Nomenclature: 5-HT2B receptor

Family: 5-Hydroxytryptamine receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates. 

Contents

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
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
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
Natural/Endogenous Ligands
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
pKd 8.7 (Kd 2.1x10-9 M) [35]
[3H]5-HT Rn Full agonist 8.1 pKd 44
pKd 8.1 (Kd 8x10-9 M) [44]
methylergonovine Hs Partial agonist 9.3 pKi 11,38
pKi 9.3 [11,38]
(+)-LSD Hs Full agonist 9.0 pKi 11
pKi 9.0 [11]
cabergoline Hs Full agonist 8.9 pKi 24
pKi 8.9 [24]
ergotamine Hs Partial agonist 8.5 – 8.9 pKi 11,38
pKi 8.5 – 8.9 [11,38]
methysergide Hs Partial agonist 8.0 – 9.4 pKi 11,38,45
pKi 8.0 – 9.4 [11,38,45]
S 16924 Hs Full agonist 8.4 pKi 22
pKi 8.4 [22]
Ro 60-0175 Hs Full agonist 8.3 pKi 11
pKi 8.3 [11]
LSD Rn Full agonist 8.3 pKi 30
pKi 8.3 [30]
AL-37350A Hs Full agonist 8.3 pKi 20
pKi 8.3 [20]
pergolide Hs Full agonist 8.2 pKi 24
pKi 8.2 [24]
methysergide Rn Partial agonist 8.2 pKi 44
pKi 8.2 [44]
5-HT Hs Full agonist 7.9 – 8.4 pKi 1,11,13,20,38
pKi 7.9 – 8.4 [1,11,13,20,38]
α-methyl-5-HT Hs Full agonist 7.9 – 8.3 pKi 1,11,13
pKi 7.9 – 8.3 [1,11,13]
5-MeOT Rn Full agonist 8.0 pKi 44
pKi 8.0 [44]
α-methyl-5-HT Rn Full agonist 8.0 pKi 44
pKi 8.0 [44]
(+)-norfenfluramine Hs Full agonist 8.0 pKi 38
pKi 8.0 [38]
5-HT Rn Full agonist 8.0 pKi 44
pKi 8.0 [44]
BW723C86 Hs Full agonist 7.3 – 8.6 pKi 1,11,39
pKi 7.3 – 8.6 [1,11,39]
m-CPP Hs Partial agonist 7.4 – 8.5 pKi 11,29,38-39,45
pKi 7.4 – 8.5 [11,29,38-39,45]
RU 24969 Rn Full agonist 7.8 pKi 44
pKi 7.8 [44]
DOI Hs Full agonist 7.6 – 7.7 pKi 13,29,39
pKi 7.6 – 7.7 [13,29,39]
m-CPP Rn Partial agonist 7.6 pKi 44
pKi 7.6 [44]
DOI Rn Full agonist 7.6 pKi 13,44
pKi 7.6 [13,44]
(+)-DOI Hs Full agonist 7.6 pKi 11
pKi 7.6 [11]
DOB Hs Full agonist 7.4 – 7.6 pKi 11,29
pKi 7.4 – 7.6 [11,29]
(R)-DOI Hs Full agonist 7.3 – 7.7 pKi 11,20,31
pKi 7.7 [20]
pKi 7.3 – 7.4 [11,31]
VER-3323 Hs Full agonist 7.5 pKi 11
pKi 7.5 [11]
org 37684 Hs Full agonist 7.4 pKi 11
pKi 7.4 [11]
BRL-15572 Hs Partial agonist 7.4 pKi 34
pKi 7.4 [34]
(-)-norfenfluramine Hs Full agonist 7.3 pKi 38
pKi 7.3 [38]
norfenfluramine Hs Full agonist 7.3 pKi 38
pKi 7.3 [38]
TFMPP Hs Full agonist 7.2 pKi 11
pKi 7.2 [11]
TFMPP Rn Full agonist 7.1 pKi 44
pKi 7.1 [44]
quipazine Hs Full agonist 7.1 pKi 11
pKi 7.1 [11]
org 12962 Hs Full agonist 7.0 pKi 11
pKi 7.0 [11]
tryptamine Hs Full agonist 7.0 pKi 11
pKi 7.0 [11]
tryptamine Rn Full agonist 7.0 pKi 44
pKi 7.0 [44]
RU 24969 Hs Full agonist 6.9 pKi 11
pKi 6.9 [11]
