DGIdb - HTR2B Gene Record

HTR2B 3357 Druggable GenomeDrug Resistance

Alternate Names:

3357
5-HYDROXYTRYPTAMINE RECEPTOR 2B
HTR2B
5-HT(2B)
5-HT-2B
5-HT2B
601122
5294
ENSG00000135914
OTTHUMG00000133222
BE0000393
P41595
5HT2B_HUMAN
Serotonin receptor 2B
5-HYDROXYTRYPTAMINE 2B RECEPTOR (5-HT-2B) (SEROTONIN RECEPTOR 2B). [SOURCE:UNIPROT/SWISSPROT;ACC:P41595]
7
5-HT<sub>2B</sub> receptor
5-HT 2B receptor
T31204
NM_000867
NP_000858

Gene Info:

Human Readable Name	G PROTEIN COUPLED RECEPTOR
Target Class	Receptors
Target Subclass	GPCR
Target Subclass	Rhodopsin
Human Readable Name	DRUGGABLE GENOME
Uniprot Status	Swiss-Prot
Uniprot Evidence	1: Evidence at protein level
Interpro Acc	IPR000276
Interpro Type	Family
Interpro Name	GPCR, rhodopsin-like, 7TM
Interpro Short Name	7TM_GPCR_Rhodpsn
Transmembrane Helix Count	7
Target Main Class	Receptors
Gene Biotype	PROTEIN_CODING
GuideToPharmacology Gene Category Name	5-Hydroxytryptamine receptors
GuideToPharmacology Gene Category ID	1

(10 More Sources)

Gene Categories: Category Details

KINASE
DRUG RESISTANCE
G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Muramatsu et al., 1988, 5-HT2 antagonists and minaprine block the 5-HT-induced inhibition of dopamine release from rat brain striatal slices., Eur. J. Pharmacol.
Kodama et al., 1992, Protective effect of minaprine against the abnormal changes of 2-deoxyglucose uptake by rat hippocampal slices induced by hypoxia/hypoglycemia., Jpn. J. Pharmacol.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Rothman et al., 2000, Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications., Circulation
Shahid et al., 2009, Asenapine: a novel psychopharmacologic agent with a unique human receptor signature., J. Psychopharmacol. (Oxford)
Citrome, 2011, Role of sublingual asenapine in treatment of schizophrenia., Neuropsychiatr Dis Treat
Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem
Sharif et al., 2009, Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes., Exp. Eye Res.
Sharif, 2010, Serotonin-2 receptor agonists as novel ocular hypotensive agents and their cellular and molecular mechanisms of action., Curr Drug Targets
Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy
Huang et al., 2009, Parallel functional activity profiling reveals valvulopathogens are potent 5-hydroxytryptamine(2B) receptor agonists: implications for drug safety assessment., Mol. Pharmacol.
Lyon et al., 1986, 3,4-Methylenedioxymethamphetamine (MDMA): stereoselective interactions at brain 5-HT1 and 5-HT2 receptors., Psychopharmacology (Berl.)
Setola et al., 2003, 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro., Mol. Pharmacol.
Fitzgerald et al., 2000, Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine., Mol. Pharmacol.
Blanpain et al., 2003, Serotonin 5-HT(2B) receptor loss of function mutation in a patient with fenfluramine-associated primary pulmonary hypertension., Cardiovasc. Res.
Kaumann et al., 2006, 5-hydroxytryptamine receptors in the human cardiovascular system., Pharmacol. Ther.
Roth, 2007, Drugs and valvular heart disease., N. Engl. J. Med.
Cussac et al., 2008, 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.
Hutcheson JD et al., 2011, Serotonin receptors and heart valve disease--it was meant 2B., Pharmacol Ther
Görnemann T et al., 2008, Characterization of the molecular fragment that is responsible for agonism of pergolide at serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A receptors., J Pharmacol Exp Ther
McCullough et al., 2006, The 5-HT2B antagonist and 5-HT4 agonist activities of tegaserod in the anaesthetized rat., Pharmacol. Res.
Beattie et al., 2004, The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo., Br. J. Pharmacol.
Greenwood-Van Meerveld et al., 2006, 5-HT2B receptors do not modulate sensitivity to colonic distension in rats with acute colorectal hypersensitivity., Neurogastroenterol. Motil.
Cooper et al., 1979, Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat., Br. J. Pharmacol.
LeWitt PA, 2004, Subcutaneously administered apomorphine: pharmacokinetics and metabolism., Neurology
Schmuck et al., 1996, Activation of meningeal 5-HT2B receptors: an early step in the generation of migraine headache?, Eur. J. Neurosci.
Maj et al., 1977, Doxepin as a blocker of central serotonin receptors., Pharmakopsychiatr Neuropsychopharmakol
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
Sargent et al., 1998, Clomipramine enhances the cortisol response to 5-HTP: implications for the therapeutic role of 5-HT2 receptors., Psychopharmacology (Berl.)
Contreras et al., Cortical and septal responses to dorsal raphe nucleus stimulation in the rat: long-term clomipramine actions., Bol Estud Med Biol
Sugimoto et al., 2003, The tricyclic antidepressant clomipramine increases plasma glucose levels of mice., J. Pharmacol. Sci.
Bonhaus et al., RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist., Neuropharmacology
Baxter et al., 1994, Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle., Br. J. Pharmacol.
Schaerlinger et al., 2003, Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy., Br. J. Pharmacol.
Porvasnik SL et al., 2010, PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats., J Pharmacol Exp Ther
Semple G et al., 2009, Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation., Bioorg Med Chem Lett
McCormack, 2015, Cariprazine: First Global Approval., Drugs
Glusa et al., 2000, Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors., Br. J. Pharmacol.
Mestres J et al., 2011, Linking pharmacology to clinical reports: cyclobenzaprine and its possible association with serotonin syndrome., Clin Pharmacol Ther
Przegaliński E et al., 1979, The central action of pizotifen., Psychopharmacology (Berl)
Mylecharane EJ, 1991, 5-HT2 receptor antagonists and migraine therapy., J Neurol
Rubio-Beltrán E et al., 2018, Is selective 5-HT<sub>1F</sub> receptor agonism an entity apart from that of the triptans in antimigraine therapy?, Pharmacol Ther
de Bartolomeis A et al., 2015, Update on the Mechanism of Action of Aripiprazole: Translational Insights into Antipsychotic Strategies Beyond Dopamine Receptor Antagonism., CNS Drugs
Peng L et al., 2014, Fluoxetine and all other SSRIs are 5-HT2B Agonists - Importance for their Therapeutic Effects., Curr Neuropharmacol
Zhang S et al., 2010, 5-HT2B receptors are expressed on astrocytes from brain and in culture and are a chronic target for all five conventional 'serotonin-specific reuptake inhibitors'., Neuron Glia Biol
Hertz L et al., 2015, Chronic SSRI stimulation of astrocytic 5-HT2B receptors change multiple gene expressions/editings and metabolism of glutamate, glucose and glycogen: a potential paradigm shift., Front Behav Neurosci

PRX-08066 HTR2B

Interaction Score: 2.81

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name PRX-08066

Novel drug target Established target

PMIDs:
20430844

Sources:
TdgClinicalTrial TTD DrugBank
CHEMBL182150 HTR2B

Interaction Score: 1.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19773162

Sources:
DTC
FENFLURAMINE HTR2B

Interaction Score: 0.82

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
12761331 10617681 14659797 16960982 17202450 11104741

Sources:
DrugBank
TRIFLUPROMAZINE HTR2B

Interaction Score: 0.7

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11752352 17139284 497523 17016423

Sources:
TEND TdgClinicalTrial TTD DrugBank
TEGASEROD HTR2B

Interaction Score: 0.7

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
16495076 15466450 16629860

Sources:
DrugBank GuideToPharmacology
MINAPRINE HTR2B

Interaction Score: 0.7

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752352 17139284 2975224 1361012 17016423

Sources:
TEND TdgClinicalTrial TTD DrugBank
LYSERGIDE HTR2B

Interaction Score: 0.42

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Biased agonist

PMIDs:
14659797

Sources:
DrugBank GuideToPharmacology
NORFLUOXETINE HTR2B

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PIBOSEROD HTR2B

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
VABICASERIN HTR2B

Interaction Score: 0.35

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
MIDOMAFETAMINE HTR2B

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
2871581

Sources:
TTD DrugBank
PERGOLIDE HTR2B

Interaction Score: 0.27

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
18703043 18691132 10641988 21440001 18096760

