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5-HT2B receptor

Family: 5-Hydroxytryptamine receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Selected 3D Structures
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 481 2q36.3-q37.1 HTR2B 5-hydroxytryptamine (serotonin) receptor 2B, G protein-coupled 13,16,40
Mouse 7 504 1 C5 Htr2b 5-hydroxytryptamine (serotonin) receptor 2B 17
Rat 7 479 9q35 Htr2b 5-hydroxytryptamine (serotonin) receptor 2B, G protein-coupled 14
Previous and Unofficial Names
Names References
5-HT2F 14,44
5-HT(2B)
5-HT2B
5-hydroxytryptamine (serotonin) receptor 2B
5-HT-2B
5-HT-2F
5-hydroxytryptamine receptor 2B
serotonin receptor 2B
stomach fundus serotonin receptor
AJ012488
AV377389
Database Links
ChEMBL Target 227 (Hs), 10021 (Mm), 12688 (Rn)
DrugBank Target 436 (Hs)
Ensembl ENSG00000135914 (Hs), ENSMUSG00000026228 (Mm), ENSRNOG00000017625 (Rn)
Entrez Gene 3357 (Hs), 15559 (Mm), 29581 (Rn)
GeneCards HTR2B (Hs)
GenitoUrinary Development Molecular Anatomy Project Htr2b (Mm)
HomoloGene 55492 (Hs)
Human Protein Reference Database 03077 (Hs)
InterPro P41595 (Hs), Q02152 (Mm), P30994 (Rn)
KEGG Gene hsa:3357 (Hs), mmu:15559 (Mm), rno:29581 (Rn)
OMIM 601122 (Hs)
PharmGKB Gene PA29554 (Hs)
PhosphoSitePlus P41595 (Hs), Q02152 (Mm), P30994 (Rn)
Protein Ontology (PRO) PRO:000001167 (Hs)
RefSeq Nucleotide NM_000867 (Hs), NM_008311 (Mm), NM_017250 (Rn)
RefSeq Protein NP_000858 (Hs), NP_032337 (Mm), NP_058946 (Rn)
TreeFam ENSG00000135914 (Hs), ENSMUSG00000026228 (Mm), ENSRNOG00000017625 (Rn)
UniGene Hs. 421649 (Hs)
UniProt P41595 (Hs), Q02152 (Mm), P30994 (Rn)
Wikipedia 5-HT2B receptor
5-Hydroxytryptamine receptors
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the chimeric protein of 5-HT2B-BRIL in complex with ergotamine
PDB Id:  4IB4
Ligand:  ergotamine
Resolution:  2.7Å
Species:  Human
References:  43
Search for other structures on the PDB
Search by keyword: 5-Hydroxytryptamine receptors 5-HT2B receptor Search by accession number: P30994, P41595, Q02152
Natural/Endogenous Ligand(s)
5-HT
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]LSD Hs Full agonist 8.7 pKd 35
[3H]5-HT Rn Full agonist 8.1 pKd 44
methylergonovine Hs Partial agonist 9.3 pKi 11,38
(+)-LSD Hs Full agonist 9.0 pKi 11
cabergoline Hs Full agonist 8.9 pKi 24
ergotamine Hs Partial agonist 8.5 – 8.9 pKi 11,38
methysergide Hs Partial agonist 8.0 – 9.4 pKi 11,38,45
S 16924 Hs Full agonist 8.4 pKi 22
AL-37350A Hs Full agonist 8.3 pKi 20
LSD Rn Full agonist 8.3 pKi 30
Ro 60-0175 Hs Full agonist 8.3 pKi 11
methysergide Rn Partial agonist 8.2 pKi 44
pergolide Hs Full agonist 8.2 pKi 24
5-HT Hs Full agonist 7.9 – 8.4 pKi 1,11,13,20,38
α-methyl-5-HT Hs Full agonist 7.9 – 8.3 pKi 1,11,13
5-HT Rn Full agonist 8.0 pKi 44
5-MeOT Rn Full agonist 8.0 pKi 44
α-methyl-5-HT Rn Full agonist 8.0 pKi 44
(+)-norfenfluramine Hs Full agonist 8.0 pKi 38
BW723C86 Hs Full agonist 7.3 – 8.6 pKi 1,11,39
m-CPP Hs Partial agonist 7.4 – 8.5 pKi 11,29,38-39,45
RU 24969 Rn Full agonist 7.8 pKi 44
(R)-DOI Hs Full agonist 7.7 pKi 20
DOI Hs Full agonist 7.6 – 7.7 pKi 13,29,39
DOI Rn Full agonist 7.6 pKi 13,44
(+)-DOI Hs Full agonist 7.6 pKi 11
m-CPP Rn Partial agonist 7.6 pKi 44
DOB Hs Full agonist 7.4 – 7.6 pKi 11,29
VER-3323 Hs Full agonist 7.5 pKi 11
BRL-15572 Hs Partial agonist 7.4 pKi 34
org 37684 Hs Full agonist 7.4 pKi 11
(R)-DOI Hs Full agonist 7.3 – 7.4 pKi 11,31
(-)-norfenfluramine Hs Full agonist 7.3 pKi 38
(±)-norfenfluramine Hs Full agonist 7.3 pKi 38
TFMPP Hs Full agonist 7.2 pKi 11
quipazine Hs Full agonist 7.1 pKi 11
TFMPP Rn Full agonist 7.1 pKi 44
org 12962 Hs Full agonist 7.0 pKi 11
tryptamine Rn Full agonist 7.0 pKi 44
tryptamine Hs Full agonist 7.0 pKi 11
quipazine Rn Full agonist 6.9 pKi 44
RU 24969 Hs Full agonist 6.9 pKi 11
5-CT Hs Full agonist 6.7 – 6.9 pKi 11,13
5-CT Rn Full agonist 6.8 pKi 13,44
lorcaserin Hs Full agonist 6.8 pKi 42
2-methyl-5-HT Rn Full agonist 6.6 pKi 44
MK-212 Hs Full agonist 6.2 – 6.8 pKi 11,39
MK-212 Rn Full agonist 6.4 pKi 44
GR-127935 Hs Partial agonist 6.2 pKi 34
CGS-12066 Hs Full agonist 6.1 pKi 11
LY344864 Hs Full agonist 5.8 pKi 32
SB 216641 Hs Partial agonist 5.8 pKi 34
SL65.0155 Hs Partial agonist 5.8 pKi 25
quinpirole Hs Full agonist 5.0 – 6.5 pKi 11,24
pindolol Hs Full agonist 5.7 pKi 11
8-OH-DPAT Rn Full agonist 5.4 pKi 44
8-OH-DPAT Hs Full agonist 5.4 pKi 11
lorcaserin Hs Full agonist 6.0 pEC50 42
View species-specific agonist tables
Agonist Comments
Methysergide is a low intrinsic efficacy partial agonist, although in some functional assays it may behave as an antagonist.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]rauwolscine Hs Antagonist 8.4 pKd 45
RS-127445 Hs Antagonist 9.0 – 9.5 pKi 2,11
EGIS-7625 Hs Antagonist 9.0 pKi 12
LY53857 Hs Antagonist 8.8 – 9.1 pKi 45
methiothepin Hs Antagonist 8.7 – 9.2 pKi 11,45
ritanserin Hs Antagonist 8.7 – 9.2 pKi 2,11,36,45
lisuride Hs Antagonist 8.9 pKi 24
metergoline Hs Antagonist 8.8 pKi 11
1-naphthylpiperazine Hs Antagonist 8.4 – 9.0 pKi 13,45
mesulergine Hs Antagonist 8.5 – 8.8 pKi 11-12,45
SB 221284 Hs Antagonist 8.6 pKi 11
clozapine Hs Antagonist 8.0 – 8.8 pKi 11,22,45
tegaserod Hs Antagonist 8.4 pKi 1
1-naphthylpiperazine Rn Antagonist 8.3 – 8.4 pKi 13,44
mianserin Hs Antagonist 7.9 – 8.8 pKi 2,11,45
ritanserin Rn Antagonist 8.3 pKi 44
SB 215505 Hs Antagonist 8.3 pKi 36
LY53857 Rn Antagonist 8.2 pKi 44
metergoline Rn Antagonist 8.2 pKi 44
terguride Hs Antagonist 8.2 pKi 24
rauwolscine Hs Antagonist 7.8 – 8.4 pKi 45
SB 206553 Hs Antagonist 7.6 – 8.5 pKi 1,11
SB 228357 Hs Antagonist 8.0 – 8.1 pKi 4,36
amesergide Rn Antagonist 8.0 pKi 44
LY86057 Rn Antagonist 7.9 pKi 44
xanomeline Hs Antagonist 7.7 pKi 46
yohimbine Hs Antagonist 7.4 – 7.9 pKi 2,13,45
roxindole Hs Antagonist 7.5 pKi 24
mesulergine Rn Antagonist 7.4 pKi 44
rauwolscine Rn Antagonist 7.4 pKi 44
bromocriptine Hs Antagonist 7.3 pKi 24
mianserin Rn Antagonist 7.3 pKi 44
yohimbine Rn Antagonist 7.3 pKi 44
trazodone Hs Antagonist 7.1 pKi 11,38
SB 243213 Hs Antagonist 7.0 pKi 4
apomorphine Hs Antagonist 6.9 pKi 24
SB 204741 Hs Antagonist 6.9 pKi 11
SB 242084 Hs Antagonist 6.8 – 7.0 pKi 10-11
S33084 Hs Antagonist 6.8 pKi 23
SDZ SER-082 Hs Antagonist 6.7 pKi 11
agomelatine Hs Antagonist 6.6 pKi 21
piboserod Hs Antagonist 6.6 pKi 1
sarpogrelate Hs Antagonist 6.6 pKi 35
spiroxatrine Hs Antagonist 6.3 – 6.8 pKi 45
ketanserin Hs Antagonist 6.1 – 6.7 pKi 5,11,13,35,45
piboserod Hs Antagonist 6.3 pKi 9
L-741,626 Hs Antagonist 6.2 pKi 23
spiperone Hs Antagonist 5.9 – 6.5 pKi 11,13,45
haloperidol Hs Antagonist 5.8 – 6.4 pKi 45
RS-102221 Hs Antagonist 6.0 – 6.1 pKi 3,11
AMI-193 Hs Antagonist 6.0 pKi 11
MDL-100,907 Hs Antagonist 6.0 pKi 11,36
piribedil Hs Antagonist 5.9 pKi 24
SB 224289 Hs Antagonist 5.9 pKi 11
SB 277011-A Hs Antagonist 5.9 pKi 37
pindolol Hs Antagonist 5.7 pKi 11
MDL-11,939 Hs Antagonist 5.5 pKi 11
spiperone Rn Antagonist 5.5 pKi 44
ketanserin Rn Antagonist 5.4 pKi 44
fluoxetine Hs Antagonist 5.3 pKi 38
norfluoxetine Hs Antagonist 5.3 pKi 38
melatonin Hs Antagonist 5.2 pKi 21
View species-specific antagonist tables

