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5-HT2B receptor









5-HT2B receptor


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HTR2B
4IB4.png







Available structures
PDB Ortholog search: PDBe RCSB



Identifiers
Aliases
HTR2B, 5-HT(2B), 5-HT2B, 5-HT-2B, 5-hydroxytryptamine receptor 2B
External IDs MGI: 109323 HomoloGene: 55492 GeneCards: HTR2B


















Gene location (Human)
Chromosome 2 (human)
Chr. Chromosome 2 (human)[1]

Chromosome 2 (human)
Genomic location for HTR2B

Genomic location for HTR2B

Band 2q37.1 Start 231,108,230 bp[1]
End 231,125,118 bp[1]























RNA expression pattern
PBB GE HTR2B 206638 at fs.png
More reference expression data















Orthologs
Species Human Mouse
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 Mb Chr 1: 86.1 – 86.11 Mb

PubMed search		 [3] [4]
Wikidata



View/Edit Human View/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).




Contents






  • 1 Function


  • 2 Clinical significance


  • 3 Ligands


    • 3.1 Agonists


    • 3.2 Antagonists




  • 4 Possible applications


  • 5 See also


  • 6 References


  • 7 Further reading


  • 8 External links





Function[edit]


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 effects include neuronal sensitization to tactile stimuli and mediation of some of the effects of hallucinogenic substituted amphetamines.


The 5-HT2B receptor subtype is involved in:



  • CNS: presynaptic inhibition, behavioural effects[7]

  • Vascular: pulmonary vasoconstriction[8]

  • Cardiac: The 5-HT2B receptor regulates cardiac structure and functions as demonstrated by the abnormal cardiac development observed in 5-HT2B receptor null mice.[9] The 5-HT2B receptor stimulation can also lead to pathological proliferation of cardiac valves fibroblasts,[10] which with chronic overstimulation of 5-HT2B can lead to a severe valvulopathy. Moreover, 5-HT2B receptors were recently shown to be overexpressed in human failing heart and antagonists of 5-HT2B receptors were uncovered to prevent both angiotensin II or beta-adrenergic agonist-induced pathological cardiac hypertrophy in mouse.[11][12][13]


  • 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,[14] and with the abnormal acute serotonin release produced by drugs such as MDMA.[7] Surprisingly however 5-HT2B receptor activation appears to be protective against the development of serotonin syndrome following elevated extracellular serotonin levels,[15] despite its role in modulating serotonin release.



Clinical significance[edit]


5-HT2B receptors have also been strongly implicated in drug-induced valvular heart disease.[16][17][18] In this context, it is generally considered to be an antitarget.


The structure of the 5-HT2B receptor was recently solved in complex with the valvulopathogenic drug ergotamine.[19]



Ligands[edit]


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.[20]



Agonists[edit]


Selective



  • BW-723C86:[21] fair functional subtype selectivity; almost full agonist. Anxiolytic in vivo.[22]


  • Ro60-0175 [21] 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[23]


Non-selective



  • Guanfacine - an α2A agonist, but has 5-HT2B agonistic activity at therapeutic concentrations.[24]


  • MDMA (Ecstasy)[25]


  • MDA[25]


  • MEM[26]


  • Pergolide[27]

  • Cabergoline


  • Norfenfluramine[21]

  • Chlorphentermine

  • Aminorex

  • mCPP

  • Bromo-dragonfly

  • DMT

  • 5-MeO-DMT


  • LSD-25 - About equal affinity for human cloned 5-HT2B and 5-HT2A receptors.[28]


  • psilocin [28]



Antagonists[edit]




  • Agomelatine - primarily a melatonin Mt1/Mt2 receptor agonist, with a less potent antagonism of 5-HT2B and 5-HT2C.[29]

  • Amisulpride

  • Aripiprazole


  • Cariprazine[30]


  • Sarpogrelate: a mixed 5-HT2A/B antagonist


  • Lisuride: a dopamine agonist of the ergoline class, that is also a 5-HT2B antagonist[31] and a dual 5-HT2A/C agonist[32]


  • Tegaserod: primarily a 5-HT4 agonist, but also a 5-HT2B antagonist[33]


  • RS-127,445:[34] high affinity; subtype selective (1000x), selective over at least eight other 5-HTR types; orally bioavailable.


  • Metadoxine: a 5ht2b antagonist and GABA-activity modulator [35]


  • SDZ SER-082: a mixed 5-HT2B/C antagonist


  • EGIS-7625: high selectivity over 5-HT2A[36]

  • PRX-08066

  • SB-200,646

  • SB-204,741


  • SB-206,553: mixed 5-HT2B/C antagonist and PAM at α7 nAChR[37]


  • SB-215,505 [38]

  • SB-228,357

  • LY-272,015



Possible applications[edit]


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.[39] More recent research has focused on possible application of 5-HT2B antagonists as treatments for chronic heart disease.[40][41] Research claims serotonin 5-HT2B receptors have effect on liver regeneration.[42]



See also[edit]


  • 5-HT receptor


References[edit]





  1. ^ abc GRCh38: Ensembl release 89: ENSG00000135914 - Ensembl, May 2017


  2. ^ abc GRCm38: Ensembl release 89: ENSMUSG00000026228 - Ensembl, May 2017


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Further reading[edit]


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  • Bonhaus DW, Bach C, DeSouza A, Salazar FH, Matsuoka BD, Zuppan P, Chan HW, Eglen RM (Jun 1995). "The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors". British Journal of Pharmacology. 115 (4): 622–8. doi:10.1111/j.1476-5381.1995.tb14977.x. PMC 1908489. PMID 7582481.


  • 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.


  • 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.


  • Launay JM, Birraux G, Bondoux D, Callebert J, Choi DS, Loric S, Maroteaux L (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". 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, Kellermann O, Launay JM (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, Lubbert H, Ullmer C (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, Launay JM (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.


  • Borman RA, Tilford NS, Harmer DW, Day N, Ellis ES, Sheldrick RL, Carey J, Coleman RA, Baxter GS (Mar 2002). "5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro". British Journal of Pharmacology. 135 (5): 1144–51. doi:10.1038/sj.bjp.0704571. PMC 1573235. PMID 11877320.


  • Matsuda A, Suzuki Y, Honda G, Muramatsu S, Matsuzaki O, Nagano Y, Doi T, Shimotohno K, Harada T, Nishida E, Hayashi H, Sugano S (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.


  • Slominski A, Pisarchik A, Zbytek B, Tobin DJ, Kauser S, Wortsman J (Jul 2003). "Functional activity of serotoninergic and melatoninergic systems expressed in the skin". Journal of Cellular Physiology. 196 (1): 144–53. doi:10.1002/jcp.10287. PMID 12767050.


  • Lin Z, Walther D, Yu XY, Drgon T, Uhl GR (Dec 2004). "The human serotonin receptor 2B: coding region polymorphisms and association with vulnerability to illegal drug abuse". Pharmacogenetics. 14 (12): 805–11. doi:10.1097/00008571-200412000-00003. PMID 15608559.




External links[edit]




  • "5-HT2B". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

  • Human HTR2B genome location and HTR2B gene details page in the UCSC Genome Browser.


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















Retrieved from "https://en.wikipedia.org/w/index.php?title=5-HT2B_receptor&oldid=875597086"





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