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5-HT2B receptor

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(Redirected from 5-HT2B) Mammalian protein found in Homo sapiens

HTR2B
Available structures
PDBOrtholog search: PDBe RCSB
List of PDB id codes

4NC3, 4IB4

Identifiers
AliasesHTR2B, 5-HT(2B), 5-HT2B, 5-HT-2B, 5-hydroxytryptamine receptor 2B
External IDsOMIM: 601122; MGI: 109323; HomoloGene: 55492; GeneCards: HTR2B; OMA:HTR2B - orthologs
Gene location (Human)
Chromosome 2 (human)
Chr.Chromosome 2 (human)
Chromosome 2 (human)Genomic location for HTR2BGenomic location for HTR2B
Band2q37.1Start231,108,230 bp
End231,125,042 bp
Gene location (Mouse)
Chromosome 1 (mouse)
Chr.Chromosome 1 (mouse)
Chromosome 1 (mouse)Genomic location for HTR2BGenomic location for HTR2B
Band1|1 C5Start86,026,748 bp
End86,039,692 bp
RNA expression pattern
Bgee
HumanMouse (ortholog)
Top expressed in
  • decidua

  • tail of epididymis

  • stromal cell of endometrium

  • caput epididymis

  • corpus epididymis

  • left adrenal gland

  • left adrenal cortex

  • right adrenal cortex

  • smooth muscle tissue

  • testicle
Top expressed in
  • decidua

  • morula

  • neural groove

  • neural fold

  • embryo

  • tail of embryo

  • genital tubercle

  • calvaria

  • right lung lobe

  • right kidney
More reference expression data
BioGPS
More reference expression data
Gene ontology
Molecular function
Cellular component
Biological process
Sources:Amigo / QuickGO
Orthologs
SpeciesHumanMouse
Entrez

3357

15559

Ensembl

ENSG00000135914

ENSMUSG00000026228

UniProt

P41595

Q02152

RefSeq (mRNA)

NM_000867
NM_001320758

NM_008311

RefSeq (protein)

NP_000858
NP_001307687

NP_032337

Location (UCSC)Chr 2: 231.11 – 231.13 MbChr 1: 86.03 – 86.04 Mb
PubMed search
Wikidata
View/Edit HumanView/Edit Mouse

5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the HTR2B gene. 5-HT2B is a member of the 5-HT2 receptor family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). Like all 5-HT2 receptors, the 5-HT2B receptor is Gq/G11-protein coupled, leading to downstream activation of phospholipase C.

Tissue distribution and function

First discovered in the stomach of rats, 5-HT2B was challenging to characterize initially because of its structural similarity to the other 5-HT2 receptors, particularly 5-HT2C. The 5-HT2 receptors (of which the 5-HT2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system (CNS) effects include neuronal sensitization to tactile stimuli and mediation of some of the effects of hallucinogenic substituted amphetamines. The 5-HT2B receptor is expressed in several areas of the CNS, including the dorsal hypothalamus, frontal cortex, medial amygdala, and meninges. However, its most important role is in the peripheral nervous system (PNS) where it maintains the viability and efficiency of the cardiac valve leaflets.

The 5-HT2B receptor subtype is involved in:

  • CNS: inhibition of serotonin and dopamine uptake, behavioral effects
  • Vascular: pulmonary vasoconstriction
  • Cardiac: The 5-HT2B receptor regulates cardiac structure and functions, as demonstrated by the abnormal cardiac development observed in 5-HT2B receptor null mice. Excessive stimulation of this receptor causes pathological proliferation of cardiac valve fibroblasts, with chronic overstimulation leading to valvulopathy. These receptors are also overexpressed in human failing heart and antagonists of 5-HT2B receptors were discovered to prevent both angiotensin II or beta-adrenergic agonist-induced pathological cardiac hypertrophy in mouse.
  • Serotonin transporter: 5-HT2B receptors regulate serotonin release via the serotonin transporter, and are important both to normal physiological regulation of serotonin levels in blood plasma, and with the abnormal acute serotonin release produced by drugs such as MDMA. Surprisingly, however, 5-HT2B receptor activation appears to be protective against the development of serotonin syndrome following elevated extracellular serotonin levels, despite its role in modulating serotonin release.

Clinical significance

5-HT2B receptors have been strongly implicated in causing drug-induced valvular heart disease. The Fen-Phen scandal in the 80s and 90s revealed the cardiotoxic effects of 5-HT2B stimulation. Today, 5-HT2B agonism is considered a toxicity signal precluding further clinical development of a compound.

Ligands

The structure of the 5-HT2B receptor was resolved in a complex with the valvulopathogenic drug ergotamine. As of 2009, few highly selective 5-HT2B receptor ligands have been discovered, although numerous potent non-selective compounds are known, particularly agents with concomitant 5-HT2C binding. Research in this area has been limited due to the cardiotoxicity of 5-HT2B agonists, and the lack of clear therapeutic application for 5-HT2B antagonists, but there is still a need for selective ligands for scientific research.

Agonists

Endogenous

Selective

  • 6-APB – ~100-fold selectivity over the 5-HT2A and 5-HT2C receptors, ≥32-fold selectivity over monoamine release, ~12-fold selectivity over α2C-adrenergic receptor
  • α-Methylserotonin – ~10-fold selectivity over 5-HT2A and 5-HT2C
  • BW-723C86 – 100-fold selectivity over 5-HT2A but only 3- to 10-fold selectivity over 5-HT2C, fair functional subtype selectivity, almost full agonist, anxiolytic in vivo
  • LY-266,097 – biased partial agonist in favor of Gq protein, no β-arrestin2 recruitment
  • VU6067416 – modest selectivity over 5-HT2A and 5-HT2C

Non-selective

Peripherally selective

  • AL-34662 – non-selective over 5-HT2A and 5-HT2C

Inactive

A number of notable drugs appear to be inactive or very weak as serotonin 5-HT2B receptor agonists, at least in vitro. These include the stimulants and/or entactogens dextroamphetamine, dextromethamphetamine, 4-fluoroamphetamine, 4-fluoromethamphetamine, phentermine, methylone, mephedrone, MDAI, and MMAI, among others. Findings are somewhat conflicting for certain psychedelics, such as psilocin and LSD, but most studies find that these drugs are indeed potent serotonin 5-HT2B receptor agonists.

Antagonists

Selective

  • 5-HCPC
  • 5-HPEC (weak)
  • 5-HPPC
  • AM1125
  • AM1476
  • BF-1 – derived from pimethixene
  • EGIS-7625 – high selectivity over 5-HT2A
  • EXT5 – highly selective
  • EXT9 – somewhat selective
  • LY-23,728
  • LY-266,097 – pKi = 9.7, 100-fold selectivity over 5-HT2A and 5-HT2C
  • LY-272,015 – fairly selective and highly potent
  • LY-287,375
  • MRS7925 – substantially selective over 5-HT2A and 5-HT2C but minimal selectivity over the adenosine A1 receptor
  • MRS8209
  • MW071 (MW01-8-071HAB) – non-MAOI minaprine analogue
  • PRX-08066 – Ki ≈ 1.7 nM, >100-fold selectivity
  • RQ-00310941 (RQ-941) – Ki = 2.0 nM, IC50 = 17 nM, >2,000-fold selectivity against >60 targets, under development for medical use
  • RS-127,445 (MT-500) – Ki = 0.3 nM, >1,000-fold selectivity over 5-HT2A and 5-HT2C and numerous other targets, selective over at least eight other serotonin receptors, developed for clinical use but discontinued
  • SB-204,741 – >135-fold selectivity over 5-HT2C and 5-HT2A
  • SB-215,505 – mixed 5-HT2B and 5-HT2C antagonist
  • VU6047534 – weak partial agonist or antagonist, peripherally selective in mice but not humans

Non-selective

Unknown or unsorted selectivity

Peripherally selective

  • Sarpogrelate (MCI-9042, LS-187,118) – non-selective 5-HT2 antagonist, but ~2 orders of magnitude lower affinity at 5-HT2B than at 5-HT2A
  • VU0530244 – 5-HT2B-selective
  • VU0631019 – 5-HT2B-selective
  • VU6055320 – 5-HT2B-selective

BW-501C67 and xylamidine are known peripherally selective antagonists of the serotonin 5-HT2 receptors, including of the serotonin 5-HT2A and 5-HT2B receptors, but their serotonin 5-HT2B receptor interactions do not appear to have been described.

Possible applications

5-HT2B antagonists have previously been proposed as treatment for migraine headaches, and RS-127,445 was trialled in humans up to Phase I for this indication, but development was not continued. More recent research has focused on possible application of 5-HT2B antagonists as treatments for chronic heart disease. Research claims serotonin 5-HT2B receptors have effect on liver regeneration. Antagonism of 5-HT2B may attenuate fibrogenesis and improve liver function in disease models in which fibrosis is pre-established and progressive.

See also

References

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Further reading

External links

  • "5-HT2B". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2017-02-02. Retrieved 2008-11-25.
  • Human HTR2B genome location and HTR2B gene details page in the UCSC Genome Browser.
  • Overview of all the structural information available in the PDB for UniProt: P41595 (5-hydroxytryptamine receptor 2B) at the PDBe-KB.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

Cell surface receptor: G protein-coupled receptors
Class A: Rhodopsin-like
Neurotransmitter
Adrenergic
Purinergic
Serotonin
Other
Metabolites and
signaling molecules
Eicosanoid
Other
Peptide
Neuropeptide
Other
Miscellaneous
Taste, bitter
Orphan
Other
Class B: Secretin-like
Adhesion
Orphan
Other
Class C: Metabotropic glutamate / pheromone
Taste, sweet
Other
Class F: Frizzled & Smoothened
Frizzled
Smoothened
Cell signaling / Signal transduction
Signaling pathways
Agents
Receptor ligands
Receptors
Second messenger
Assistants:
Transcription factors
By distance
Other concepts
Serotonin receptor modulators
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Categories: