5-HT2B receptor

Target id: 7

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.  » Email us

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 receptor 2B 14,17,42
Mouse 7 504 1 C5 Htr2b 5-hydroxytryptamine (serotonin) receptor 2B 18
Rat 7 479 9q35 Htr2b 5-hydroxytryptamine receptor 2B 15
Previous and Unofficial Names
Names References
5-HT2F 15,46
5-HT2B
serotonin receptor 2B
stomach fundus serotonin receptor
5-hydroxytryptamine (serotonin) receptor 2B, G protein-coupled
Database Links
Specialist databases
GPCRDB 5ht2b_human (Hs), 5ht2b_mouse (Mm), 5ht2b_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
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:  45
Natural/Endogenous Ligands
5-hydroxytryptamine

Download all structure-activity data for this target as a CSV file

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 36
pKd 8.7 (Kd 2.1x10-9 M) [36]
[3H]5-HT Rn Full agonist 8.1 pKd 46
pKd 8.1 (Kd 8x10-9 M) [46]
[125I]DOI Hs Full agonist 7.6 – 7.7 pKd
pKd 7.6 – 7.7 (Kd 2.5x10-8 – 2x10-8 M)
methylergonovine Hs Partial agonist 9.3 pKi 12,39
pKi 9.3 [12,39]
(+)-LSD Hs Full agonist 9.0 pKi 12
pKi 9.0 [12]
cabergoline Hs Full agonist 8.9 pKi 25
pKi 8.9 [25]
methysergide Hs Partial agonist 8.0 – 9.4 pKi 12,39,47
pKi 8.0 – 9.4 [12,39,47]
ergotamine Hs Partial agonist 8.5 – 8.9 pKi 12,39
pKi 8.5 – 8.9 [12,39]
Lysergide Hs Biased agonist 8.4 pKi 45
pKi 8.4 [45]
Description: Biased for β-arrestin sihnalling.
S 16924 Hs Full agonist 8.4 pKi 23
pKi 8.4 [23]
Lysergide Rn Full agonist 8.3 pKi 31
pKi 8.3 [31]
AL-37350A Hs Full agonist 8.3 pKi 21
pKi 8.3 [21]
Ro 60-0175 Hs Full agonist 8.3 pKi 12
pKi 8.3 (Ki 5.01x10-9 M) [12]
pergolide Hs Full agonist 8.2 pKi 25
pKi 8.2 [25]
methysergide Rn Partial agonist 8.2 pKi 46
pKi 8.2 [46]
5-hydroxytryptamine Hs Full agonist 7.9 – 8.4 pKi 1,12,14,21,39
pKi 7.9 – 8.4 [1,12,14,21,39]
α-methyl-5-HT Hs Full agonist 7.9 – 8.3 pKi 1,12,14
pKi 7.9 – 8.3 [1,12,14]
5-hydroxytryptamine Rn Full agonist 8.0 pKi 46
pKi 8.0 [46]
5-MeOT Rn Full agonist 8.0 pKi 46
pKi 8.0 [46]
α-methyl-5-HT Rn Full agonist 8.0 pKi 46
pKi 8.0 [46]
(+)-norfenfluramine Hs Full agonist 8.0 pKi 39
pKi 8.0 [39]
BW723C86 Hs Full agonist 7.3 – 8.6 pKi 1,12,40
pKi 7.3 – 8.6 (Ki 5.01x10-8 – 2.51x10-9 M) [1,12,40]
m-chlorophenylpiperazine Hs Partial agonist 7.4 – 8.5 pKi 12,30,39-40,47
pKi 7.4 – 8.5 [12,30,39-40,47]
RU 24969 Rn Full agonist 7.8 pKi 46
pKi 7.8 [46]
DOI Hs Full agonist 7.6 – 7.7 pKi 14,30,40
pKi 7.6 – 7.7 (Ki 2.51x10-8 – 1.99x10-8 M) [14,30,40]
m-chlorophenylpiperazine Rn Partial agonist 7.6 pKi 46
pKi 7.6 [46]
DOI Rn Full agonist 7.6 pKi 14,46
pKi 7.6 [14,46]
(+)-DOI Hs Full agonist 7.6 pKi 12
pKi 7.6 [12]
relenopride Hs Agonist 7.5 pKi 10
pKi 7.5 (Ki 3.1x10-8 M) [10]
(R)-DOI Hs Full agonist 7.3 – 7.7 pKi 12,21,32
pKi 7.7 [21]
pKi 7.3 – 7.4 [12,32]
brolamfetamine Hs Full agonist 7.4 – 7.6 pKi 12,30
pKi 7.4 – 7.6 [12,30]
VER-3323 Hs Full agonist 7.5 pKi 12
pKi 7.5 [12]
dihydroergocryptine Hs Biased agonist 7.5 pKi 45
pKi 7.5 [45]
Description: Biased for β-arrestin signalling.
BRL-15572 Hs Partial agonist 7.4 pKi 35
pKi 7.4 [35]
ORG-37684 Hs Full agonist 7.4 pKi 12
pKi 7.4 [12]
norfenfluramine Hs Full agonist 7.3 pKi 39
pKi 7.3 [39]
(-)-norfenfluramine Hs Full agonist 7.3 pKi 39
pKi 7.3 [39]
TFMPP Hs Full agonist 7.2 pKi 12
pKi 7.2 [12]
TFMPP Rn Full agonist 7.1 pKi 46
pKi 7.1 [46]
quipazine Hs Full agonist 7.1 pKi 12
pKi 7.1 [12]
tryptamine Hs Full agonist 7.0 pKi 12
pKi 7.0 [12]
tryptamine Rn Full agonist 7.0 pKi 46
pKi 7.0 [46]
Org 12962 Hs Full agonist 7.0 pKi 12
pKi 7.0 [12]
RU 24969 Hs Full agonist 6.9 pKi 12
pKi 6.9 [12]
quipazine Rn Full agonist 6.9 pKi 46
pKi 6.9 [46]
5-CT Hs Full agonist 6.7 – 6.9 pKi 12,14
pKi 6.7 – 6.9 [12,14]
5-CT Rn Full agonist 6.8 pKi 14,46
pKi 6.8 [14,46]
lorcaserin Hs Full agonist 6.8 pKi 44
pKi 6.8 [44]
2-methyl-5-HT Rn Full agonist 6.6 pKi 46
pKi 6.6 [46]
MK-212 Hs Full agonist 6.2 – 6.8 pKi 12,40
pKi 6.2 – 6.8 [12,40]
MK-212 Rn Full agonist 6.4 pKi 46
pKi 6.4 [46]
GR 127935 Hs Partial agonist 6.2 pKi 35
pKi 6.2 [35]
CGS-12066 Hs Full agonist 6.1 pKi 12
pKi 6.1 [12]
LY344864 Hs Full agonist 5.8 pKi 33
pKi 5.8 [33]
SB 216641 Hs Partial agonist 5.8 pKi 35
pKi 5.8 [35]
capeserod Hs Partial agonist 5.8 pKi 26
pKi 5.8 [26]
quinpirole Hs Full agonist 5.0 – 6.5 pKi 12,25
pKi 5.0 – 6.5 [12,25]
pindolol Hs Full agonist 5.7 pKi 12
pKi 5.7 [12]
8-OH-DPAT Hs Full agonist 5.4 pKi 12
pKi 5.4 [12]
8-OH-DPAT Rn Full agonist 5.4 pKi 46
pKi 5.4 [46]
lorcaserin Hs Full agonist 6.0 pEC50 44
pEC50 6.0 [44]
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 47
pKd 8.4 [47]
[3H]mesulergine Hs Inverse agonist 7.9 pKd 12
pKd 7.9 (Kd 1.29x10-8 M) [12]
BF-1 Hs Antagonist 10.1 pKi 41
pKi 10.1 [41]
RS-127445 Hs Antagonist 9.0 – 9.5 pKi 2,12
pKi 9.0 – 9.5 (Ki 1x10-9 – 3.2x10-10 M) [2,12]
EGIS-7625 Hs Antagonist 9.0 pKi 13
pKi 9.0 (Ki 1x10-9 M) [13]
LY53857 Hs Antagonist 8.8 – 9.1 pKi 47
pKi 8.8 – 9.1 [47]
methiothepin Hs Antagonist 8.7 – 9.2 pKi 12,47
pKi 8.7 – 9.2 [12,47]
ritanserin Hs Antagonist 8.7 – 9.2 pKi 2,12,37,47
pKi 8.7 – 9.2 [2,12,37,47]
lisuride Hs Antagonist 8.9 pKi 25
pKi 8.9 [25]
metergoline Hs Antagonist 8.8 pKi 12
pKi 8.8 [12]
1-naphthylpiperazine Hs Antagonist 8.4 – 9.0 pKi 14,47
pKi 8.4 – 9.0 [14,47]
mesulergine Hs Antagonist 8.5 – 8.8 pKi 12-13,47
pKi 8.5 – 8.8 [12-13,47]
SB 221284 Hs Antagonist 8.6 pKi 12
pKi 8.6 [12]
clozapine Hs Antagonist 8.0 – 8.8 pKi 12,23,47
pKi 8.0 – 8.8 [12,23,47]
tegaserod Hs Antagonist 8.4 pKi 1
pKi 8.4 [1]
1-naphthylpiperazine Rn Antagonist 8.3 – 8.4 pKi 14,46
pKi 8.3 – 8.4 [14,46]
mianserin Hs Antagonist 7.9 – 8.8 pKi 2,12,47
pKi 7.9 – 8.8 [2,12,47]
ritanserin Rn Antagonist 8.3 pKi 46
pKi 8.3 [46]
SB 215505 Hs Antagonist 8.3 pKi 37
pKi 8.3 [37]
terguride Hs Antagonist 8.2 pKi 25
pKi 8.2 [25]
metergoline Rn Antagonist 8.2 pKi 46
pKi 8.2 [46]
LY53857 Rn Antagonist 8.2 pKi 46
pKi 8.2 [46]
rauwolscine Hs Antagonist 7.8 – 8.4 pKi 47
pKi 7.8 – 8.4 [47]
SB 206553 Hs Antagonist 7.6 – 8.5 pKi 1,12
pKi 7.6 – 8.5 [1,12]
SB 228357 Hs Antagonist 8.0 – 8.1 pKi 4,37
pKi 8.0 – 8.1 [4,37]
amesergide Rn Antagonist 8.0 pKi 46
pKi 8.0 [46]
LY86057 Rn Antagonist 7.9 pKi 46
pKi 7.9 [46]
xanomeline Hs Antagonist 7.7 pKi 48
pKi 7.7 [48]
yohimbine Hs Antagonist 7.4 – 7.9 pKi 2,14,47
pKi 7.4 – 7.9 [2,14,47]
roxindole Hs Antagonist 7.5 pKi 25
pKi 7.5 [25]
rauwolscine Rn Antagonist 7.4 pKi 46
pKi 7.4 [46]
mesulergine Rn Antagonist 7.4 pKi 46
pKi 7.4 [46]
bromocriptine Hs Antagonist 7.3 pKi 25
pKi 7.3 [25]
yohimbine Rn Antagonist 7.3 pKi 46
pKi 7.3 [46]
mianserin Rn Antagonist 7.3 pKi 46
pKi 7.3 [46]
trazodone Hs Antagonist 7.1 pKi 12,39
pKi 7.1 [12,39]
SB 243213 Hs Antagonist 7.0 pKi 4
pKi 7.0 [4]
apomorphine Hs Antagonist 6.9 pKi 25
pKi 6.9 [25]
SB 242084 Hs Antagonist 6.8 – 7.0 pKi 11-12
pKi 6.8 – 7.0 [11-12]
SB 204741 Hs Antagonist 6.9 pKi 12
pKi 6.9 [12]
S33084 Hs Antagonist 6.8 pKi 24
pKi 6.8 [24]
SDZ SER-082 Hs Antagonist 6.7 pKi 12
pKi 6.7 [12]
agomelatine Hs Antagonist 6.6 pKi 22
pKi 6.6 [22]
sarpogrelate Hs Antagonist 6.6 pKi 36
pKi 6.6 [36]
spiroxatrine Hs Antagonist 6.3 – 6.8 pKi 47
pKi 6.3 – 6.8 [47]
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 5,12,14,36,47
pKi 6.1 – 6.7 [5,12,14,36,47]
spiperone Hs Antagonist 5.9 – 6.5 pKi 12,14,47
pKi 5.9 – 6.5 [12,14,47]
L-741,626 Hs Antagonist 6.2 pKi 24
pKi 6.2 [24]
haloperidol Hs Antagonist 5.8 – 6.4 pKi 47
pKi 5.8 – 6.4 [47]
RS-102221 Hs Antagonist 6.0 – 6.1 pKi 3,12
pKi 6.0 – 6.1 [3,12]
spiramide Hs Antagonist 6.0 pKi 12
pKi 6.0 [12]
volinanserin Hs Antagonist 6.0 pKi 12,37
pKi 6.0 [12,37]
piribedil Hs Antagonist 5.9 pKi 25
pKi 5.9 [25]
SB 224289 Hs Antagonist 5.9 pKi 12
pKi 5.9 [12]
SB 277011-A Hs Antagonist 5.9 pKi 38
pKi 5.9 [38]
pindolol Hs Antagonist 5.7 pKi 12
pKi 5.7 [12]
spiperone Rn Antagonist 5.5 pKi 46
pKi 5.5 [46]
glemanserin Hs Antagonist 5.5 pKi 12
pKi 5.5 [12]
ketanserin Rn Antagonist 5.4 pKi 46
pKi 5.4 [46]
fluoxetine Hs Antagonist 5.3 pKi 39
pKi 5.3 [39]
norfluoxetine Hs Antagonist 5.3 pKi 39
pKi 5.3 [39]
melatonin Hs Antagonist 5.2 pKi 22
pKi 5.2 [22]
View species-specific antagonist tables
Antagonist Comments
Mianserin has activity across 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:  16,19
Tissue Distribution
Uterus, trachea, small intestine > liver, heart, ovary, skeletal muscle, brain, kidney, testis, placenta, prostate, pancreas.
Species:  Human
Technique:  RT-PCR.
References:  14
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:  49
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  43
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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