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

Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family
References:  15,18
Tissue Distribution
Uterus, trachea, small intestine > liver, heart, ovary, skeletal muscle, brain, kidney, testis, placenta, prostate, pancreas.
Species:  Human
Technique:  RT-PCR.
References:  13
Stomach > small intestine, large intestine > heart, lung, kidney, cerebellum > cerebrum.
Species:  Mouse
Technique:  RT-PCR.
References:  6
Renal artery.
Species:  Rat
Technique:  Western blotting and immunohistochemistry.
References:  47
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  41
Expression Datasets

Click here to show/hide data

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 IP and IP3 levels in AV12 cells transfected with the rat 5-HT2B receptor.
Species:  Rat
Tissue:  AV12 cells.
Response measured:  IP and IP3 production.
References:  19
Measurement of intracellular Ca2+ levels using a fluorometric imaging plate reader (FLIPR) in CHO-K1 cells transfected with the human 5-HT2B receptor.
Species:  Human
Tissue:  CHO-K1 cells.
Response measured:  Increase in intracellular [Ca2+].
References:  33
Physiological Functions
Contraction.
Species:  Rat
Tissue:  Stomach fundus.
References:  7
Endothelium-dependent relaxation.
Species:  Rat
Tissue:  Jugular vein.
References:  8
Regulation of the differentiation and proliferation of the developing and adult heart.
Species:  Mouse
Tissue:  In vivo.
References:  26-27
Physiological Consequences of Altering Gene Expression
5-HT2B receptor knockout mice exhibit gross heart defects.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  26-27
Overexpression of the 5-HT2B receptor in the heart causes mitochondrial proliferation leading to ventricular hypertrophy.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  28
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0002127 abnormal cardiovascular system morphology PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0001544 abnormal cardiovascular system physiology PMID: 12244304 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0003567 abnormal fetal cardiomyocyte proliferation PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0000267 abnormal heart development PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0005294 abnormal heart ventricle morphology PMID: 10944220  12244304 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0008775 abnormal heart ventricular pressure PMID: 12244304 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0000230 abnormal systemic arterial blood pressure PMID: 12244304 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0000296 absent trabeculae carneae PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0001262 decreased body weight PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0001698 decreased embryo size PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0002834 decreased heart weight PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0003140 dilated heart atrium PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0002190 disorganized myocardium PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0003984 embryonic growth retardation PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0006207 embryonic lethality during organogenesis PMID: 10944220 
Htr2btm1Dgen Htr2btm1Dgen/Htr2btm1Dgen
involves: 129P2/OlaHsd * C57BL/6		 MGI:109323  MP:0006207 embryonic lethality during organogenesis
Htr2b+|Htr2btm1Dgen Htr2btm1Dgen/Htr2b+
involves: 129P2/OlaHsd * C57BL/6		 MGI:109323  MP:0002169 no abnormal phenotype detected
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0002082 postnatal lethality PMID: 10944220 
Htr2btm1Lum Htr2btm1Lum/Htr2btm1Lum
129S2/SvPas-Htr2b		 MGI:109323  MP:0001921 reduced fertility PMID: 10944220 

REFERENCES

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To cite this database page, please use the following:

Rodrigo Andrade, Nicholas M. Barnes, Gordon Baxter, Joel Bockaert, Theresa Branchek, Marlene L. Cohen, Aline Dumuis, Richard M. Eglen, Manfred Göthert, Mark Hamblin, Michel Hamon, Paul R. Hartig, René Hen, Katharine Herrick-Davis, Rebecca Hills, Daniel Hoyer, Patrick P. A. Humphrey, Klaus Peter Latté, Luc Maroteaux, Graeme R. Martin, Derek N. Middlemiss, Ewan Mylecharane, Stephen J. Peroutka, Pramod R. Saxena, Andrew Sleight, Carlos M. Villalon, Frank Yocca.
5-Hydroxytryptamine receptors: 5-HT2B receptor. Last modified on 12/02/2013. Accessed on 25/05/2013. IUPHAR database (IUPHAR-DB), http://iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=7.


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