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H3 receptor

Family: Histamine receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
Biologically Significant Variants
References
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 12,38
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 10280 (Hs), 11299 (Mm), 11300 (Rn)
DrugBank Target 1341 (Hs)
Ensembl ENSG00000101180 (Hs), ENSMUSG00000039059 (Mm), ENSRNOG00000008080 (Rn)
Entrez Gene 11255 (Hs), 99296 (Mm), 85268 (Rn)
GeneCards HRH3 (Hs)
GenitoUrinary Development Molecular Anatomy Project Hrh3 (Mm)
HomoloGene 5232 (Hs)
Human Protein Reference Database 05162 (Hs)
InterPro Q9Y5N1 (Hs), P58406 (Mm), Q9QYN8 (Rn)
KEGG Gene hsa:11255 (Hs), mmu:99296 (Mm), rno:85268 (Rn)
OMIM 604525 (Hs)
PharmGKB Gene PA29458 (Hs)
PhosphoSitePlus Q9Y5N1 (Hs), P58406 (Mm), Q9QYN8 (Rn)
Protein Ontology (PRO) PRO:000001564 (Hs)
RefSeq Nucleotide NM_007232 (Hs), NM_133849 (Mm), NM_053506 (Rn)
RefSeq Protein NP_009163 (Hs), NP_598610 (Mm), NP_445958 (Rn)
TreeFam ENSG00000101180 (Hs), ENSMUSG00000039059 (Mm), ENSRNOG00000008080 (Rn)
UniGene Hs. 251399 (Hs)
UniProt Q9Y5N1 (Hs), P58406 (Mm), Q9QYN8 (Rn)
Wikipedia H3 receptor
Histamine receptors
Search for 3D structures on the PDB
Search by keyword: Histamine receptors H3 receptor Search by accession number: Q9QYN8, Q9Y5N1, P58406
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
[3H](R)-α-methylhistamine Hs Full agonist 9.2 pKd 29
N-[3H]methylhistamine Hs Full agonist 9.1 pKd 29
N-[3H]methylhistamine Rn Full agonist 9.1 pKd 30
N-[3H]α-methylhistamine Mm Full agonist 9.0 pKd 12
[3H]histamine Hs Full agonist 8.0 pKd 29,34
iodoproxyfan Hs Full agonist 10.0 pKi 45
immepip Mm Full agonist 9.8 pKi 12
iodoproxyfan Rn Full agonist 9.6 pKi 45
Perceptin® Rn Full agonist 9.5 pKi 45
imetit Rn Full agonist 9.0 – 9.7 pKi 30,33,45
imetit Mm Full agonist 8.8 – 9.7 pKi 12,38
imetit Hs Full agonist 8.8 – 9.7 pKi 15,29-30,44-45
immepip Hs Full agonist 8.8 – 9.7 pKi 15,25,29-30,45
immethridine Hs Full agonist 9.1 pKi 26
N-α-methylhistamine Mm Full agonist 9.0 pKi 12
methimepip Hs Full agonist 9.0 pKi 24
N-methylhistamine Hs Full agonist 8.6 – 9.3 pKi 15,29-30
immepip Rn Full agonist 8.8 – 8.9 pKi 30,45
N-methylhistamine Rn Full agonist 8.8 pKi 30
(R)-α-methylhistamine Hs Full agonist 8.4 – 9.2 pKi 15,28-30,44-45
GR 175737 Hs Partial agonist 8.6 pKi 45
Perceptin® Hs Full agonist 8.6 pKi 45
VUF 8328 Hs Partial agonist 8.5 pKi 44
imbutamine Hs Full agonist 8.4 pKi 25
(R)-α-methylhistamine Mm Full agonist 8.4 pKi 12
(R)-α-methylhistamine Rn Full agonist 8.0 – 8.7 pKi 28,30,45
proxyfan Mm Full agonist 8.2 – 8.5 pKi 38
GR 175737 Rn Partial agonist 8.3 pKi 45
impentamine Hs Full agonist 8.3 pKi 25
proxyfan Hs Full agonist 8.3 pKi 45
proxyfan Rn Full agonist 8.0 – 8.5 pKi 33,45
histamine Hs Full agonist 7.8 – 8.3 pKi 15,25,28-30,45
VUF 5207 Hs Full agonist 7.8 pKi 44
(S)-α-methylhistamine Hs Full agonist 7.6 pKi 45
histamine Rn Full agonist 7.2 – 7.9 pKi 28,30,33
histamine Mm Full agonist 7.1 – 7.8 pKi 12,38
impromidine Hs Partial agonist 7.2 pKi 29
(S)-α-methylhistamine Rn Full agonist 6.6 pKi 45
dimaprit Hs Full agonist 6.1 pKi 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
[123I]iodoproxyfan Hs Antagonist 10.2 pKd 28
[125I]iodophenpropit Rn Antagonist 9.2 pKd 23
clobenpropit Mm Antagonist 9.5 pKi 12
A-349821 Hs Inverse agonist 9.4 pKi 17
ABT-239 Hs Inverse agonist 9.4 pKi 18
clobenpropit Rn Antagonist 8.9 – 9.8 pKi 19,28,30,33,44-45
ciproxifan Mm Antagonist 9.1 – 9.4 pKi 38
1-[4-(3-piperidin-1-ylpropoxy)benzyl]piperidine Hs Antagonist 9.2 pKi 1
A-317920 Rn Antagonist 9.2 pKi 17,19
iodophenpropit Rn Antagonist 8.8 – 9.1 pKi 44-45
ABT-239 Rn Inverse agonist 8.9 pKi 18
clobenpropit Hs Antagonist 8.4 – 9.4 pKi 15,19,28-30,44-45
ciproxifan Rn Antagonist 8.4 – 9.3 pKi 17,19,28,33,45
A-349821 Rn Inverse agonist 8.8 pKi 17
thioperamide Mm Antagonist 8.6 – 8.8 pKi 38
FUB 349 Hs Antagonist 8.7 pKi 28
A-304121 Rn Antagonist 8.6 pKi 17,19
proxyfan Hs Antagonist 8.6 pKi 28
A331440 Hs Antagonist 8.5 pKi 20
proxyfan Rn Antagonist 8.5 pKi 28
iodophenpropit Hs Antagonist 8.2 – 8.7 pKi 44-45
impentamine Rn Antagonist 8.3 pKi 44
impentamine Hs Antagonist 8.3 pKi 44
thioperamide Rn Antagonist 7.7 – 8.8 pKi 17,19,28,30,33,44-45
FUB 349 Rn Antagonist 7.9 pKi 28
VUF 4904 Hs Antagonist 7.9 pKi 44
FUB 349 Mm Antagonist 7.6 – 7.8 pKi 38
GT2394 Rn Antagonist 7.7 pKi 45
4-(3-piperdin-1-yl-propoxy)benzonitrile Hs Antagonist 7.6 pKi 29
thioperamide Hs Antagonist 7.1 – 7.7 pKi 15,17,19,28,30,44-45
burimamide Rn Antagonist 7.3 pKi 44
JB 98064 Hs Antagonist 7.3 pKi 45
burimamide Hs Antagonist 7.1 pKi 29,44
A-317920 Hs Antagonist 7.0 pKi 17,19
ciproxifan Hs Antagonist 6.7 – 7.3 pKi 15,17,19,28,45
JB 98064 Rn Antagonist 7.0 pKi 45
FUB 465 Rn Antagonist 6.4 – 6.9 pKi 33
GT2394 Hs Antagonist 6.4 pKi 45
A-304121 Hs Antagonist 6.1 pKi 17,19
clozapine Rn Antagonist 5.8 pKi 30
View species-specific antagonist tables
Antagonist Comments
VUF 4904 is a neutral antagonist [44].

