) Identification of rat H3 receptor isoforms with different brain expression and signaling properties. Mol Pharmacol59: 1-8. [PMID:11125017]

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To cite this database page, please use the following:

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: H3 receptor. Last modified on 11/03/2014. Accessed on 01/10/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=264.

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