5-hydroxytryptamine receptor 2B
Also known as: HTR2B
Function
G protein-coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. HTR2B is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Plays a role in the regulation of dopamine and 5-hydroxytryptamine release, 5-hydroxytryptamine uptake and in the regulation of extracellular dopamine and 5-hydroxytryptamine levels, and thereby affects neural activity. May play a role in the perception of pain (By similarity). Plays a role in the regulation of behavior, including impulsive behavior. Required for normal proliferation of embryonic cardiac myocytes and normal heart development (By similarity). Protects cardiomyocytes against apoptosis (By similarity). Plays a role in the adaptation of pulmonary arteries to chronic hypoxia (By similarity). Plays a role in vasoconstriction (By similarity). Required for normal osteoblast function and proliferation, and for maintaining normal bone density (By similarity). Required for normal proliferation of the interstitial cells of Cajal in the intestine (By similarity).
Classification
- Family (Pfam)
- PF00001 7tm_1
- InterPro
- 5HT2B_rcpt, 5HT_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
- Functional cluster
- Protein Serine/Threonine Kinases
Experimental structures · PDB · 12
- 4IB4 X-ray 2.70A
- 4NC3 X-ray 2.80A
- 5TUD X-ray 3.00A
- 5TVN X-ray 2.90A
- 6DRX X-ray 3.10A
- 6DRY X-ray 2.92A
- 6DRZ X-ray 3.10A
- 6DS0 X-ray 3.19A
- 7SRQ EM 2.70A
- 7SRR EM 2.90A
- 7SRS EM 3.30A
- 9JGK EM 3.60A
A predicted model is available from AlphaFold.
Gene Ontology · 40
- GO:0005737 cytoplasm
- GO:0030425 dendrite
- GO:0098666 G protein-coupled serotonin receptor complex
- GO:0005654 nucleoplasm
- GO:0005886 plasma membrane
- GO:0045202 synapse
- GO:0004993 G protein-coupled serotonin receptor activity
- GO:0001965 G-protein alpha-subunit binding
- GO:0001587 Gq/11-coupled serotonin receptor activity
- GO:0005096 GTPase activator activity
- GO:0030594 neurotransmitter receptor activity
- GO:0051378 serotonin binding
- GO:0099589 serotonin receptor activity
- GO:0019722 calcium-mediated signaling
- GO:0003300 cardiac muscle hypertrophy
- GO:0007268 chemical synaptic transmission
- GO:0048598 embryonic morphogenesis
- GO:0070371 ERK1 and ERK2 cascade
- GO:0007186 G protein-coupled receptor signaling pathway
- GO:0007187 G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
- GO:0098664 G protein-coupled serotonin receptor signaling pathway
- GO:0003007 heart morphogenesis
- GO:0014827 intestine smooth muscle contraction
- GO:0006874 intracellular calcium ion homeostasis
- GO:0043066 negative regulation of apoptotic process
- GO:0014033 neural crest cell differentiation
- GO:0001755 neural crest cell migration
- GO:0007208 phospholipase C-activating serotonin receptor signaling pathway
- GO:0043123 positive regulation of canonical NF-kappaB signal transduction
- GO:0051781 positive regulation of cell division
- GO:0008284 positive regulation of cell population proliferation
- GO:0001819 positive regulation of cytokine production
- GO:0001938 positive regulation of endothelial cell proliferation
- GO:0070374 positive regulation of ERK1 and ERK2 cascade
- GO:0010513 positive regulation of phosphatidylinositol biosynthetic process
- GO:0050795 regulation of behavior
- GO:0051209 release of sequestered calcium ion into cytosol
- GO:0009410 response to xenobiotic stimulus
- GO:0007210 serotonin receptor signaling pathway
- GO:0042310 vasoconstriction
Drugs targeting this protein · 10
- METHYLERGONOVINE MALEATE partial agonist
- METHYSERGIDE MALEATE antagonist
- MINAPRINE HYDROCHLORIDE antagonist
- DEXFENFLURAMINE HYDROCHLORIDE agonist
- VABICASERIN HYDROCHLORIDE antagonist
- ZIMELDINE HYDROCHLORIDE antagonist
- AMISULPRIDE antagonist
- MINAPRINE antagonist
- CLOTHIAPINE antagonist
- PRX-08066 antagonist
Related proteins · sequence + function similarity
- 5-hydroxytryptamine receptor 2B 0.97
- 5-hydroxytryptamine receptor 2B 0.97
- 5-hydroxytryptamine receptor 2B 0.94
- 5-hydroxytryptamine receptor 2A 0.92
- 5-hydroxytryptamine receptor 2A 0.91
- 5-hydroxytryptamine receptor 2A 0.91
- 5-hydroxytryptamine receptor 2A 0.91
- 5-hydroxytryptamine receptor 2A 0.91
- 5-hydroxytryptamine receptor 2A 0.90
- 5-hydroxytryptamine receptor 2A 0.90
- 5-hydroxytryptamine receptor 2A 0.90
- 5-hydroxytryptamine receptor 2A 0.90
Co-cited proteins · studied together in the literature
- 5-hydroxytryptamine receptor 1B 4 shared papers
- 5-hydroxytryptamine receptor 2C 4 shared papers
- 5-hydroxytryptamine receptor 2A 5 shared papers
- 5-hydroxytryptamine receptor 1D 2 shared papers
- 5-hydroxytryptamine receptor 1F 2 shared papers
- 5-hydroxytryptamine receptor 1E 2 shared papers
- 5-hydroxytryptamine receptor 1A 2 shared papers
- Multiple PDZ domain protein 1 shared papers
- Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 1 shared papers
- Multiple PDZ domain protein 1 shared papers
- D(1A) dopamine receptor 1 shared papers
- 5-hydroxytryptamine receptor 2B 1 shared papers
Literature · 20 cited papers
- Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD. Neuron · 2022
- Structural determinants of 5-HT2B receptor activation and biased agonism. Nat. Struct. Mol. Biol. · 2018
- Crystal structure of an LSD-bound human serotonin receptor. Cell · 2017
- Serial femtosecond crystallography of G protein-coupled receptors. Science · 2013
- Structural features for functional selectivity at serotonin receptors. Science · 2013
- Structural basis for molecular recognition at serotonin receptors. Science · 2013
- A population-specific HTR2B stop codon predisposes to severe impulsivity. Nature · 2010
- Serotonin receptors - from molecular biology to clinical applications. Physiol. Res. · 2011
- Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells. Eur. J. Pharmacol. · 2008
- Serotonin receptors. Chem. Rev. · 2008
- Generation and annotation of the DNA sequences of human chromosomes 2 and 4. Nature · 2005
- The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
- … and 8 more in the literature graph