5-hydroxytryptamine receptor 4

A 5-hydroxytryptamine receptor 4 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q13639]

Synonyms

5-HT-4;
5-HT4;
Serotonin receptor 4

Research

Bioassay Publications (43)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	1 (2.33)	18.7374
1990's	3 (6.98)	18.2507
2000's	19 (44.19)	29.6817
2010's	18 (41.86)	24.3611
2020's	2 (4.65)	2.80

Compounds (35)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
5-methoxytryptamine	Homo sapiens (human)	Ki	0.1362	2	2
cisapride	Homo sapiens (human)	Ki	0.0850	3	3
ebastine	Homo sapiens (human)	IC50	0.0610	1	1
haloperidol	Homo sapiens (human)	Ki	0.0006	1	1
sdz 205-557	Homo sapiens (human)	Ki	0.0063	1	1
gr 127935	Homo sapiens (human)	Ki	10.0000	1	1
gr 113808	Homo sapiens (human)	IC50	0.0002	1	1
gr 113808	Homo sapiens (human)	Ki	0.0003	13	13
sb 204070a	Homo sapiens (human)	Ki	0.0000	1	1
piboserod	Homo sapiens (human)	IC50	0.0006	1	1
piboserod	Homo sapiens (human)	Ki	0.0004	9	9
3-(piperidine-1-yl)propyl 4-amino-5-chloro-2-methoxybenzoate hydrochloride	Homo sapiens (human)	IC50	0.0490	1	1
rs 23597-190	Homo sapiens (human)	Ki	0.0316	1	1
rs 67333	Homo sapiens (human)	Ki	0.0093	1	1
tropisetron	Homo sapiens (human)	Ki	0.1995	1	1
snap 37889	Homo sapiens (human)	Ki	0.0720	1	1
norcisapride	Homo sapiens (human)	IC50	0.0190	1	1
prucalopride	Homo sapiens (human)	Ki	0.2800	3	4
4-amino-5-chloro-N-[(3R,4S)-1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxybenzamide	Homo sapiens (human)	IC50	0.4830	1	1
4-amino-5-chloro-N-[(3R,4S)-1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxybenzamide	Homo sapiens (human)	Ki	0.1000	2	2
ml 10302	Homo sapiens (human)	Ki	0.0055	12	12
sb 207710	Homo sapiens (human)	Ki	0.0022	1	1
sb 271046	Homo sapiens (human)	Ki	3.9811	1	1
sb 269970	Homo sapiens (human)	Ki	5.6295	2	2
n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide	Homo sapiens (human)	Ki	5.0119	1	1
sb258741	Homo sapiens (human)	Ki	10.0000	1	1
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride	Homo sapiens (human)	Ki	1.0000	1	1
sb-656104-a	Homo sapiens (human)	Ki	1.9055	1	1
barettin	Homo sapiens (human)	Ki	1.9100	1	1
naluzotan	Homo sapiens (human)	Ki	5.0000	1	1
td-5108	Homo sapiens (human)	Ki	0.0200	1	1
donecopride	Homo sapiens (human)	Ki	0.0092	4	4
clozapine	Homo sapiens (human)	Ki	0.2239	1	1
tegaserod	Homo sapiens (human)	Ki	0.0094	5	5

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
methylbufotenin	Homo sapiens (human)	Kd	0.0794	1	1
cisapride	Homo sapiens (human)	EC50	0.0794	1	1
rs 67333	Homo sapiens (human)	EC50	0.0020	1	1
curcumin	Homo sapiens (human)	EC50	10.0000	1	1
norcisapride	Homo sapiens (human)	EC50	0.2900	1	1
prucalopride	Homo sapiens (human)	EC50	0.0121	3	3
4-amino-5-chloro-N-[(3R,4S)-1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinyl]-2-methoxybenzamide	Homo sapiens (human)	EC50	0.0497	2	2
ml 10302	Homo sapiens (human)	EC50	0.0268	2	2
sb 207710	Homo sapiens (human)	EC50	0.0126	1	1
brl 24682	Homo sapiens (human)	EC50	0.4401	3	3
td-5108	Homo sapiens (human)	EC50	0.0028	2	2
donecopride	Homo sapiens (human)	EC50	0.0113	1	1
tegaserod	Homo sapiens (human)	EC50	0.0048	5	5

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
metergoline	Homo sapiens (human)	Activity	1.2740	1	1
gr 113808	Homo sapiens (human)	Kb	0.0000	1	1

Enables

This protein enables 4 target(s):

Target	Category	Definition
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]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
serotonin receptor activity	molecular function	Combining with the biogenic amine serotonin and transmitting a signal across a membrane by activating some effector activity. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:dos]
neurotransmitter receptor activity	molecular function	Combining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling]

Located In

This protein is located in 5 target(s):

Target	Category	Definition
cytoplasm	cellular component	The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
endosome	cellular component	A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797]
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]
membrane	cellular component	A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194]
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]

Active In

This protein is active 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]
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 9 target(s):

Target	Category	Definition
G protein-coupled receptor signaling pathway	biological process	The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor]
maintenance of gastrointestinal epithelium	biological process	Protection of epithelial surfaces of the gastrointestinal tract from proteolytic and caustic digestive agents. [GOC:mah]
regulation of appetite	biological process	Any process which modulates appetite, the desire or physical craving for food. [GOC:add]
mucus secretion	biological process	The regulated release of mucus by the mucosa. Mucus is a viscous slimy secretion consisting of mucins and various inorganic salts dissolved in water, with suspended epithelial cells and leukocytes. The mucosa, or mucous membrane, is the membrane covered with epithelium that lines the tubular organs of the body. Mucins are carbohydrate-rich glycoproteins that have a lubricating and protective function. [GOC:add, ISBN:068340007X, ISBN:0721662544]
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]
large intestinal transit	biological process	Migration of ingested material along the length of the large intestine. [GOC:sl, PMID:28157109]
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	biological process	A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [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]
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]