Explore drug-target interactions for this set of compounds using iPHACE

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: cerebral cortex, striatum, hypothalamus.
Species:  Mouse
Technique:  Southern blotting and RT-PCR.
References:  38
Brain: cerebral cortex, basal ganglia, caudate putamen, nucleus accumbens, subthalamic nucleus, hypothalamus, thalamus, hippocampus, dentate gyrus, cerebellum.
Species:  Mouse
Technique:  in situ hybridisation.
References:  38
Brain: cerebral cortex, hippocampus, cerebellum, striatum, olfactory tubercle, substantia nigra, thalamus.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  11
Brain: thalamus, hypothalamus, hippocampus > cerebellum, brainstem.
Species:  Mouse
Technique:  Radioligand binding.
References:  22
Skin, dorsal root ganglia, superior cervical ganglia, spinal cord.
Species:  Rat
Technique:  Immunohistochemistry.
References:  9
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
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:  36
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:  30,44
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:  44
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:  47
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:  40
Inhibition of acetylcholine release.
Species:  Rat
Tissue:  Isolated stomach.
References:  46
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:  7,35
Vasoconstriction.
Species:  Human
Tissue:  Turbinate mucosa strips.
References:  43
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:  8
Physiological Consequences of Altering Gene Expression
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:  37
H3 receptor knockout mice exhibit hyperphagia and late-onset obesity.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  41
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:  42
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:  39
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
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
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.
Type:  Splice variants.
Species:  Human
References:  15
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.
Type:  Splice variants.
Species:  Rat
References:  4,33

REFERENCES

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1. Apodaca, R., Dvorak, C. A., Xiao, W., Barbier, A. J., Boggs, J. D., Wilson, S. J., Lovenberg, T. W. and Carruthers, N. I. (2003) A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines. J Med Chem, 46: 3938-3944. [PMID:12930154]

2. Arrang, J. M., Garbarg, M. and Schwartz, J.-C. (1983) Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature, 302: 1-5. [PMID:6188956]

3. Azuma, H., Sawada, S., Takeuchi, S., Higashiyama, K., Kakigi, A. and Takeda, T. (2003) Expression of mRNA encoding the H1, H2, and H3 histamine receptors in the rat cochlea. Neuroreport, 14: 423-425. [PMID:12634496]

4. Bakker, R. A., Lozada, A. F., van Marle, A., Shenton, F. C., Drutel, G., Karlstedt, K., Hoffmann, M., Lintunen, M., Yamamoto, Y., van Rijn, R. M., Chazot, P. L., Panula, P. and Leurs, R. (2006) Discovery of naturally occurring splice variants of the rat histamine H3 receptor that act as dominant-negative isoforms. Mol Pharmacol, 69: 1194-1206. [PMID:16415177]

5. Barocelli, E., Ballabeni, V., Chiavarini, M. and Impicciatore, M. (1995) R-alpha-methylhistamine-induced inhibition of gastric acid secretion in pylorus-ligated rats via central histamine H3 receptors. Br J Pharmacol, 115: 1326-1330. [PMID:7582564]

6. Brown, R. E. and Haas, H. L. (1999) On the mechanism of histaminergic inhibition of glutamate release in the rat dentate gyrus. J Physiol, 515: 777-786. [PMID:10066904]

7. Cangioli, I., Baldi, E., Mannaioni, P. F., Bucherelli, C., Blandina, P. and Passani, M. B. (2002) Activation of histaminergic H3 receptors in the rat basolateral amygdala improves expression of fear memory and enhances acetylcholine release. Eur J Neurosci, 16: 521-528. [PMID:12193196]

8. Cannon, K. E. and Hough, L. B. (2005) Inhibition of chemical and low-intensity mechanical nociception by activation of histamine H3 receptors. J Pain, 6: 193-200. [PMID:15772913]