quipazine Rn Full agonist 6.9 pKi 44
pKi 6.9 [44]
lorcaserin Hs Full agonist 6.8 pKi 42
pKi 6.8 [42]
5-CT Hs Full agonist 6.7 – 6.9 pKi 11,13
pKi 6.7 – 6.9 [11,13]
5-CT Rn Full agonist 6.8 pKi 13,44
pKi 6.8 [13,44]
2-methyl-5-HT Rn Full agonist 6.6 pKi 44
pKi 6.6 [44]
MK-212 Hs Full agonist 6.2 – 6.8 pKi 11,39
pKi 6.2 – 6.8 [11,39]
MK-212 Rn Full agonist 6.4 pKi 44
pKi 6.4 [44]
GR-127935 Hs Partial agonist 6.2 pKi 34
pKi 6.2 [34]
CGS-12066 Hs Full agonist 6.1 pKi 11
pKi 6.1 [11]
SB 216641 Hs Partial agonist 5.8 pKi 34
pKi 5.8 [34]
SL65.0155 Hs Partial agonist 5.8 pKi 25
pKi 5.8 [25]
LY344864 Hs Full agonist 5.8 pKi 32
pKi 5.8 [32]
quinpirole Hs Full agonist 5.0 – 6.5 pKi 11,24
pKi 5.0 – 6.5 [11,24]
pindolol Hs Full agonist 5.7 pKi 11
pKi 5.7 [11]
8-OH-DPAT Hs Full agonist 5.4 pKi 11
pKi 5.4 [11]
8-OH-DPAT Rn Full agonist 5.4 pKi 44
pKi 5.4 [44]
lorcaserin Hs Full agonist 6.0 pEC50 42
pEC50 6.0 [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
pKd 8.4 [45]
RS-127445 Hs Antagonist 9.0 – 9.5 pKi 2,11
pKi 9.0 – 9.5 [2,11]
EGIS-7625 Hs Antagonist 9.0 pKi 12
pKi 9.0 [12]
LY53857 Hs Antagonist 8.8 – 9.1 pKi 45
pKi 8.8 – 9.1 [45]
methiothepin Hs Antagonist 8.7 – 9.2 pKi 11,45
pKi 8.7 – 9.2 [11,45]
ritanserin Hs Antagonist 8.7 – 9.2 pKi 2,11,36,45
pKi 8.7 – 9.2 [2,11,36,45]
lisuride Hs Antagonist 8.9 pKi 24
pKi 8.9 [24]
metergoline Hs Antagonist 8.8 pKi 11
pKi 8.8 [11]
1-naphthylpiperazine Hs Antagonist 8.4 – 9.0 pKi 13,45
pKi 8.4 – 9.0 [13,45]
mesulergine Hs Antagonist 8.5 – 8.8 pKi 11-12,45
pKi 8.5 – 8.8 [11-12,45]
SB 221284 Hs Antagonist 8.6 pKi 11
pKi 8.6 [11]
clozapine Hs Antagonist 8.0 – 8.8 pKi 11,22,45
pKi 8.0 – 8.8 [11,22,45]
tegaserod Hs Antagonist 8.4 pKi 1
pKi 8.4 [1]
mianserin Hs Antagonist 7.9 – 8.8 pKi 2,11,45
pKi 7.9 – 8.8 [2,11,45]
1-naphthylpiperazine Rn Antagonist 8.3 – 8.4 pKi 13,44
pKi 8.3 – 8.4 [13,44]
SB 215505 Hs Antagonist 8.3 pKi 36
pKi 8.3 [36]
ritanserin Rn Antagonist 8.3 pKi 44
pKi 8.3 [44]
terguride Hs Antagonist 8.2 pKi 24
pKi 8.2 [24]
metergoline Rn Antagonist 8.2 pKi 44
pKi 8.2 [44]
LY53857 Rn Antagonist 8.2 pKi 44
pKi 8.2 [44]
rauwolscine Hs Antagonist 7.8 – 8.4 pKi 45
pKi 7.8 – 8.4 [45]
SB 206553 Hs Antagonist 7.6 – 8.5 pKi 1,11
pKi 7.6 – 8.5 [1,11]
SB 228357 Hs Antagonist 8.0 – 8.1 pKi 4,36
pKi 8.0 – 8.1 [4,36]
amesergide Rn Antagonist 8.0 pKi 44
pKi 8.0 [44]
LY86057 Rn Antagonist 7.9 pKi 44
pKi 7.9 [44]
xanomeline Hs Antagonist 7.7 pKi 46
pKi 7.7 [46]
yohimbine Hs Antagonist 7.4 – 7.9 pKi 2,13,45
pKi 7.4 – 7.9 [2,13,45]
roxindole Hs Antagonist 7.5 pKi 24
pKi 7.5 [24]
mesulergine Rn Antagonist 7.4 pKi 44
pKi 7.4 [44]
rauwolscine Rn Antagonist 7.4 pKi 44
pKi 7.4 [44]
mianserin Rn Antagonist 7.3 pKi 44
pKi 7.3 [44]
yohimbine Rn Antagonist 7.3 pKi 44
pKi 7.3 [44]
bromocriptine Hs Antagonist 7.3 pKi 24
pKi 7.3 [24]
trazodone Hs Antagonist 7.1 pKi 11,38
pKi 7.1 [11,38]
SB 243213 Hs Antagonist 7.0 pKi 4
pKi 7.0 [4]
SB 204741 Hs Antagonist 6.9 pKi 11
pKi 6.9 [11]
apomorphine Hs Antagonist 6.9 pKi 24
pKi 6.9 [24]
SB 242084 Hs Antagonist 6.8 – 7.0 pKi 10-11
pKi 6.8 – 7.0 [10-11]
S33084 Hs Antagonist 6.8 pKi 23
pKi 6.8 [23]
SDZ SER-082 Hs Antagonist 6.7 pKi 11
pKi 6.7 [11]
agomelatine Hs Antagonist 6.6 pKi 21
pKi 6.6 [21]
sarpogrelate Hs Antagonist 6.6 pKi 35
pKi 6.6 [35]
spiroxatrine Hs Antagonist 6.3 – 6.8 pKi 45
pKi 6.3 – 6.8 [45]
piboserod Hs Antagonist 6.3 – 6.6 pKi 1,9
pKi 6.6 [1]
pKi 6.3 [9]
ketanserin Hs Antagonist 6.1 – 6.7 pKi 5,11,13,35,45
pKi 6.1 – 6.7 [5,11,13,35,45]
spiperone Hs Antagonist 5.9 – 6.5 pKi 11,13,45
pKi 5.9 – 6.5 [11,13,45]
L-741,626 Hs Antagonist 6.2 pKi 23
pKi 6.2 [23]
haloperidol Hs Antagonist 5.8 – 6.4 pKi 45
pKi 5.8 – 6.4 [45]
RS-102221 Hs Antagonist 6.0 – 6.1 pKi 3,11
pKi 6.0 – 6.1 [3,11]
spiramide Hs Antagonist 6.0 pKi 11
pKi 6.0 [11]
volinanserin Hs Antagonist 6.0 pKi 11,36
pKi 6.0 [11,36]
SB 224289 Hs Antagonist 5.9 pKi 11
pKi 5.9 [11]
SB 277011-A Hs Antagonist 5.9 pKi 37
pKi 5.9 [37]
piribedil Hs Antagonist 5.9 pKi 24
pKi 5.9 [24]
pindolol Hs Antagonist 5.7 pKi 11
pKi 5.7 [11]
spiperone Rn Antagonist 5.5 pKi 44
pKi 5.5 [44]
glemanserin Hs Antagonist 5.5 pKi 11
pKi 5.5 [11]
ketanserin Rn Antagonist 5.4 pKi 44
pKi 5.4 [44]
norfluoxetine Hs Antagonist 5.3 pKi 38
pKi 5.3 [38]
fluoxetine Hs Antagonist 5.3 pKi 38
pKi 5.3 [38]
melatonin Hs Antagonist 5.2 pKi 21
pKi 5.2 [21]
View species-specific antagonist tables
Antagonist Comments
Mianserin has activity accross several families of GPCRs, including the histamine H1 receptor, 5-HT receptors and α-adrenoceptors, but may have additional actions. The 5-HT2A, 2B and 2C receptors have been tagged as the primary targets of this drug in view of their high affinity. This does not preclude clinically relevant actions at other molecular targets.
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

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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 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
Overexpression of the 5-HT2B receptor in the heart causes mitochondrial proliferation leading to ventricular hypertrophy.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  28
5-HT2B receptor knockout mice exhibit gross heart defects.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  26-27
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