5-HT2B receptor

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)[1]
Chromosome 2 (human)
Genomic location for HTR2B
Genomic location for HTR2B
Band2q37.1Start231,108,230 bp[1]
End231,125,042 bp[1]
Gene location (Mouse)
Chromosome 1 (mouse)
Chr.Chromosome 1 (mouse)[2]
Chromosome 1 (mouse)
Genomic location for HTR2B
Genomic location for HTR2B
Band1|1 C5Start86,026,748 bp[2]
End86,039,692 bp[2]
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
  • G protein-coupled receptor activity
  • GTPase activator activity
  • signal transducer activity
  • G protein-coupled serotonin receptor activity
  • G-protein alpha-subunit binding
  • serotonin binding
  • neurotransmitter receptor activity
Cellular component
  • cytoplasm
  • integral component of membrane
  • membrane
  • plasma membrane
  • synapse
  • cell junction
  • neuron projection
  • integral component of plasma membrane
  • nucleoplasm
  • dendrite
Biological process
  • intestine smooth muscle contraction
  • smooth muscle contraction
  • G protein-coupled receptor internalization
  • release of sequestered calcium ion into cytosol
  • regulation of behavior
  • positive regulation of endothelial cell proliferation
  • positive regulation of MAP kinase activity
  • phosphorylation
  • positive regulation of cytokine production
  • vasoconstriction
  • ERK1 and ERK2 cascade
  • positive regulation of phosphatidylinositol biosynthetic process
  • cardiac muscle hypertrophy
  • heart morphogenesis
  • cellular calcium ion homeostasis
  • neural crest cell differentiation
  • negative regulation of apoptotic process
  • negative regulation of cell death
  • activation of phospholipase C activity
  • protein kinase C signaling
  • cGMP biosynthetic process
  • cellular response to temperature stimulus
  • positive regulation of GTPase activity
  • heart development
  • positive regulation of nitric-oxide synthase activity
  • protein kinase C-activating G protein-coupled receptor signaling pathway
  • embryonic morphogenesis
  • serotonin receptor signaling pathway
  • neural crest cell migration
  • positive regulation of cell population proliferation
  • positive regulation of ERK1 and ERK2 cascade
  • positive regulation of I-kappaB kinase/NF-kappaB signaling
  • phosphatidylinositol 3-kinase signaling
  • negative regulation of autophagy
  • positive regulation of cell division
  • calcium-mediated signaling
  • signal transduction
  • phospholipase C-activating G protein-coupled receptor signaling pathway
  • G protein-coupled serotonin receptor signaling pathway
  • G protein-coupled receptor signaling pathway
  • animal behaviour
  • cGMP-mediated signaling
  • G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
  • chemical synaptic transmission
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[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

Selective
  • BW-723C86[28] – fair functional subtype selectivity; almost full agonist. Anxiolytic in vivo[29]
  • Ro60-0175[28] – functionally selective over 5-HT2A, potent agonist at both 5-HT2B/C
  • VER-3323 – selective for 5-HT2B/C over 5-HT2A
  • α-Methyl-5-HT – moderately selective over 5-HT2A/C
  • 6-APB
  • LY-266,097 – biased partial agonist in favor of Gq protein, no β-arrestin2 recruitment[30]
  • VU6067416
Non-selective

Antagonists

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.[47] More recent research has focused on possible application of 5-HT2B antagonists as treatments for chronic heart disease.[48][49] Research claims serotonin 5-HT2B receptors have effect on liver regeneration.[50] 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

  • Raymond JR, Mukhin YV, Gelasco A, Turner J, Collinsworth G, Gettys TW, et al. (2002). "Multiplicity of mechanisms of serotonin receptor signal transduction". Pharmacology & Therapeutics. 92 (2–3): 179–212. doi:10.1016/S0163-7258(01)00169-3. PMID 11916537.
  • Choi DS, Birraux G, Launay JM, Maroteaux L (Oct 1994). "The human serotonin 5-HT2B receptor: pharmacological link between 5-HT2 and 5-HT1D receptors". FEBS Letters. 352 (3): 393–9. doi:10.1016/0014-5793(94)00968-6. PMID 7926008. S2CID 26931598.
  • Kursar JD, Nelson DL, Wainscott DB, Baez M (Aug 1994). "Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor". Molecular Pharmacology. 46 (2): 227–34. PMID 8078486.
  • Schmuck K, Ullmer C, Engels P, Lübbert H (Mar 1994). "Cloning and functional characterization of the human 5-HT2B serotonin receptor". FEBS Letters. 342 (1): 85–90. doi:10.1016/0014-5793(94)80590-3. PMID 8143856. S2CID 11232259.
  • Launay JM, Birraux G, Bondoux D, Callebert J, Choi DS, Loric S, et al. (Feb 1996). "Ras involvement in signal transduction by the serotonin 5-HT2B receptor". The Journal of Biological Chemistry. 271 (6): 3141–7. doi:10.1074/jbc.271.6.3141. PMID 8621713.
  • Le Coniat M, Choi DS, Maroteaux L, Launay JM, Berger R (Feb 1996). "The 5-HT2B receptor gene maps to 2q36.3-2q37.1" (PDF). Genomics. 32 (1): 172–3. doi:10.1006/geno.1996.0101. PMID 8786115.
  • Kim SJ, Veenstra-VanderWeele J, Hanna GL, Gonen D, Leventhal BL, Cook EH (Feb 2000). "Mutation screening of human 5-HT(2B)receptor gene in early-onset obsessive-compulsive disorder". Molecular and Cellular Probes. 14 (1): 47–52. doi:10.1006/mcpr.1999.0281. PMID 10722792.
  • Manivet P, Mouillet-Richard S, Callebert J, Nebigil CG, Maroteaux L, Hosoda S, et al. (Mar 2000). "PDZ-dependent activation of nitric-oxide synthases by the serotonin 2B receptor". The Journal of Biological Chemistry. 275 (13): 9324–31. doi:10.1074/jbc.275.13.9324. PMID 10734074.
  • Becamel C, Figge A, Poliak S, Dumuis A, Peles E, Bockaert J, et al. (Apr 2001). "Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1". The Journal of Biological Chemistry. 276 (16): 12974–82. doi:10.1074/jbc.M008089200. PMID 11150294.
  • Manivet P, Schneider B, Smith JC, Choi DS, Maroteaux L, Kellermann O, et al. (May 2002). "The serotonin binding site of human and murine 5-HT2B receptors: molecular modeling and site-directed mutagenesis". The Journal of Biological Chemistry. 277 (19): 17170–8. doi:10.1074/jbc.M200195200. PMID 11859080.
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  • Matsuda A, Suzuki Y, Honda G, Muramatsu S, Matsuzaki O, Nagano Y, et al. (May 2003). "Large-scale identification and characterization of human genes that activate NF-kappaB and MAPK signaling pathways". Oncogene. 22 (21): 3307–18. doi:10.1038/sj.onc.1206406. PMID 12761501. S2CID 38880905.
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  • "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.

  • v
  • t
  • e
Neurotransmitter
Adrenergic
Purinergic
Serotonin
Other
Metabolites and
signaling molecules
Eicosanoid
Other
Peptide
Neuropeptide
Other
Miscellaneous
Taste, bitter
Orphan
Other
Adhesion
Orphan
Other
Taste, sweet
Other
Class F: Frizzled & Smoothened
Frizzled
Smoothened
  • v
  • t
  • e
Signaling pathways
Agents
Receptor ligands
Receptors
Second messenger
Assistants:
Transcription factors
By distance
Other concepts
  • v
  • t
  • e
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
  • See also: Receptor/signaling modulators
  • Adrenergics
  • Dopaminergics
  • Melatonergics
  • Monoamine reuptake inhibitors and releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins