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H3 receptor

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 264

Nomenclature: H3 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 7 445 20q13.33 HRH3 histamine receptor H3 16,38
Mouse 7 445 2 102.62 cM Hrh3 histamine receptor H3 13,51
Rat 7 445 3q43 Hrh3 histamine receptor H3 37
Previous and Unofficial Names Click here for help
GPCR97 | H3R | HH3R
Database Links Click here for help
Specialist databases
GPCRdb hrh3_human (Hs), hrh3_mouse (Mm), hrh3_rat (Rn)
Other databases
Alphafold Q9Y5N1 (Hs), P58406 (Mm), Q9QYN8 (Rn)
ChEMBL Target CHEMBL264 (Hs), CHEMBL3263 (Mm), CHEMBL4124 (Rn)
DrugBank Target Q9Y5N1 (Hs)
Ensembl Gene ENSG00000101180 (Hs), ENSMUSG00000039059 (Mm), ENSRNOG00000061153 (Rn)
Entrez Gene 11255 (Hs), 99296 (Mm), 85268 (Rn)
Human Protein Atlas ENSG00000101180 (Hs)
KEGG Gene hsa:11255 (Hs), mmu:99296 (Mm), rno:85268 (Rn)
OMIM 604525 (Hs)
Pharos Q9Y5N1 (Hs)
RefSeq Nucleotide NM_007232 (Hs), NM_133849 (Mm), NM_053506 (Rn)
RefSeq Protein NP_009163 (Hs), NP_598610 (Mm), NP_445958 (Rn)
UniProtKB Q9Y5N1 (Hs), P58406 (Mm), Q9QYN8 (Rn)
Wikipedia HRH3 (Hs)
Natural/Endogenous Ligands Click here for help
histamine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H](R)-α-methylhistamine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 9.2 pKd 36
⤷ pKd 9.2 (Kd 6x10-10 M) [36]
N-[3H]methylhistamine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 9.1 pKd 36
⤷ pKd 9.1 [36]
N-[3H]methylhistamine Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Full agonist 9.1 pKd 37
⤷ pKd 9.1 [37]
N-[3H]α-methylhistamine Small molecule or natural product Ligand is labelled Ligand is radioactive Mm Full agonist 9.0 pKd 13
⤷ pKd 9.0 (Kd 1x10-9 M) [13]
[3H]histamine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Full agonist 8.0 pKd 36,44
⤷ pKd 8.0 [36,44]
iodoproxyfan Small molecule or natural product Hs Full agonist 10.0 pKi 59
⤷ pKi 10.0 [59]
immepip Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Mm Full agonist 9.8 pKi 13
⤷ pKi 9.8 [13]
GSK-189254 Small molecule or natural product Hs Inverse agonist 9.7 pKi 40
⤷ pKi 9.7 (Ki 2x10-10 M) [40]
iodoproxyfan Small molecule or natural product Rn Full agonist 9.6 pKi 59
⤷ pKi 9.6 [59]
cipralisant Small molecule or natural product Rn Full agonist 9.5 pKi 59
⤷ pKi 9.5 [59]
imetit Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Rn Full agonist 9.0 – 9.7 pKi 37,42,59
⤷ pKi 9.0 – 9.7 [37,42,59]
imetit Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 8.8 – 9.7 pKi 16,36-37,58-59
⤷ pKi 8.8 – 9.7 [16,36-37,58-59]
imetit Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Mm Full agonist 8.8 – 9.7 pKi 13,51
⤷ pKi 8.8 – 9.7 [13,51]
immepip Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Full agonist 8.8 – 9.7 pKi 16,32,36-37,59
⤷ pKi 8.8 – 9.7 [16,32,36-37,59]
immethridine Small molecule or natural product Ligand has a PDB structure Hs Full agonist 9.1 pKi 31
⤷ pKi 9.1 [31]
N-α-methylhistamine Small molecule or natural product Mm Full agonist 9.0 pKi 13
⤷ pKi 9.0 [13]
methimepip Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 30
⤷ pKi 9.0 (Ki 1x10-9 M) [30]
N-methylhistamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.6 – 9.3 pKi 16,36-37
⤷ pKi 8.6 – 9.3 [16,36-37]
immepip Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Rn Full agonist 8.8 – 8.9 pKi 37,59
⤷ pKi 8.8 – 8.9 [37,59]
N-methylhistamine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 8.8 pKi 37
⤷ pKi 8.8 [37]
(R)-α-methylhistamine Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Full agonist 8.4 – 9.2 pKi 16,34,36-37,58-59
⤷ pKi 8.4 – 9.2 [16,34,36-37,58-59]
MK-0249 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.8 pKi 43
⤷ pKi 8.8 (Ki 1.7x10-9 M) [43]
GR 175737 Small molecule or natural product Hs Partial agonist 8.6 pKi 59
⤷ pKi 8.6 [59]
cipralisant Small molecule or natural product Hs Full agonist 8.6 pKi 59
⤷ pKi 8.6 [59]
VUF 8328 Small molecule or natural product Hs Partial agonist 8.5 pKi 58
⤷ pKi 8.5 [58]
(R)-α-methylhistamine Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Mm Full agonist 8.4 pKi 13
⤷ pKi 8.4 [13]
imbutamine Small molecule or natural product Hs Full agonist 8.4 pKi 32
⤷ pKi 8.4 [32]
compound 3a [PMID: 18606542] Small molecule or natural product Hs Inverse agonist 8.4 pKi 50
⤷ pKi 8.4 (Ki 4x10-9 M) [50]
Description: Affinity measured in a saturation binding experiment using human H3 receptor-expressing CHO cells, and [3H]-(R)-α-methylhistamine as tracer.
(R)-α-methylhistamine Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Rn Full agonist 8.0 – 8.7 pKi 34,37,59
⤷ pKi 8.0 – 8.7 [34,37,59]
proxyfan Small molecule or natural product Ligand has a PDB structure Mm Full agonist 8.2 – 8.5 pKi 51
⤷ pKi 8.2 – 8.5 [51]
GR 175737 Small molecule or natural product Rn Partial agonist 8.3 pKi 59
⤷ pKi 8.3 [59]
impentamine Small molecule or natural product Hs Full agonist 8.3 pKi 32
⤷ pKi 8.3 [32]
