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5-HT2B

Previous and Unofficial Names
Names References
5-HT2F 207,214
Structural Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Name Reference
Human 7 481 2q36.3-q37.1 HTR2B 208-210
Rat 7 479 9q35 Htr2b 207
Mouse 7 504 1 C5 Htr2b 211
Contents:
Previous and Unofficial Names
Structural Information
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Database Links
ChEMBL Target 227 (Hs), 10021 (Mm), 12688 (Rn)
Ensembl ENSG00000135914 (Hs), ENSMUSG00000026228 (Mm), ENSRNOG00000017625 (Rn)
Entrez Gene 3357 (Hs), 15559 (Mm), 29581 (Rn)
GeneCards HTR2B (Hs)
HomoloGene 55492 (Hs)
OMIM 601122 (Hs)
PharmGKB Gene PA29554 (Hs)
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)
UniGene Hs. 421649 (Hs)
UniProt P41595 (Hs), Q02152 (Mm), P30994 (Rn)
Wikipedia 5-HT2B
Search for 3D structures on the PDB
Search using keywords: 5-Hydroxytryptamine receptors 5-HT2B Search using accession numbers: P30994 || P41595 || Q02152
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 202
methylergonovine Hs Partial agonist 9.3 pKi 182,190
(+)-LSD Hs Full agonist 9.0 pKi 182
cabergoline Hs Full agonist 8.9 pKi 69
ergotamine Hs Partial agonist 8.5 – 8.9 pKi 182,190
methysergide Hs Partial agonist 8.0 – 9.4 pKi 182,190,222
S 16924 Hs Full agonist 8.4 pKi 66
AL-37350A Hs Full agonist 8.3 pKi 186
LSD Rn Full agonist 8.3 pKi 61
Ro 60-0175 Hs Full agonist 8.3 pKi 182
methysergide Rn Partial agonist 8.2 pKi 214
pergolide Hs Full agonist 8.2 pKi 69
5-HT Hs Full agonist 7.9 – 8.4 pKi 182,186,190,209,221
5-HT Rn Full agonist 8.1 pKi 214
α-methyl-5-HT Hs Full agonist 7.9 – 8.3 pKi 182,209,221
5-HT Rn Full agonist 8.0 pKi 214
5-MeOT Rn Full agonist 8.0 pKi 214
α-methyl-5-HT Rn Full agonist 8.0 pKi 214
(+)-norfenfluramine Hs Full agonist 8.0 pKi 190
BW723C86 Hs Full agonist 7.3 – 8.6 pKi 182,221,223
m-CPP Hs Partial agonist 7.4 – 8.5 pKi 182,190,192,222-223
RU 24969 Rn Full agonist 7.8 pKi 214
(R)-DOI Hs Full agonist 7.7 pKi 186
DOI Hs Full agonist 7.6 – 7.7 pKi 192,209,223
DOI Rn Full agonist 7.6 pKi 209,214
(+)-DOI Hs Full agonist 7.6 pKi 182
m-CPP Rn Partial agonist 7.6 pKi 214
DOB Hs Full agonist 7.4 – 7.6 pKi 182,192
VER-3323 Hs Full agonist 7.5 pKi 182
BRL-15572 Hs Partial agonist 7.4 pKi 58
org 37684 Hs Full agonist 7.4 pKi 182
(R)-DOI Hs Full agonist 7.3 – 7.4 pKi 182,185
(-)-norfenfluramine Hs Full agonist 7.3 pKi 190
(±)-norfenfluramine Hs Full agonist 7.3 pKi 190
TFMPP Hs Full agonist 7.2 pKi 182
quipazine Hs Full agonist 7.1 pKi 182
TFMPP Rn Full agonist 7.1 pKi 214
org 12962 Hs Full agonist 7.0 pKi 182
tryptamine Rn Full agonist 7.0 pKi 214
tryptamine Hs Full agonist 7.0 pKi 182
quipazine Rn Full agonist 6.9 pKi 214
RU 24969 Hs Full agonist 6.9 pKi 182
5-CT Rn Full agonist 6.8 pKi 209,214
5-CT Hs Full agonist 6.7 – 6.9 pKi 182,209
2-methyl-5-HT Rn Full agonist 6.6 pKi 214
MK-212 Hs Full agonist 6.2 – 6.8 pKi 182,223
MK-212 Rn Full agonist 6.4 pKi 214
GR-127935 Hs Partial agonist 6.2 pKi 58
CGS-12066 Hs Full agonist 6.1 pKi 182
LY344864 Hs Full agonist 5.8 pKi 64
SB 216641 Hs Partial agonist 5.8 pKi 58
SL65.0155 Hs Partial agonist 5.8 pKi 67
quinpirole Hs Full agonist 5.0 – 6.5 pKi 69,182
pindolol Hs Full agonist 5.7 pKi 182
8-OH-DPAT Rn Full agonist 5.4 pKi 214
8-OH-DPAT Hs Full agonist 5.4 pKi 182
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 222
RS-127445 Hs Antagonist 9.5 pKi 224
EGIS-7625 Hs Antagonist 9.0 pKi 195
RS-127445 Hs Antagonist 9.0 pKi 182
LY53857 Hs Antagonist 8.8 – 9.1 pKi 222
methiothepin Hs Antagonist 8.7 – 9.2 pKi 182,222
ritanserin Hs Antagonist 8.7 – 9.2 pKi 182,197,222,224
lisuride Hs Antagonist 8.9 pKi 69
metergoline Hs Antagonist 8.8 pKi 182
1-naphthylpiperazine Hs Antagonist 8.4 – 9.0 pKi 209,222
mesulergine Hs Antagonist 8.5 – 8.8 pKi 182,195,222
SB 221284 Hs Antagonist 8.6 pKi 182
clozapine Hs Antagonist 8.0 – 8.8 pKi 66,182,222
tegaserod Hs Antagonist 8.4 pKi 221
1-naphthylpiperazine Rn Antagonist 8.3 – 8.4 pKi 209,214
mianserin Hs Antagonist 7.9 – 8.8 pKi 182,222,224
ritanserin Rn Antagonist 8.3 pKi 214
SB 215505 Hs Antagonist 8.3 pKi 197
LY53857 Rn Antagonist 8.2 pKi 214
metergoline Rn Antagonist 8.2 pKi 214
terguride Hs Antagonist 8.2 pKi 69
rauwolscine Hs Antagonist 7.8 – 8.4 pKi 222
SB 206553 Hs Antagonist 7.6 – 8.5 pKi 182,221
SB 228357 Hs Antagonist 8.0 – 8.1 pKi 197,200
amesergide Rn Antagonist 8.0 pKi 214
LY86057 Rn Antagonist 7.9 pKi 214
xanomeline Hs Antagonist 7.7 pKi 73
yohimbine Hs Antagonist 7.4 – 7.9 pKi 209,222,224
roxindole Hs Antagonist 7.5 pKi 69
mesulergine Rn Antagonist 7.4 pKi 214
rauwolscine Rn Antagonist 7.4 pKi 214
bromocriptine Hs Antagonist 7.3 pKi 69
mianserin Rn Antagonist 7.3 pKi 214
yohimbine Rn Antagonist 7.3 pKi 214
trazodone Hs Antagonist 7.1 pKi 182,190
SB 243213 Hs Antagonist 7.0 pKi 200
apomorphine Hs Antagonist 6.9 pKi 69
SB 204741 Hs Antagonist 6.9 pKi 182
SB 242084 Hs Antagonist 6.8 – 7.0 pKi 182,201
S33084 Hs Antagonist 6.8 pKi 75
SDZ SER-082 Hs Antagonist 6.7 pKi 182
agomelatine Hs Antagonist 6.6 pKi 203
piboserod Hs Antagonist 6.6 pKi 221
sarpogrelate Hs Antagonist 6.6 pKi 202
spiroxatrine Hs Antagonist 6.3 – 6.8 pKi 222
ketanserin Hs Antagonist 6.1 – 6.7 pKi 182,196,202,209,222
piboserod Hs Antagonist 6.3 pKi 225
L-741,626 Hs Antagonist 6.2 pKi 75
spiperone Hs Antagonist 5.9 – 6.5 pKi 182,209,222
haloperidol Hs Antagonist 5.8 – 6.4 pKi 222
RS-102221 Hs Antagonist 6.0 – 6.1 pKi 182,198
AMI-193 Hs Antagonist 6.0 pKi 182
MDL-100,907 Hs Antagonist 6.0 pKi 182,197
piribedil Hs Antagonist 5.9 pKi 69
SB 224289 Hs Antagonist 5.9 pKi 182
SB 277011-A Hs Antagonist 5.9 pKi 147
pindolol Hs Antagonist 5.7 pKi 182
MDL-11,939 Hs Antagonist 5.5 pKi 182
spiperone Rn Antagonist 5.5 pKi 214
ketanserin Rn Antagonist 5.4 pKi 214
fluoxetine Hs Antagonist 5.3 pKi 190
norfluoxetine Hs Antagonist 5.3 pKi 190
melatonin Hs Antagonist 5.2 pKi 203
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:  212-213
Tissue Distribution
Uterus, trachea, small intestine > liver, heart, ovary, skeletal muscle, brain, kidney, testis, placenta, prostate, pancreas.
Species:  Human
Technique:  RT-PCR.
References:  209
Stomach > small intestine, large intestine > heart, lung, kidney, cerebellum > cerebrum.
Species:  Mouse
Technique:  RT-PCR.
References:  218
Renal artery.
Species:  Rat
Technique:  Western blotting and immunohistochemistry.
References:  173
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  116
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:  167
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:  168
Physiological Functions
Contraction.
Species:  Rat
Tissue:  Stomach fundus.
References:  219
Endothelium-dependent relaxation.
Species:  Rat
Tissue:  Jugular vein.
References:  220
Regulation of the differentiation and proliferation of the developing and adult heart.
Species:  Mouse
Tissue:  In vivo.
References:  215-216
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:  215-216
Overexpression of the 5-HT2B receptor in the heart causes mitochondrial proliferation leading to ventricular hypertrophy.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  217

To cite this receptor data 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. Last modified on 2010-06-28. Accessed on 2010-09-03. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=7.


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