9. Cannon, K. E., Chazot, P. L., Hann, V., Shenton, F., Hough, L. B. and Rice, F. L. (2007) Immunohistochemical localization of histamine H3 receptors in rodent skin, dorsal root ganglia, superior cervical ganglia, and spinal cord: potential antinociceptive targets. Pain, 129: 76-92. [PMID:17134835]

10. Cannon, K. E., Nalwalk, J. W., Stadel, R., Ge, P., Lawson, D., Silos-Santiago, I. and Hough, L. B. (2003) Activation of spinal histamine H3 receptors inhibits mechanical nociception. Eur J Pharmacol, 470: 139-147. [PMID:12798951]

11. Chazot, P. L., Hann, V., Wilson, C., Lees, G. and Thompson, C. L. (2001) Immunological identification of the mammalian H3 histamine receptor in the mouse brain. Neuroreport, 12: 259-262. [PMID:11209931]

12. Chen, J., Liu, C. and Lovenberg, T. W. (2003) Molecular and pharmacological characterization of the mouse histamine H3 receptor. Eur J Pharmacol, 467: 57-65. [PMID:12706455]

13. Clark, E. A. and Hill, S. J. (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, M. A., Korte, A. and Egan, R. W. (1993) Guanine nucleotides and pertussis toxin reduce the affinity of histamine H3 receptors on AtT-20 cells. Agents Actions, 40: 129-134. [PMID:8023737]

15. Cogé, F., Guénin, S. P., Audinot, V., Renouard-Try, A., Beauverger, P., Macia, C., Ouvry, C., Nagel, N., Rique, H., Boutin, J. A. and Galizzi, J. P. (2001) Genomic organization and characterization of splice variants of the human histamine H3 receptor. Biochem J, 355: 279-288. [PMID:11284713]

16. Drutel, G., Peitsaro, N., Karlstedt, K., Wieland, K., Smit, M. J., Timmerman, H., Panula, P. and Leurs, R. (2001) Identification of rat H3 receptor isoforms with different brain expression and signaling properties. Mol Pharmacol, 59: 1-8. [PMID:11125017]

17. Esbenshade, T. A., Fox, G. B., Krueger, K. M., Baranowski, J. L., Miller, T. R., Kang, C. H., Denny, L. I., Witte, D. G., Yao, B. B., Pan, J. B., Faghih, R., Bennani, Y. L., Williams, M. and Hancock, A. A. (2004) Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. Biochem Pharmacol, 68: 933-945. [PMID:15294456]

18. Esbenshade, T. A., Fox, G. B., Krueger, K. M., Miller, T. R., Kang, C. H., Denny, L. I., Witte, D. G., Yao, B. B., Pan, L., Wetter, J., Marsh, K., Bennani, Y. L., Cowart, M. D., Sullivan, J. P. and Hancock, A. A. (2005) Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. J Pharmacol Exp Ther, 313: 165-175. [PMID:15608078]

19. Esbenshade, T. A., Krueger, K. M., Miller, T. R., Kang, C. H., Denny, L. I., Witte, D. G., Yao, B. B., Fox, G. B., Faghih, R., Bennani, Y. L., Williams, M. and Hancock, A. A. (2003) Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. J Pharmacol Exp Ther, 305: 887-896. [PMID:12606603]

20. Hancock, AA; Bennani, YL; Bush, EN; Esbenshade, TA; Faghih, R; Fox, GB; Jacobson, P; Knourek-Segel, V; Krueger, KM; Nuss, ME; et al.. (2004) Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist. Eur. J. Pharmacol., 487 (1-3): 183-97. [PMID:15033391]

21. Héron, A., Rouleau, A., Cochois, V., Pillot, C., Schwartz, J. C. and Arrang, J. M. (2001) Expression analysis of the histamine H(3) receptor in developing rat tissues. Mech Dev, 105: 167-173. [PMID:11429293]

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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 28/02/2013. Accessed on 23/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=264.


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