5-HT_2B receptor

5-Hydroxytryptamine receptor 2B (5-HT_2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the HTR2B gene.[5][6] 5-HT_2B is a member of the 5-HT₂ receptor family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT).

HTR2B
Available structures PDB Ortholog search: PDBe RCSB List of PDB id codes 4NC3, 4IB4
Identifiers
Aliases	HTR2B, 5-HT(2B), 5-HT2B, 5-HT-2B, 5-hydroxytryptamine receptor 2B
External IDs	OMIM: 601122 MGI: 109323 HomoloGene: 55492 GeneCards: HTR2B
Gene location (Human) Chr. Chromosome 2 (human)[1] Band 2q37.1 Start 231,108,230 bp[1] End 231,125,042 bp[1]
Gene location (Mouse) Chr. Chromosome 1 (mouse)[2] Band 1|1 C5 Start 86,099,026 bp[2] End 86,111,970 bp[2]
RNA expression pattern More reference expression data
Gene ontology Molecular function • G-protein coupled receptor activity • GO:0005097, GO:0005099, GO:0005100 GTPase activator activity • signal transducer activity • G-protein coupled serotonin receptor activity • drug binding • G-protein alpha-subunit binding • serotonin binding • neurotransmitter receptor activity Cellular component • cytoplasm • integral component of membrane • membrane • cell 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 cytokine secretion • 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 • GO:0032320, GO:0032321, GO:0032855, GO:0043089, GO:0032854 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 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 • response to drug • 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 behavior • cGMP-mediated signaling • G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger • chemical synaptic transmission Sources:Amigo / QuickGO
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

Tissue distribution and function

The 5-HT₂ receptors (of which the 5-HT_2B 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-HT_2B receptor is highly expressed in the liver and kidney, with lower levels of expression being seen in the cerebral cortex, whole brain, pancreas, and spleen.[7]

The 5-HT_2B receptor subtype is involved in:

• CNS: presynaptic inhibition, behavioural effects[8]
• Vascular: pulmonary vasoconstriction[9]
• Cardiac: The 5-HT_2B receptor regulates cardiac structure and functions as demonstrated by the abnormal cardiac development observed in 5-HT_2B receptor null mice.[10] The 5-HT_2B receptor stimulation can also lead to pathological proliferation of cardiac valve fibroblasts,[11] which with chronic overstimulation of 5-HT_2B can lead to a severe valvulopathy. Moreover, 5-HT_2B receptors were recently shown to be overexpressed in human failing heart and antagonists of 5-HT_2B receptors were uncovered to prevent both angiotensin II or beta-adrenergic agonist-induced pathological cardiac hypertrophy in mouse.[12][13][14]
• Serotonin transporter: 5-HT_2B receptors regulate serotonin release via the serotonin transporter, and are important both to normal physiological regulation of serotonin levels in blood plasma,[15] and with the abnormal acute serotonin release produced by drugs such as MDMA.[8] Surprisingly however 5-HT_2B receptor activation appears to be protective against the development of serotonin syndrome following elevated extracellular serotonin levels,[16] despite its role in modulating serotonin release.

Clinical significance

5-HT_2B receptors have also been strongly implicated in drug-induced valvular heart disease.[17][18][19] In this context, it is generally considered to be an antitarget.

The structure of the 5-HT_2B receptor was resolved in a complex with the valvulopathogenic drug ergotamine.[20]

Ligands

As of 2009, few highly selective 5-HT_2B receptor ligands have been discovered, although numerous potent non-selective compounds are known, particularly agents with concomitant 5-HT_2C binding. Research in this area has been limited due to the cardiotoxicity of 5-HT_2B agonists, and the lack of clear therapeutic application for 5-HT_2B antagonists, but there is still a need for selective ligands for scientific research.[21]

Agonists

Selective

• BW-723C86:[22] fair functional subtype selectivity; almost full agonist. Anxiolytic in vivo.[23]
• Ro60-0175 [22] functionally selective over 5-HT_2A, potent agonist at both 5-HT_2B/C
• VER-3323: selective for 5-HT_2B/C over 5-HT_2A
• α-Methyl-5-HT - moderately selective over 5-HT_2A/C
• 6-APB
• LY-266,097 - biased partial agonist in favor of G_q protein, no β-arrestin2 recruitment[24]

Non-selective

• Guanfacine - an α_2A agonist, but has 5-HT_2B agonistic activity at therapeutic concentrations.[25]
• MDMA[26]
• MDA[26]
• MEM[27]
• Pergolide[28]
• Cabergoline
• Norfenfluramine[22]
• Chlorphentermine
• Aminorex
• Bromo-dragonfly
• DMT
• 5-MeO-DMT
• LSD - About equal affinity for human cloned 5-HT_2B and 5-HT_2A receptors.[29]
• psilocin [29]
• Xylometazoline
• Oxymetazoline
• Quinidine
• Ropinirole
• Fenoldopam
• Lorcaserin
• Methylergonovine
• Ergotamine
• Ergonovine

Antagonists

• Agomelatine - primarily a melatonin Mt1/Mt2 receptor agonist, with a less potent antagonism of 5-HT_2B and 5-HT_2C.[30]
• Amisulpride
• Aripiprazole
• Cariprazine[31]
• Clozapine
• mCPP (in humans)
• Sarpogrelate: a mixed 5-HT_2A/B antagonist
• Lisuride: a dopamine agonist of the ergoline class, that is also a 5-HT_2B antagonist[32] and a dual 5-HT_2A/C agonist[33]
• Tegaserod: primarily a 5-HT₄ agonist, but also a 5-HT_2B antagonist[34]
• RS-127,445:[35] high affinity; subtype selective (1000x), selective over at least eight other 5-HTR types; orally bioavailable.
• Metadoxine: a 5ht_2b antagonist and GABA-activity modulator [36]
• SDZ SER-082: a mixed 5-HT_2B/C antagonist
• Promethazine [37]
• EGIS-7625: high selectivity over 5-HT_2A[38]
• PRX-08066
• SB-200,646
• SB-204,741
• SB-206,553: mixed 5-HT_2B/C antagonist and PAM at α₇ nAChR[39]
• SB-215,505 [40]
• SB-228,357
• LY-272,015

Possible applications

5-HT_2B 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.[41] More recent research has focused on possible application of 5-HT_2B antagonists as treatments for chronic heart disease.[42][43] Research claims serotonin 5-HT2B receptors have effect on liver regeneration.[44]

See also

• 5-HT receptor

References

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Further reading

• Raymond JR, Mukhin YV, Gelasco A, Turner J, Collinsworth G, Gettys TW, Grewal JS, Garnovskaya MN (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.
• 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

• "5-HT_2B". 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.
• 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.