5-HT2B receptor

HTR2B
Available structures
PDBOrtholog search: PDBe RCSB
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
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[3][4]
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][6] 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.[7] 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.[8] However, its most important role is in the peripheral nervous system (PNS) where it maintains the viability and efficiency of the cardiac valve leaflets.[9]

The 5-HT2B receptor subtype is involved in:

  • CNS: inhibition of serotonin and dopamine uptake, behavioral effects[10]
  • Vascular: pulmonary vasoconstriction[11]
  • Cardiac: The 5-HT2B receptor regulates cardiac structure and functions, as demonstrated by the abnormal cardiac development observed in 5-HT2B receptor null mice.[12] Excessive stimulation of this receptor causes pathological proliferation of cardiac valve fibroblasts,[13] with chronic overstimulation leading to valvulopathy.[14][15] 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.[16][17][18]
  • 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,[19] and with the abnormal acute serotonin release produced by drugs such as MDMA.[10] Surprisingly, however, 5-HT2B receptor activation appears to be protective against the development of serotonin syndrome following elevated extracellular serotonin levels,[20] despite its role in modulating serotonin release.

Clinical significance

5-HT2B receptors have been strongly implicated in causing drug-induced valvular heart disease.[21][22][23] The Fen-Phen scandal in the 80s and 90s revealed the cardiotoxic effects of 5-HT2B stimulation.[24] Today, 5-HT2B agonism is considered a toxicity signal precluding further clinical development of a compound.[25]

Ligands

The structure of the 5-HT2B receptor was resolved in a complex with the valvulopathogenic drug ergotamine.[26] 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.[27]

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[30][37]
  • α-Methylserotonin – ~10-fold selectivity over 5-HT2A and 5-HT2C[34][38][36]
  • BW-723C86 – 100-fold selectivity over 5-HT2A but only 3- to 10-fold selectivity over 5-HT2C,[34][39] fair functional subtype selectivity, almost full agonist, anxiolytic in vivo[40]
  • LY-266,097 – biased partial agonist in favor of Gq protein, no β-arrestin2 recruitment[41]
  • VU6067416 – modest selectivity over 5-HT2A and 5-HT2C[42]

Non-selective

Peripherally selective

Inactive

A number of notable drugs appear to be inactive or very weak as serotonin 5-HT2B receptor agonists, at least in vitro.[30] These include the stimulants and/or entactogens dextroamphetamine, dextromethamphetamine, 4-fluoroamphetamine, 4-fluoromethamphetamine, phentermine, methylone, mephedrone, MDAI, and MMAI, among others.[30][47][37][71][72][73] 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.[63][30][32]

Antagonists

Selective

Non-selective

Unknown or unsorted selectivity

Peripherally 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.[122][123][124]

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.[125] More recent research has focused on possible application of 5-HT2B antagonists as treatments for chronic heart disease.[126][127] Research claims serotonin 5-HT2B receptors have effect on liver regeneration.[128] 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

  • "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.