Histamine H3 receptor

A histamine H3 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9Y5N1]

Synonyms

H3R;
HH3R;
G-protein coupled receptor 97

Research

Bioassay Publications (149)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	57 (38.26)	29.6817
2010's	75 (50.34)	24.3611
2020's	17 (11.41)	2.80

Compounds (75)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
histamine	Homo sapiens (human)	Ki	0.0801	16	16
melatonin	Homo sapiens (human)	Ki	0.0005	1	1
n-methylhistamine	Homo sapiens (human)	Ki	0.0040	2	2
amitriptyline	Homo sapiens (human)	Ki	1.0000	1	1
azelastine	Homo sapiens (human)	Ki	0.1514	3	3
chlorpromazine	Homo sapiens (human)	Ki	1.0000	1	1
clobenpropit	Homo sapiens (human)	IC50	0.0011	4	4
clobenpropit	Homo sapiens (human)	Ki	0.0016	17	17
decamethonium	Homo sapiens (human)	IC50	0.8200	1	1
desipramine	Homo sapiens (human)	Ki	5.0000	1	1
donepezil	Homo sapiens (human)	IC50	0.3500	1	1
fluphenazine	Homo sapiens (human)	Ki	1.0000	1	1
fluoxetine	Homo sapiens (human)	Ki	7.3000	4	4
tele-methylhistamine	Homo sapiens (human)	Ki	20.0000	1	1
imetit	Homo sapiens (human)	Ki	0.0029	9	9
maprotiline	Homo sapiens (human)	Ki	1.0000	1	1
n-methylquipazine	Homo sapiens (human)	Ki	0.4100	1	1
risperidone	Homo sapiens (human)	Ki	1.1055	1	1
histamine dihydrochloride	Homo sapiens (human)	Ki	0.1712	5	5
indopan	Homo sapiens (human)	Ki	10.0000	1	1
4-methylhistamine	Homo sapiens (human)	Ki	6.3096	1	1
impromidine	Homo sapiens (human)	Ki	0.1125	2	2
cabergoline	Homo sapiens (human)	Ki	0.0014	1	1
aripiprazole	Homo sapiens (human)	Ki	2.3610	1	1
duloxetine	Homo sapiens (human)	Ki	5.0000	1	1
iodoproxyfan	Homo sapiens (human)	Ki	0.0107	4	4
alpha-methylhistamine	Homo sapiens (human)	IC50	0.0023	1	1
alpha-methylhistamine	Homo sapiens (human)	Ki	0.0079	12	12
imidazolyl-4-propylamine	Homo sapiens (human)	Ki	0.0497	3	3
nantenine, (+-)-isomer	Homo sapiens (human)	Ki	10.0000	1	1
interferon-gamma	Homo sapiens (human)	Ki	0.0300	3	3
conessine	Homo sapiens (human)	Ki	3.3388	5	9
cannabidiol	Homo sapiens (human)	Ki	3.1000	1	1
chlorprothixene	Homo sapiens (human)	Ki	1.0000	1	1
jnj-5207852	Homo sapiens (human)	IC50	0.0005	1	1
jnj-5207852	Homo sapiens (human)	Ki	0.0009	24	25
burimamide	Homo sapiens (human)	Ki	0.0485	2	2
triptorelin	Homo sapiens (human)	Ki	0.0060	1	1
4-(1h-imidazol-4-ylmethyl)piperidine	Homo sapiens (human)	Ki	0.0004	11	11
thioperamide	Homo sapiens (human)	IC50	0.3072	6	6
thioperamide	Homo sapiens (human)	Ki	0.8734	32	37
vuf 8430	Homo sapiens (human)	Ki	0.6581	2	2
jnj 7777120	Homo sapiens (human)	IC50	100.0000	1	1
jnj 7777120	Homo sapiens (human)	Ki	3.9079	10	27
proxyfan	Homo sapiens (human)	Ki	0.0077	4	4
ciproxifan	Homo sapiens (human)	Ki	1.3289	20	25
gt 2331	Homo sapiens (human)	Ki	0.0031	2	2
(2S)-1-(1H-imidazol-5-yl)-2-propanamine	Homo sapiens (human)	Ki	0.5365	4	4
impentamine	Homo sapiens (human)	Ki	0.0050	4	4
nnc 38-1049	Homo sapiens (human)	Ki	0.0012	3	3
dibutyl phthalate	Homo sapiens (human)	IC50	0.0006	1	1
dibutyl phthalate	Homo sapiens (human)	Ki	0.0002	6	6
n-demethylloperamide	Homo sapiens (human)	Ki	0.0093	1	1
benzonitrile, 4-(2-(2-((2r)-2-methyl-1-pyrrolidinyl)ethyl)-5-benzofuranyl)-	Homo sapiens (human)	IC50	0.0006	1	1
benzonitrile, 4-(2-(2-((2r)-2-methyl-1-pyrrolidinyl)ethyl)-5-benzofuranyl)-	Homo sapiens (human)	Ki	0.0017	17	19
gw 803430	Homo sapiens (human)	Ki	0.2080	1	1
a 304121	Homo sapiens (human)	Ki	0.7682	4	4
jnj 10181457	Homo sapiens (human)	Ki	0.0011	4	4
pitolisant	Homo sapiens (human)	IC50	0.0120	1	1
pitolisant	Homo sapiens (human)	Ki	0.0060	25	25
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride	Homo sapiens (human)	Ki	1.0000	1	1
gsk239512	Homo sapiens (human)	Ki	0.0026	4	4
4-(1H-imidazol-5-ylmethyl)pyridine	Homo sapiens (human)	Ki	0.0008	5	5
1-phenyl-3-dimethylamino-1,2,3,4-tetrahydronaphthalene	Homo sapiens (human)	Ki	0.0300	1	1
4-[3-(1H-imidazol-5-yl)propyl]piperidine	Homo sapiens (human)	Ki	0.0045	3	3
a 317920	Homo sapiens (human)	Ki	0.0954	3	3
jnj 10191584	Homo sapiens (human)	Ki	12.6780	3	3
methimepip	Homo sapiens (human)	Ki	0.0010	4	4
mk-0249	Homo sapiens (human)	IC50	0.0017	1	1
mk-0249	Homo sapiens (human)	Ki	0.0033	5	5
4-(1h-imidazol-4-yl)butanamine	Homo sapiens (human)	Ki	0.0041	6	6
pf 03654746	Homo sapiens (human)	Ki	0.0020	2	4
sp 203	Homo sapiens (human)	Ki	10.0000	1	1
gsk 1004723	Homo sapiens (human)	Ki	0.0003	4	4
pf-3893787	Homo sapiens (human)	Ki	0.1862	1	1
n-alpha-benzoyl-n5-(2-chloro-1-iminoethyl)-l-ornithine amide	Homo sapiens (human)	IC50	5.9000	1	1
cep 26401	Homo sapiens (human)	Ki	0.0020	6	6
nitd 609	Homo sapiens (human)	IC50	10.0000	1	1
AZD1979	Homo sapiens (human)	IC50	0.4000	1	1
n,n-diallyl-5-methoxytryptamine	Homo sapiens (human)	Ki	5.8491	2	2
ass234	Homo sapiens (human)	Ki	0.0842	2	2
a-1155463	Homo sapiens (human)	Ki	1.8111	2	0
clozapine	Homo sapiens (human)	Ki	0.8155	2	2

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
histamine	Homo sapiens (human)	EC50	0.0615	17	17
histamine	Homo sapiens (human)	Kd	0.0030	1	1
n-methylhistamine	Homo sapiens (human)	EC50	0.0004	1	1
clobenpropit	Homo sapiens (human)	Kd	0.0292	2	3
imetit	Homo sapiens (human)	EC50	0.0018	4	4
histamine dihydrochloride	Homo sapiens (human)	EC50	0.0033	1	1
4-methylhistamine	Homo sapiens (human)	EC50	12.4000	1	1
iodoproxyfan	Homo sapiens (human)	EC50	0.0001	1	1
alpha-methylhistamine	Homo sapiens (human)	EC50	0.0109	4	4
imidazolyl-4-propylamine	Homo sapiens (human)	EC50	0.0412	2	2
sk&f 91486	Homo sapiens (human)	EC50	0.0076	1	1
jnj-5207852	Homo sapiens (human)	Kd	0.0003	5	5
4-(1h-imidazol-4-ylmethyl)piperidine	Homo sapiens (human)	EC50	0.0003	6	6
thioperamide	Homo sapiens (human)	EC50	0.0784	3	3
thioperamide	Homo sapiens (human)	Kd	0.0534	2	2
vuf 8430	Homo sapiens (human)	EC50	0.3162	1	1
jnj 7777120	Homo sapiens (human)	EC50	1.0000	1	1
proxyfan	Homo sapiens (human)	EC50	0.0032	1	1
(2S)-1-(1H-imidazol-5-yl)-2-propanamine	Homo sapiens (human)	EC50	0.0100	1	1
impentamine	Homo sapiens (human)	EC50	0.0038	3	3
benzonitrile, 4-(2-(2-((2r)-2-methyl-1-pyrrolidinyl)ethyl)-5-benzofuranyl)-	Homo sapiens (human)	EC50	0.0013	1	2
benzonitrile, 4-(2-(2-((2r)-2-methyl-1-pyrrolidinyl)ethyl)-5-benzofuranyl)-	Homo sapiens (human)	Kd	0.0129	1	1
jnj 10181457	Homo sapiens (human)	Kd	0.0005	2	2
4-(1H-imidazol-5-ylmethyl)pyridine	Homo sapiens (human)	EC50	0.0004	4	4
4-[3-(1H-imidazol-5-yl)propyl]piperidine	Homo sapiens (human)	EC50	0.0083	1	1
4-[3-(1H-imidazol-5-yl)propyl]piperidine	Homo sapiens (human)	Kd	0.0079	1	1
jnj 10191584	Homo sapiens (human)	EC50	3.1623	1	1
methimepip	Homo sapiens (human)	EC50	0.0003	3	3
mk-0249	Homo sapiens (human)	Kd	0.0006	1	1
4-(1h-imidazol-4-yl)butanamine	Homo sapiens (human)	EC50	0.0051	4	4
cep 26401	Homo sapiens (human)	EC50	0.0011	1	1

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
clobenpropit	Homo sapiens (human)	Kb	0.0002	1	1
thioperamide	Homo sapiens (human)	Kb	0.0428	2	2
jnj 7777120	Homo sapiens (human)	Kb	2.0000	1	1
ciproxifan	Homo sapiens (human)	Kb	0.1995	1	1
benzonitrile, 4-(2-(2-((2r)-2-methyl-1-pyrrolidinyl)ethyl)-5-benzofuranyl)-	Homo sapiens (human)	Kb	0.0072	2	2
pitolisant	Homo sapiens (human)	Kb	0.0022	3	3
cep 26401	Homo sapiens (human)	Kb	0.0004	1	1

Enables

This protein enables 3 target(s):

Target	Category	Definition
histamine receptor activity	molecular function	Combining with histamine to initiate a change in cell activity. Histamine is a physiologically active amine, found in plant and animal tissue and released from mast cells as part of an allergic reaction in humans. [GOC:ai]
G protein-coupled acetylcholine receptor activity	molecular function	Combining with acetylcholine and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, GOC:fj, GOC:mah]
G protein-coupled serotonin receptor activity	molecular function	Combining with the biogenic amine serotonin and transmitting the signal across the membrane by activating an associated G-protein. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:ai]

Located In

This protein is located in 2 target(s):

Target	Category	Definition
plasma membrane	cellular component	The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
presynapse	cellular component	The part of a synapse that is part of the presynaptic cell. [GOC:dos]

Active In

This protein is active in 3 target(s):

Target	Category	Definition
plasma membrane	cellular component	The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
synapse	cellular component	The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110]
dendrite	cellular component	A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732]

Involved In

This protein is involved in 5 target(s):

Target	Category	Definition
neurotransmitter secretion	biological process	The regulated release of neurotransmitter from the presynapse into the synaptic cleft via calcium-regulated exocytosis during synaptic transmission. [GOC:dph]
G protein-coupled serotonin receptor signaling pathway	biological process	The series of molecular signals generated as a consequence of a G protein-coupled serotonin receptor binding to one of its physiological ligands. [GOC:mah]
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	biological process	A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194]
chemical synaptic transmission	biological process	The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435]
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	biological process	An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by acetylcholine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb]