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5-HT2B receptor

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 7

Nomenclature: 5-HT2B receptor

Family: 5-Hydroxytryptamine receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 481 2q37.1 HTR2B 5-hydroxytryptamine receptor 2B 16,19,44
Mouse 7 479 1 C5 Htr2b 5-hydroxytryptamine (serotonin) receptor 2B 20
Rat 7 479 9q35 Htr2b 5-hydroxytryptamine receptor 2B 17
Previous and Unofficial Names Click here for help
5-HT2F [17,50] | 5-HT2B | serotonin receptor 2B | stomach fundus serotonin receptor | 5-hydroxytryptamine (serotonin) receptor 2B, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRdb 5ht2b_human (Hs), 5ht2b_mouse (Mm), 5ht2b_rat (Rn)
Other databases
Alphafold P41595 (Hs), Q02152 (Mm), P30994 (Rn)
ChEMBL Target CHEMBL1833 (Hs), CHEMBL2583 (Mm), CHEMBL323 (Rn)
DrugBank Target P41595 (Hs)
Ensembl Gene ENSG00000135914 (Hs), ENSMUSG00000026228 (Mm), ENSRNOG00000017625 (Rn)
Entrez Gene 3357 (Hs), 15559 (Mm), 29581 (Rn)
Human Protein Atlas ENSG00000135914 (Hs)
KEGG Gene hsa:3357 (Hs), mmu:15559 (Mm), rno:29581 (Rn)
OMIM 601122 (Hs)
Pharos P41595 (Hs)
RefSeq Nucleotide NM_000867 (Hs), NM_008311 (Mm), NM_017250 (Rn)
RefSeq Protein NP_000858 (Hs), NP_032337 (Mm), NP_058946 (Rn)
UniProtKB P41595 (Hs), Q02152 (Mm), P30994 (Rn)
Wikipedia HTR2B (Hs)
Selected 3D Structures Click here for help
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:  49
Natural/Endogenous Ligands Click here for help
5-hydroxytryptamine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.7 pKd 38
⤷ pKd 8.7 (Kd 2.1x10-9 M) [38]
[3H]5-HT Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Full agonist 8.1 pKd 50
⤷ pKd 8.1 (Kd 8x10-9 M) [50]
[125I]DOI Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 7.6 – 7.7 pKd
⤷ pKd 7.6 – 7.7 (Kd 2.5x10-8 – 2x10-8 M)
methylergonovine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 9.3 pKi 14,41
⤷ pKi 9.3 [14,41]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 14
⤷ pKi 9.0 [14]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.9 pKi 27
⤷ pKi 8.9 [27]
methysergide Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.0 – 9.4 pKi 14,41,51
⤷ pKi 8.0 – 9.4 [14,41,51]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.5 – 8.9 pKi 14,41
⤷ pKi 8.5 – 8.9 [14,41]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Biased agonist 8.4 pKi 49
⤷ pKi 8.4 [49]
Description: Biased for β-arrestin sihnalling.
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.4 pKi 25
⤷ pKi 8.4 [25]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.3 pKi 33
⤷ pKi 8.3 [33]
AL-37350A Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.3 pKi 23
⤷ pKi 8.3 [23]
Ro 60-0175 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.3 pKi 14
⤷ pKi 8.3 (Ki 5.01x10-9 M) [14]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.2 pKi 27
⤷ pKi 8.2 [27]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 8.2 pKi 50
⤷ pKi 8.2 [50]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.9 – 8.4 pKi 2,14,16,23,41
⤷ pKi 7.9 – 8.4 [2,14,16,23,41]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.9 – 8.3 pKi 2,14,16
⤷ pKi 7.9 – 8.3 [2,14,16]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 8.0 pKi 50
⤷ pKi 8.0 [50]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.0 pKi 50
⤷ pKi 8.0 [50]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 8.0 pKi 50
⤷ pKi 8.0 [50]
(+)-norfenfluramine Small molecule or natural product Hs Full agonist 8.0 pKi 41
⤷ pKi 8.0 [41]
BW723C86 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 – 8.6 pKi 2,14,42
⤷ pKi 7.3 – 8.6 (Ki 5.01x10-8 – 2.51x10-9 M) [2,14,42]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.4 – 8.5 pKi 14,32,41-42,51
⤷ pKi 7.4 – 8.5 [14,32,41-42,51]
RU 24969 Small molecule or natural product Rn Full agonist 7.8 pKi 50
⤷ pKi 7.8 [50]
DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.6 – 7.7 pKi 16,32,42
⤷ pKi 7.6 – 7.7 (Ki 2.51x10-8 – 1.99x10-8 M) [16,32,42]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 7.6 pKi 50
⤷ pKi 7.6 [50]
DOI Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.6 pKi 16,50
⤷ pKi 7.6 [16,50]
(+)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.6 pKi 14
⤷ pKi 7.6 [14]
relenopride Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.5 pKi 12
⤷ pKi 7.5 (Ki 3.1x10-8 M) [12]
(R)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 – 7.7 pKi 14,23,34
⤷ pKi 7.7 [23]
pKi 7.3 – 7.4 [14,34]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 – 7.6 pKi 14,32
⤷ pKi 7.4 – 7.6 [14,32]
VER-3323 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 14
⤷ pKi 7.5 [14]
dihydroergocryptine Small molecule or natural product Hs Biased agonist 7.5 pKi 49
⤷ pKi 7.5 [49]
Description: Biased for β-arrestin signalling.
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 7.4 pKi 37
⤷ pKi 7.4 [37]
ORG-37684 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 14
⤷ pKi 7.4 [14]
norfenfluramine Small molecule or natural product Hs Full agonist 7.3 pKi 41
⤷ pKi 7.3 [41]
(-)-norfenfluramine Small molecule or natural product Hs Full agonist 7.3 pKi 41
⤷ pKi 7.3 [41]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pKi 14
⤷ pKi 7.2 [14]
TFMPP Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.1 pKi 50
⤷ pKi 7.1 [50]
quipazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.1 pKi 14
⤷ pKi 7.1 [14]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.0 pKi 14
⤷ pKi 7.0 [14]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.0 pKi 50
⤷ pKi 7.0 [50]
Org 12962 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.0 pKi 14
⤷ pKi 7.0 [14]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 14
⤷ pKi 6.9 [14]
quipazine Small molecule or natural product Rn Full agonist 6.9 pKi 50
⤷ pKi 6.9 [50]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.7 – 6.9 pKi 14,16
⤷ pKi 6.7 – 6.9 [14,16]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 6.8 pKi 16,50
⤷ pKi 6.8 [16,50]
lorcaserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.8 pKi 48
⤷ pKi 6.8 [48]
2-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.6 pKi 50
⤷ pKi 6.6 [50]
MK-212 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.2 – 6.8 pKi 14,42
⤷ pKi 6.2 – 6.8 [14,42]
MK-212 Small molecule or natural product Rn Full agonist 6.4 pKi 50
⤷ pKi 6.4 [50]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.2 pKi 37
⤷ pKi 6.2 [37]
CGS-12066 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.1 pKi 14
⤷ pKi 6.1 [14]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.8 pKi 35
⤷ pKi 5.8 [35]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.8 pKi 37
⤷ pKi 5.8 [37]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.8 pKi 28
⤷ pKi 5.8 [28]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.0 – 6.5 pKi 14,27
⤷ pKi 5.0 – 6.5 [14,27]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.7 pKi 14
⤷ pKi 5.7 [14]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 14
⤷ pKi 5.4 [14]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.4 pKi 50
⤷ pKi 5.4 [50]
lorcaserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.0 pEC50 48
⤷ pEC50 6.0 [48]
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 Value Parameter Reference
balovaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 11.6 pKd 45
⤷ pKd 11.6 (Kd 2.7x10-12 M) [45]
[3H]rauwolscine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 8.4 pKd 51
⤷ pKd 8.4 [51]
[3H]mesulergine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Inverse agonist 7.9 pKd 14
⤷ pKd 7.9 (Kd 1.29x10-8 M) [14]
BF-1 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Antagonist 10.1 pKi 43
⤷ pKi 10.1 [43]
RS-127445 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 – 9.5 pKi 3,14
⤷ pKi 9.0 – 9.5 (Ki 1x10-9 – 3.2x10-10 M) [3,14]
EGIS-7625 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 pKi 15
⤷ pKi 9.0 (Ki 1x10-9 M) [15]
LY53857 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 – 9.1 pKi 51
⤷ pKi 8.8 – 9.1 [51]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.7 – 9.2 pKi 14,51
⤷ pKi 8.7 – 9.2 [14,51]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.7 – 9.2 pKi 3,14,39,51
⤷ pKi 8.7 – 9.2 [3,14,39,51]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.9 pKi 27
⤷ pKi 8.9 [27]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 14
⤷ pKi 8.8 [14]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 – 9.0 pKi 16,51
⤷ pKi 8.4 – 9.0 [16,51]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 – 8.8 pKi 14-15,51
⤷ pKi 8.5 – 8.8 [14-15,51]
SB 221284 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 14
⤷ pKi 8.6 [14]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.0 – 8.8 pKi 14,25,51
⤷ pKi 8.0 – 8.8 [14,25,51]
tegaserod Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.4 pKi 2
⤷ pKi 8.4 [2]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.3 – 8.4 pKi 16,50
⤷ pKi 8.3 – 8.4 [16,50]
mianserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.9 – 8.8 pKi 3,14,51
⤷ pKi 7.9 – 8.8 [3,14,51]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.3 pKi 50
⤷ pKi 8.3 [50]
SB 215505 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 39
⤷ pKi 8.3 [39]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.2 pKi 27
⤷ pKi 8.2 [27]
metergoline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.2 pKi 50
⤷ pKi 8.2 [50]
LY53857 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.2 pKi 50
⤷ pKi 8.2 [50]
rauwolscine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 – 8.4 pKi 51
⤷ pKi 7.8 – 8.4 [51]
SB 206553 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.6 – 8.5 pKi 2,14
⤷ pKi 7.6 – 8.5 [2,14]
SB 228357 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 – 8.1 pKi 5,39
⤷ pKi 8.0 – 8.1 [5,39]
amesergide Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.0 pKi 50
⤷ pKi 8.0 [50]
LY86057 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.9 pKi 50
⤷ pKi 7.9 [50]
xanomeline Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.7 pKi 53
⤷ pKi 7.7 [53]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.4 – 7.9 pKi 3,16,51
⤷ pKi 7.4 – 7.9 [3,16,51]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 27
⤷ pKi 7.5 [27]
rauwolscine Small molecule or natural product Rn Antagonist 7.4 pKi 50
⤷ pKi 7.4 [50]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.4 pKi 50
⤷ pKi 7.4 [50]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.3 pKi 27
⤷ pKi 7.3 [27]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.3 pKi 50
⤷ pKi 7.3 [50]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.3 pKi 50
⤷ pKi 7.3 [50]
trazodone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.1 pKi 14,41
⤷ pKi 7.1 [14,41]
SB 243213 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.0 pKi 5
⤷ pKi 7.0 [5]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.9 pKi 27
⤷ pKi 6.9 [27]
SB 242084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 – 7.0 pKi 13-14
⤷ pKi 6.8 – 7.0 [13-14]
SB 204741 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.9 pKi 14
⤷ pKi 6.9 [14]
S33084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 26
⤷ pKi 6.8 [26]
SDZ SER-082 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pKi 14
⤷ pKi 6.7 [14]
agomelatine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.6 pKi 24
⤷ pKi 6.6 [24]
sarpogrelate Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.6 pKi 38
⤷ pKi 6.6 [38]
spiroxatrine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 – 6.8 pKi 51
⤷ pKi 6.3 – 6.8 [51]
piboserod Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 – 6.6 pKi 2,11
⤷ pKi 6.6 [2]
pKi 6.3 [11]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.1 – 6.7 pKi 6,14,16,38,51
⤷ pKi 6.1 – 6.7 [6,14,16,38,51]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.9 – 6.5 pKi 14,16,51
⤷ pKi 5.9 – 6.5 [14,16,51]
L-741,626 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 26
⤷ pKi 6.2 [26]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.8 – 6.4 pKi 51
⤷ pKi 5.8 – 6.4 [51]
RS-102221 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 – 6.1 pKi 4,14
⤷ pKi 6.0 – 6.1 [4,14]
spiramide Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 14
⤷ pKi 6.0 [14]
volinanserin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 14,39
⤷ pKi 6.0 [14,39]
piribedil Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 27
⤷ pKi 5.9 [27]
SB 224289 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 14
⤷ pKi 5.9 [14]
SB 277011-A Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 40
⤷ pKi 5.9 [40]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.7 pKi 14
⤷ pKi 5.7 [14]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 5.5 pKi 50
⤷ pKi 5.5 [50]
glemanserin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.5 pKi 14
⤷ pKi 5.5 [14]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 5.4 pKi 50
⤷ pKi 5.4 [50]
fluoxetine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.3 pKi 41
⤷ pKi 5.3 [41]
norfluoxetine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.3 pKi 41
⤷ pKi 5.3 [41]
melatonin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 5.2 pKi 24
⤷ pKi 5.2 [24]
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.
Immunopharmacology Comments
The expression of 5-HT2B receptors on immune cells indicates that it plays some part in immune/inflammatory responses [52].
Cell Type Associations
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   mature eosinophil (CL:0000041)
Comment:  Expressed by eosinophils.
References:  52
Immuno Cell Type:  Dendritic cells
Cell Ontology Term:   dendritic cell (CL:0000451)
Comment:  Expressed by DCs.
References:  1,46,52
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   microglial cell (CL:0000129)
macrophage (CL:0000235)
Comment:  Expressed by microglia. 5-HT2B receptor activation has also been shown to promote anti-inflammatory macrophage polarization.
References:  1,9,46,52
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Immuno Process:  Antigen presentation
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family
References:  18,21
Tissue Distribution Click here for help
Uterus, trachea, small intestine > liver, heart, ovary, skeletal muscle, brain, kidney, testis, placenta, prostate, pancreas.
Species:  Human
Technique:  RT-PCR.
References:  16
Stomach > small intestine, large intestine > heart, lung, kidney, cerebellum > cerebrum.
Species:  Mouse
Technique:  RT-PCR.
References:  7
Renal artery.
Species:  Rat
Technique:  Western blotting and immunohistochemistry.
References:  54
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  47
Expression Datasets Click here for help

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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 Click here for help
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:  22
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:  36
Physiological Functions Click here for help
Contraction.
Species:  Rat
Tissue:  Stomach fundus.
References:  8
Endothelium-dependent relaxation.
Species:  Rat
Tissue:  Jugular vein.
References:  10
Regulation of the differentiation and proliferation of the developing and adult heart.
Species:  Mouse
Tissue:  In vivo.
References:  29-30
Physiological Consequences of Altering Gene Expression Click here for help
5-HT2B receptor knockout mice exhibit gross heart defects.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  29-30
Overexpression of the 5-HT2B receptor in the heart causes mitochondrial proliferation leading to ventricular hypertrophy.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  31
Phenotypes, Alleles and Disease Models Click here for help 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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