proxyfan Small molecule or natural product Ligand has a PDB structure Hs Full agonist 8.3 pKi 59
⤷ pKi 8.3 [59]
proxyfan Small molecule or natural product Ligand has a PDB structure Rn Full agonist 8.0 – 8.5 pKi 42,59
⤷ pKi 8.0 – 8.5 [42,59]
SUVN-G3031 Small molecule or natural product Hs Inverse agonist 8.1 pKi 45
⤷ pKi 8.1 (Ki 8.73x10-9 M) [45]
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 7.8 – 8.3 pKi 16,32,34,36-37,59
⤷ pKi 7.8 – 8.3 [16,32,34,36-37,59]
VUF 5207 Small molecule or natural product Hs Full agonist 7.8 pKi 58
⤷ pKi 7.8 [58]
(S)-α-methylhistamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.6 pKi 59
⤷ pKi 7.6 [59]
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 Rn Full agonist 7.2 – 7.9 pKi 34,37,42
⤷ pKi 7.2 – 7.9 [34,37,42]
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 Mm Full agonist 7.1 – 7.8 pKi 13,51
⤷ pKi 7.1 – 7.8 [13,51]
impromidine Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 7.2 pKi 36
⤷ pKi 7.2 [36]
(S)-α-methylhistamine Small molecule or natural product Rn Full agonist 6.6 pKi 59
⤷ pKi 6.6 [59]
ST-1006 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.3 pKi 46
⤷ pKi 6.3 [46]
dimaprit Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.1 pKi 36
⤷ pKi 6.1 [36]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[123I]iodoproxyfan Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Antagonist 10.3 pKd 34
⤷ pKd 10.3 [34]
[123I]iodoproxyfan Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 10.2 pKd 34
⤷ pKd 10.2 (Kd 6.3x10-11 M) [34]
[125I]iodophenpropit Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Antagonist 9.2 pKd 29
⤷ pKd 9.2 (Kd 6x10-10 M) [29]
GSK334429 Small molecule or natural product Primary target of this compound Hs Antagonist 9.5 – 9.9 pKi 6,35
⤷ pKi 9.5 – 9.9 (Ki 3.2x10-10 – 1.3x10-10 M) [6,35]
clobenpropit Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Mm Antagonist 9.5 pKi 13
⤷ pKi 9.5 [13]
A-349821 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 9.4 pKi 18
⤷ pKi 9.4 [18]
ABT-239 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 9.4 pKi 19
⤷ pKi 9.4 [19]
clobenpropit Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Rn Antagonist 8.9 – 9.8 pKi 20,34,37,42,58-59
⤷ pKi 8.9 – 9.8 [20,34,37,42,58-59]
ciproxifan Small molecule or natural product Mm Antagonist 9.1 – 9.4 pKi 51
⤷ pKi 9.1 – 9.4 [51]
A-317920 Small molecule or natural product Rn Antagonist 9.2 pKi 18,20
⤷ pKi 9.2 [18,20]
JNJ-5207852 Small molecule or natural product Hs Antagonist 9.2 pKi 1
⤷ pKi 9.2 [1]
iodophenpropit Small molecule or natural product Rn Antagonist 8.8 – 9.1 pKi 58-59
⤷ pKi 8.8 – 9.1 [58-59]
clobenpropit Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 8.4 – 9.4 pKi 16,20,34,36-37,58-59
⤷ pKi 8.4 – 9.4 (Ki 3.9x10-9 – 3.9x10-10 M) [16,20,34,36-37,58-59]
ABT-239 Small molecule or natural product Rn Inverse agonist 8.9 pKi 19
⤷ pKi 8.9 [19]
ciproxifan Small molecule or natural product Rn Antagonist 8.4 – 9.3 pKi 18,20,34,42,59
⤷ pKi 8.4 – 9.3 [18,20,34,42,59]
A-349821 Small molecule or natural product Rn Inverse agonist 8.8 pKi 18
⤷ pKi 8.8 [18]
enerisant Small molecule or natural product Hs Inverse agonist 8.8 pKi 25
⤷ pKi 8.8 (Ki 1.65x10-9 M) [25]
Description: Determined using [3H]N-α-methylhistamine binding to the membranes of CHO-K1 cells expressing human recombinant H3 receptors.
thioperamide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 8.6 – 8.8 pKi 51
⤷ pKi 8.6 – 8.8 [51]
FUB 349 Small molecule or natural product Hs Antagonist 8.7 pKi 34
⤷ pKi 8.7 [34]
PF-03654746 Small molecule or natural product Hs Antagonist 8.6 pKi 57
⤷ pKi 8.6 (Ki 2.3x10-9 M) [57]
proxyfan Small molecule or natural product Ligand has a PDB structure Hs Antagonist 8.6 pKi 34
⤷ pKi 8.6 [34]
A-304121 Small molecule or natural product Rn Antagonist 8.6 pKi 18,20
⤷ pKi 8.6 [18,20]
proxyfan Small molecule or natural product Ligand has a PDB structure Rn Antagonist 8.5 pKi 34
⤷ pKi 8.5 [34]
A331440 Small molecule or natural product Hs Antagonist 8.5 pKi 23
⤷ pKi 8.5 [23]
iodophenpropit Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 8.7 pKi 58-59
⤷ pKi 8.2 – 8.7 (Ki 6.31x10-9 – 1.99x10-9 M) [58-59]
pitolisant Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.1 – 8.6 pKi 46,62
⤷ pKi 8.1 – 8.6 (Ki 2.7x10-9 M) [46,62]
Description: Measured in a [125I]iodoproxyfan binding assay in cells exogenously expressing the human H3 receptor.
impentamine Small molecule or natural product Hs Antagonist 8.3 pKi 58
⤷ pKi 8.3 [58]
impentamine Small molecule or natural product Rn Antagonist 8.3 pKi 58
⤷ pKi 8.3 [58]
conessine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 46
⤷ pKi 8.3 [46]
ST-1478 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 27
⤷ pKi 8.3 (Ki 5.25x10-9 M) [27]
thioperamide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.7 – 8.8 pKi 18,20,34,37,42,58-59
⤷ pKi 7.7 – 8.8 [18,20,34,37,42,58-59]
ST-1505 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 27
⤷ pKi 8.3 (Ki 5.59x10-9 M) [27]
MK-0249 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 pKi 46
⤷ pKi 8.2 [46]
enerisant Small molecule or natural product Rn Inverse agonist 8.1 pKi 25
⤷ pKi 8.1 (Ki 7.87x10-9 M) [25]
FUB 349 Small molecule or natural product Rn Antagonist 7.9 pKi 34
⤷ pKi 7.9 [34]
VUF 4904 Small molecule or natural product Hs Antagonist 7.9 pKi 58
⤷ pKi 7.9 [58]
VUF14862 Small molecule or natural product Hs Antagonist 7.7 pKi 24
⤷ pKi 7.7 (Ki 1.95x10-8 M) [24]
Description: Ki measured in the dark and compound in the trans configuration.
FUB 349 Small molecule or natural product Mm Antagonist 7.6 – 7.8 pKi 51
⤷ pKi 7.6 – 7.8 [51]
GT2394 Small molecule or natural product Rn Antagonist 7.7 pKi 59
⤷ pKi 7.7 [59]
UCL-2138 Small molecule or natural product Hs Antagonist 7.6 pKi 36
⤷ pKi 7.6 [36]
PF-03654746 Small molecule or natural product Mm Antagonist 7.4 pKi 57
⤷ pKi 7.4 (Ki 3.7x10-8 M) [57]
thioperamide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.1 – 7.7 pKi 16,18,20,34,37,58-59
⤷ pKi 7.1 – 7.7 (Ki 7.94x10-8 – 1.99x10-8 M) Selective for H3/H4 compared to H1 and H3. [16,18,20,34,37,58-59]
VUF14738 Small molecule or natural product Hs Antagonist 7.3 pKi 24
⤷ pKi 7.3 (Ki 4.786x10-8 M) [24]
Description: Ki measured under UV illumination, and compound in cis configuration.
burimamide Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.3 pKi 58
⤷ pKi 7.3 [58]
JB 98064 Small molecule or natural product Hs Antagonist 7.3 pKi 59
⤷ pKi 7.3 [59]
burimamide Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.1 pKi 36,58
⤷ pKi 7.1 [36,58]
A-317920 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.0 pKi 18,20
⤷ pKi 7.0 [18,20]
JB 98064 Small molecule or natural product Rn Antagonist 7.0 pKi 59
⤷ pKi 7.0 [59]
ciproxifan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 – 7.3 pKi 16,18,20,34,46,59
⤷ pKi 6.7 – 7.3 [16,18,20,34,46,59]
adriforant Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.7 pKi 46
⤷ pKi 6.7 [46]
FUB 465 Small molecule or natural product Rn Antagonist 6.4 – 6.9 pKi 42
⤷ pKi 6.4 – 6.9 [42]
GT2394 Small molecule or natural product Hs Antagonist 6.4 pKi 59
⤷ pKi 6.4 [59]
INCB-38579 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 pKi 46
⤷ pKi 6.4 [46]
A-304121 Small molecule or natural product Hs Antagonist 6.1 pKi 18,20
⤷ pKi 6.1 [18,20]
JNJ-39758979 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.0 pKi 46
⤷ pKi 6.0 (Ki 1x10-6 M) [46]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 5.8 pKi 37
⤷ pKi 5.8 [37]
View species-specific antagonist tables
Antagonist Comments
VUF 4904 is a neutral antagonist [58]. The affinity of VUF14738 decreases to 646 nM in the trans configuration adopted in the dark [24]. VUF14862 operates in the opposite direction, its affinity increases to 1.7 nM in the cis configuration adopted in the dark [24].
Immunopharmacology Comments
H3 receptor expression is low in peripheral tissues, but high in neuronal mast cells and eosinophils. It is not currently considered an important target in allergy.
Cell Type Associations
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  In humans, H3R expression is restricted to brain mast cells.
References:  21
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   eosinophil (CL:0000771)
Comment:  Eosinophils express all four histamine receptor subtypes.
References:  22,41
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
References:  14-15
Tissue Distribution Click here for help
Brain: thalamus, caudate nucleus, putamen, cerebellum, amygdala, substantia nigra, hippocampus, hypothalamus, cerebral cortex.
Species:  Human
Technique:  Northern blotting and RT-PCR.
References:  16
Brain: thalamus, hypothalamus, hippocampus > cerebellum, brainstem.
Species:  Mouse
Technique:  Radioligand binding.
References:  28
Brain: cerebral cortex, basal ganglia, caudate putamen, nucleus accumbens, subthalamic nucleus, hypothalamus, thalamus, hippocampus, dentate gyrus, cerebellum.
Species:  Mouse
Technique:  in situ hybridisation.
References:  51
Brain: cerebral cortex, hippocampus, cerebellum, striatum, olfactory tubercle, substantia nigra, thalamus.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  12
Brain: cerebral cortex, striatum, hypothalamus.
Species:  Mouse
Technique:  Southern blotting and RT-PCR.
References:  51
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:  26
Skin, dorsal root ganglia, superior cervical ganglia, spinal cord.
Species:  Rat
Technique:  Immunohistochemistry.
References:  9
Brain: cerebral cortex, hippocampus, midbrain, hypothalamus, striatum, brainstem, cerebellum, olfactory tuberculum.
Species:  Rat
Technique:  Southern blotting and RT-PCR.
References:  42
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:  48
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:  26
Cochlea.
Species:  Rat
Technique:  RT-PCR.
References:  3
Embryo: adipose tissue, liver.
Adult: brain.
Species:  Rat
Technique:  RT-PCR and Southern blotting.
References:  26
Expression Datasets Click here for help

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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 Click here for help
Measurement of Ca2+ levels in CHO cells transfected with the human H3 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Ca2+ mobilisation.
References:  16
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:  37,58
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:  13
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:  58
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:  17
Physiological Functions Click here for help
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:  61
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:  53
Inhibition of acetylcholine release.
Species:  Rat
Tissue:  Isolated stomach.
References:  60
Inhibition of glutamate release.
Species:  Rat
Tissue:  Dentate gyrus.
References:  7
Inhibition of cholinergic transmission.
Role in consolidation of fear conditioning.
Species:  Rat
Tissue:  In vivo.
References:  8,47
Vasoconstriction.
Species:  Human
Tissue:  Turbinate mucosa strips.
References:  56
Regulation of food intake and body weight.
Species:  Rat
Tissue:  In vivo.
References:  39
Activation of spinal H3 receptors inhibits mechanical nociception.
Species:  Human
Tissue:  In vivo.
References:  11
Autoreceptor: inhibition of histamine release.
Species:  Rat
Tissue:  Cerebral cortex.
References:  2
Inhibition of chemical and mechanical nociception.
Species:  Rat
Tissue:  In vivo.
References:  10
Physiological Consequences of Altering Gene Expression Click here for help
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:  55
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:  52
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:  33
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:  49
H3 receptor knockout mice exhibit hyperphagia and late-onset obesity.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  54
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
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 Click here for help
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:  4,42
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:  16

References

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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 Chem, 46 (18): 3938-44. [PMID:12930154]

2. Arrang JM, Garbarg M, Schwartz JC. (1983) Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature, 302 (5911): 832-7. [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. Neuroreport, 14 (3): 423-5. [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 et al.. (2006) Discovery of naturally occurring splice variants of the rat histamine H3 receptor that act as dominant-negative isoforms. Mol Pharmacol, 69 (4): 1194-206. [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 Pharmacol, 115 (7): 1326-30. [PMID:7582564]

6. Berlin M, Boyce CW, Ruiz Mde L. (2011) Histamine H3 receptor as a drug discovery target. J Med Chem, 54 (1): 26-53. [PMID:21062081]

7. Brown RE, Haas HL. (1999) On the mechanism of histaminergic inhibition of glutamate release in the rat dentate gyrus. J Physiol (Lond.), 515 ( Pt 3): 777-86. [PMID:10066904]

8. 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 Neurosci, 16 (3): 521-8. [PMID:12193196]

9. 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. Pain, 129 (1-2): 76-92. [PMID:17134835]

10. Cannon KE, Hough LB. (2005) Inhibition of chemical and low-intensity mechanical nociception by activation of histamine H3 receptors. J Pain, 6 (3): 193-200. [PMID:15772913]

11. 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 Pharmacol, 470 (3): 139-47. [PMID:12798951]

12. Chazot PL, Hann V, Wilson C, Lees G, Thompson CL. (2001) Immunological identification of the mammalian H3 histamine receptor in the mouse brain. Neuroreport, 12 (2): 259-62. [PMID:11209931]

13. Chen J, Liu C, Lovenberg TW. (2003) Molecular and pharmacological characterization of the mouse histamine H3 receptor. Eur J Pharmacol, 467 (1-3): 57-65. [PMID:12706455]

14. Clark EA, Hill SJ. (1996) Sensitivity of histamine H3 receptor agonist-stimulated [35S]GTP gamma[S] binding to pertussis toxin. Eur J Pharmacol, 296 (2): 223-5. [PMID:8838460]

15. Clark MA, Korte A, Egan RW. (1993) Guanine nucleotides and pertussis toxin reduce the affinity of histamine H3 receptors on AtT-20 cells. Agents Actions, 40 (3-4): 129-34. [PMID:8023737]

16. Cogé F, Guénin SP, Audinot V, Renouard-Try A, Beauverger P, Macia C, Ouvry C, Nagel N, Rique H, Boutin JA et al.. (2001) Genomic organization and characterization of splice variants of the human histamine H3 receptor. Biochem J, 355 (Pt 2): 279-88. [PMID:11284713]

17. 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 Pharmacol, 59 (1): 1-8. [PMID:11125017]

18. Esbenshade TA, Fox GB, Krueger KM, Baranowski JL, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan JB et al.. (2004) Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. Biochem Pharmacol, 68 (5): 933-45. [PMID:15294456]

19. Esbenshade TA, Fox GB, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan L, Wetter J et al.. (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 (1): 165-75. [PMID:15608078]

20. Esbenshade TA, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Fox GB, Faghih R, Bennani YL et al.. (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 (3): 887-96. [PMID:12606603]

21. Gangwar RS, Landolina N, Arpinati L, Levi-Schaffer F. (2017) Mast cell and eosinophil surface receptors as targets for anti-allergic therapy. Pharmacol Ther, 170: 37-63. [PMID:27773785]

22. Gibbs BF, Levi-Schaffer F. (2012) H₄ receptors in mast cells and basophils: a new therapeutic target for allergy?. Front Biosci (Landmark Ed), 17: 430-7. [PMID:22201753]

23. 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]

24. Hauwert NJ, Mocking TAM, Da Costa Pereira D, Kooistra AJ, Wijnen LM, Vreeker GCM, Verweij EWE, De Boer AH, Smit MJ, De Graaf C et al.. (2018) Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology. J Am Chem Soc, 140 (12): 4232-4243. [PMID:29470065]

25. Hino N, Marumo T, Kotani M, Shimazaki T, Kaku-Fukumoto A, Hikichi H, Karasawa JI, Tomishima Y, Komiyama H, Tatsuda E et al.. (2020) A Novel Potent and Selective Histamine H3 Receptor Antagonist Enerisant: In Vitro Profiles, In Vivo Receptor Occupancy, and Wake-Promoting and Procognitive Effects in Rodents. J Pharmacol Exp Ther, 375 (2): 276-285. DOI: 10.1124/jpet.120.000185 [PMID:32862143]

26. Héron A, Rouleau A, Cochois V, Pillot C, Schwartz JC, Arrang JM. (2001) Expression analysis of the histamine H(3) receptor in developing rat tissues. Mech Dev, 105 (1-2): 167-73. [PMID:11429293]

27. Imeri F, Stepanovska Tanturovska B, Zivkovic A, Enzmann G, Schwalm S, Pfeilschifter J, Homann T, Kleuser B, Engelhardt B, Stark H et al.. (2021) Novel compounds with dual S1P receptor agonist and histamine H3 receptor antagonist activities act protective in a mouse model of multiple sclerosis. Neuropharmacology, 186: 108464. [PMID:33460688]

28. Jansen FP, Mochizuki T, Maeyama K, Leurs R, Timmerman H. (2000) Characterization of histamine H3 receptors in mouse brain using the H3 antagonist [125I]iodophenpropit. Naunyn Schmiedebergs Arch Pharmacol, 362 (1): 60-7. [PMID:10935534]

29. Jansen FP, Wu TS, Voss HP, Steinbusch HW, Vollinga RC, Rademaker B, Bast A, Timmerman H. (1994) Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain. Br J Pharmacol, 113 (2): 355-62. [PMID:7834183]

30. Kitbunnadaj R, Hashimoto T, Poli E, Zuiderveld OP, Menozzi A, Hidaka R, de Esch IJ, Bakker RA, Menge WM, Yamatodani A et al.. (2005) N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist. J Med Chem, 48 (6): 2100-7. [PMID:15771452]

31. Kitbunnadaj R, Zuiderveld OP, Christophe B, Hulscher S, Menge WM, Gelens E, Snip E, Bakker RA, Celanire S, Gillard M et al.. (2004) Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist. J Med Chem, 47 (10): 2414-7. [PMID:15115383]

32. Kitbunnadaj R, Zuiderveld OP, De Esch IJ, Vollinga RC, Bakker R, Lutz M, Spek AL, Cavoy E, Deltent MF, Menge WM et al.. (2003) Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists. J Med Chem, 46 (25): 5445-57. [PMID:14640553]

33. Koyama M, Seyedi N, Fung-Leung WP, Lovenberg TW, Levi R. (2003) Norepinephrine release from the ischemic heart is greatly enhanced in mice lacking histamine H3 receptors. Mol Pharmacol, 63 (2): 378-82. [PMID:12527809]

34. Ligneau X, Morisset S, Tardivel-Lacombe J, Gbahou F, Ganellin CR, Stark H, Schunack W, Schwartz JC, Arrang JM. (2000) Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. Br J Pharmacol, 131 (7): 1247-50. [PMID:11090094]

35. Lipani L, Odadzic D, Weizel L, Schwed JS, Sadek B, Stark H. (2014) Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs. Eur J Med Chem, 86: 578-88. [PMID:25218907]

36. Liu C, Ma X, Jiang X, Wilson SJ, Hofstra CL, Blevitt J, Pyati J, Li X, Chai W, Carruthers N et al.. (2001) Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol, 59 (3): 420-6. [PMID:11179434]

37. Lovenberg TW, Pyati J, Chang H, Wilson SJ, Erlander MG. (2000) Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles. J Pharmacol Exp Ther, 293 (3): 771-8. [PMID:10869375]

38. Lovenberg TW, Roland BL, Wilson SJ, Jiang X, Pyati J, Huvar A, Jackson MR, Erlander MG. (1999) Cloning and functional expression of the human histamine H3 receptor. Mol Pharmacol, 55 (6): 1101-7. [PMID:10347254]

39. Malmlöf K, Zaragoza F, Golozoubova V, Refsgaard HH, Cremers T, Raun K, Wulff BS, Johansen PB, Westerink B, Rimvall K. (2005) Influence of a selective histamine H3 receptor antagonist on hypothalamic neural activity, food intake and body weight. Int J Obes (Lond.), 29 (12): 1402-12. [PMID:16151415]

40. Medhurst AD, Atkins AR, Beresford IJ, Brackenborough K, Briggs MA, Calver AR, Cilia J, Cluderay JE, Crook B, Davis JB et al.. (2007) GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther, 321 (3): 1032-45. [PMID:17327487]

41. Migalovich-Sheikhet H, Friedman S, Mankuta D, Levi-Schaffer F. (2012) Novel identified receptors on mast cells. Front Immunol, 3: 238. [PMID:22876248]

42. Morisset S, Sasse A, Gbahou F, Héron A, Ligneau X, Tardivel-Lacombe J, Schwartz JC, Arrang JM. (2001) The rat H3 receptor: gene organization and multiple isoforms. Biochem Biophys Res Commun, 280 (1): 75-80. [PMID:11162480]

43. Nagase T, Mizutani T, Ishikawa S, Sekino E, Sasaki T, Fujimura T, Ito S, Mitobe Y, Miyamoto Y, Yoshimoto R et al.. (2008) Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. J Med Chem, 51 (15): 4780-9. [PMID:18598020]

44. Nguyen T, Shapiro DA, George SR, Setola V, Lee DK, Cheng R, Rauser L, Lee SP, Lynch KR, Roth BL et al.. (2001) Discovery of a novel member of the histamine receptor family. Mol Pharmacol, 59 (3): 427-33. [PMID:11179435]

45. Nirogi R, Shinde A, Mohammed AR, Badange RK, Reballi V, Bandyala TR, Saraf SK, Bojja K, Manchineella S, Achanta PK et al.. (2019) Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H3 Receptor Inverse Agonist with Robust Wake-Promoting Activity. J Med Chem, 62 (3): 1203-1217. [PMID:30629436]

46. Panula P, Chazot PL, Cowart M, Gutzmer R, Leurs R, Liu WL, Stark H, Thurmond RL, Haas HL. (2015) International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors. Pharmacol Rev, 67 (3): 601-55. [PMID:26084539]

47. Passani MB, Cangioli I, Baldi E, Bucherelli C, Mannaioni PF, Blandina P. (2001) Histamine H3 receptor-mediated impairment of contextual fear conditioning and in-vivo inhibition of cholinergic transmission in the rat basolateral amygdala. Eur J Neurosci, 14 (9): 1522-32. [PMID:11722614]

48. Pillot C, Heron A, Cochois V, Tardivel-Lacombe J, Ligneau X, Schwartz JC, Arrang JM. (2002) A detailed mapping of the histamine H(3) receptor and its gene transcripts in rat brain. Neuroscience, 114 (1): 173-93. [PMID:12207964]

49. Rizk A, Curley J, Robertson J, Raber J. (2004) Anxiety and cognition in histamine H3 receptor-/- mice. Eur J Neurosci, 19 (7): 1992-6. [PMID:15078574]

50. Roche O, Nettekoven M, Vifian W, Sarmiento RM. (2008) Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists. Bioorg Med Chem Lett, 18 (15): 4377-9. [PMID:18606542]

51. Rouleau A, Héron A, Cochois V, Pillot C, Schwartz JC, Arrang JM. (2004) Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms. J Neurochem, 90 (6): 1331-8. [PMID:15341517]

52. Takahashi K, Suwa H, Ishikawa T, Kotani H. (2002) Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype. J Clin Invest, 110 (12): 1791-9. [PMID:12488429]

53. Threlfell S, Cragg SJ, Kalló I, Turi GF, Coen CW, Greenfield SA. (2004) Histamine H3 receptors inhibit serotonin release in substantia nigra pars reticulata. J Neurosci, 24 (40): 8704-10. [PMID:15470136]

54. Tokita S, Takahashi K, Kotani H. (2006) Recent advances in molecular pharmacology of the histamine systems: physiology and pharmacology of histamine H3 receptor: roles in feeding regulation and therapeutic potential for metabolic disorders. J Pharmacol Sci, 101 (1): 12-8. [PMID:16648667]

55. Toyota H, Dugovic C, Koehl M, Laposky AD, Weber C, Ngo K, Wu Y, Lee DH, Yanai K, Sakurai E et al.. (2002) Behavioral characterization of mice lacking histamine H(3) receptors. Mol Pharmacol, 62 (2): 389-97. [PMID:12130692]

56. Varty LM, Gustafson E, Laverty M, Hey JA. (2004) Activation of histamine H3 receptors in human nasal mucosa inhibits sympathetic vasoconstriction. Eur J Pharmacol, 484 (1): 83-9. [PMID:14729385]

57. Wager TT, Pettersen BA, Schmidt AW, Spracklin DK, Mente S, Butler TW, Howard H, Lettiere DJ, Rubitski DM, Wong DF et al.. (2011) Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem, 54 (21): 7602-20. [PMID:21928839]

58. Wieland K, Bongers G, Yamamoto Y, Hashimoto T, Yamatodani A, Menge WM, Timmerman H, Lovenberg TW, Leurs R. (2001) Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists. J Pharmacol Exp Ther, 299 (3): 908-14. [PMID:11714875]

59. Wulff BS, Hastrup S, Rimvall K. (2002) Characteristics of recombinantly expressed rat and human histamine H3 receptors. Eur J Pharmacol, 453 (1): 33-41. [PMID:12393057]

60. Yokotani K, Murakami Y, Okada S, Wang M, Nakamura K. (2000) Histamine H(3) receptor-mediated inhibition of endogenous acetylcholine release from the isolated, vascularly perfused rat stomach. Eur J Pharmacol, 392 (1-2): 23-9. [PMID:10748268]

61. Zhou FW, Xu JJ, Zhao Y, LeDoux MS, Zhou FM. (2006) Opposite functions of histamine H1 and H2 receptors and H3 receptor in substantia nigra pars reticulata. J Neurophysiol, 96 (3): 1581-91. [PMID:16738217]

62. Łazewska D, Kuder K, Ligneau X, Camelin JC, Schunack W, Stark H, Kieć-Kononowicz K. (2009) Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands. Bioorg Med Chem, 17 (8): 3037-42. [PMID:19329325]

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