Sources:
DrugBank GuideToPharmacology
CABERGOLINE HTR2B

Interaction Score: 0.25

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
18691132 18992242 20426763 10641988 19570945

Sources:
DrugBank GuideToPharmacology
BROLAMFETAMINE HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
RS-102,221 HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
AGOMELATINE HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name agomelatine, AGO178C, S-20098,Valdoxan, Thymanax

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology
RELENOPRIDE HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
METHYLERGONOVINE MALEATE HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2b (5-HT2b) receptor partial agonist

PMIDs:
None found

Sources:
ChemblInteractions
VOLINANSERIN HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
GLEMANSERIN HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
LORCASERIN HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
VABICASERIN HYDROCHLORIDE HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2b (5-HT2b) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL473186 HTR2B

Interaction Score: 0.23

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
CHLORPROTHIXENE HTR2B

Interaction Score: 0.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17139284 17016423

Sources:
TEND TdgClinicalTrial
DIHYDROERGOTAMINE HTR2B

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
12970106 11752352

Sources:
DrugBank
CARIPRAZINE HTR2B

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
26510944

Sources:
DrugBank
METHYLERGONOVINE HTR2B

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
11104741

Sources:
DrugBank GuideToPharmacology
BALOVAPTAN HTR2B

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Direct Interaction? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
DIHYDROERGOCRYPTINE HTR2B

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Details of the Assay for Interaction Biased for β-arrestin signalling.

Specific Action of the Ligand Biased agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
QUIPAZINE HTR2B

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
SARPOGRELATE HTR2B

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
CLOMIPRAMINE HTR2B

Interaction Score: 0.17

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
9862411 1296670 14501155

Sources:
DrugBank
ZOLMITRIPTAN HTR2B

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
29352859

Sources:
DrugBank
YOHIMBINE HTR2B

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
9225287 8032658

Sources:
DrugBank GuideToPharmacology
RENZAPRIDE HTR2B

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name renzapride

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
MESULERGINE HTR2B

Interaction Score: 0.14

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PIZOTYLINE HTR2B

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
111296 2045831

Sources:
DrugBank
ASENAPINE HTR2B

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Asenapine

PMIDs:
18308814 21655346

Sources:
TdgClinicalTrial DrugBank
METHYSERGIDE HTR2B

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
8743744

Sources:
DrugBank GuideToPharmacology
LISURIDE HTR2B

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
18691132

Sources:
DrugBank GuideToPharmacology
ERGOTAMINE HTR2B

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
11104741

Sources:
DrugBank GuideToPharmacology
SPIRAMIDE HTR2B

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
DOXEPIN HTR2B

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
309138 7855217

Sources:
TdgClinicalTrial DrugBank
APOMORPHINE HTR2B

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
15037665 18691132

Sources:
DrugBank GuideToPharmacology
CHEMBL309760 HTR2B

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BROMOCRIPTINE HTR2B

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
18703043 18691132 10641988

Sources:
DrugBank GuideToPharmacology
CYCLOBENZAPRINE HTR2B

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
21975349

Sources:
DrugBank
TERGURIDE HTR2B

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name terguride

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology
MK-212 HTR2B

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
RAUWOLSCINE HTR2B

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
PINDOLOL HTR2B

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
PAROXETINE HTR2B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
25342944 20846463 25750618

Sources:
DrugBank
BRL-15,572 HTR2B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CAPESEROD HTR2B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
QUINPIROLE HTR2B

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
SPIROXATRINE HTR2B

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
LEVOMEPROMAZINE HTR2B

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TEND TdgClinicalTrial
8-OH-DPAT HTR2B

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CHEMBL609728 HTR2B

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
PIPAMPERONE HTR2B

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
TRYPTAMINE HTR2B

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
PIRIBEDIL HTR2B

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
MIANSERIN HTR2B

Interaction Score: 0.05

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology
TRAZODONE HTR2B

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ROXINDOLE HTR2B

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
AMOXAPINE HTR2B

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
10821800

Sources:
DrugBank
OCAPERIDONE HTR2B

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
XANOMELINE HTR2B

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SUMATRIPTAN HTR2B

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
SPIPERONE HTR2B

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
METERGOLINE HTR2B

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
KETANSERIN HTR2B

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
METITEPINE HTR2B

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
RITANSERIN HTR2B

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
QUETIAPINE HTR2B

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Seroquel

PMIDs:
None found

Sources:
TEND TdgClinicalTrial
SEROTONIN HTR2B

Interaction Score: 0.03

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? True

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
ARIPIPRAZOLE HTR2B

Interaction Score: 0.03

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

PMIDs:
26346901

Sources:
DrugBank
MELATONIN HTR2B

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
FLUOXETINE HTR2B

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
HALOPERIDOL HTR2B

Interaction Score: 0.01

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CLOZAPINE HTR2B

Interaction Score: 0.01

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Ensembl: ENSG00000135914
- Version: 101_38
Alternate Names:

HTR2B Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P41595
- Version: 01-August-2011
Alternate Names:

P41595 Uniprot Accession

HTR2B Gene Symbol

3357 Entrez Gene Id

Gene Info:

Target Subclass Rhodopsin

Transmembrane Helix Count 7

Target Subclass GPCR

Publications:
HopkinsGroom: P41595
- Version: 11-September-2012
Alternate Names:

5-HYDROXYTRYPTAMINE RECEPTOR 2B Uniprot Protein Name

P41595 Uniprot Accession

5HT2B_HUMAN Uniprot Id

Gene Info:

Human Readable Name G PROTEIN COUPLED RECEPTOR

Human Readable Name DRUGGABLE GENOME

Uniprot Status Swiss-Prot

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
RussLampel: ENSG00000135914
- Version: 26-July-2011
Alternate Names:

ENSG00000135914 Ensembl Gene Id

HTR2B Display Id

5-HYDROXYTRYPTAMINE 2B RECEPTOR (5-HT-2B) (SEROTONIN RECEPTOR 2B). [SOURCE:UNIPROT/SWISSPROT;ACC:P41595] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P41595
- Version: January-2014
Alternate Names:

HTR2B Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
GuideToPharmacology: 3357
- Version: 29-September-2020
Alternate Names:

5294 HUGO Gene ID

5294 HUGO Gene Symbol

5-hydroxytryptamine receptor 2B HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name 5-Hydroxytryptamine receptors

GuideToPharmacology Gene Category ID 1

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

DrugBank: BE0000393

Version: 5.1.7

Alternate Names:

HTR2B DrugBank Gene Name

P41595 UniProt Accession

3357 Entrez Gene Id

Gene Info:

Publications:

Schaerlinger et al., 2003, Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy., Br. J. Pharmacol.

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

DTC: HTR2B
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Semple G et al., 2009, Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation., Bioorg Med Chem Lett
ChemblInteractions: HTR2B
- Version: chembl_23
Alternate Names:

HTR2B GENE_SYMBOL

5-hydroxytryptamine receptor 2B UNIPROT

Serotonin receptor 2B UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000135914
- Version: 31-May-2017
Alternate Names:

ENSG00000135914 Gene Symbol

HTR2B Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
Pharos: HTR2B
- Version: 03-September-2020
Alternate Names:

P41595 UniProt ID

5-hydroxytryptamine receptor 2B Gene Name

Gene Info:

Gene Categories:

KINASE

Publications:
dGene: HTR2B
- Version: 27-Jun-2013
Alternate Names:

3357 Gene ID

5-HT(2B) dGene Synonym

5-HT2B dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: 5-HT 2B receptor
- Version: 2020.06.01
Alternate Names:

HTR2B TTD Gene Abbreviation

T31204 TTD Target ID

Gene Info:

Publications:
GO: HTR2B
- Version: 05-September-2020
Alternate Names:

Gene Info:

Gene Categories:

DRUG RESISTANCE, G PROTEIN COUPLED RECEPTOR

Publications:

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Direct Interaction?	False
Endogenous Drug?	False
Specific Action of the Ligand	Biased agonist

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False

Trial Name	agomelatine, AGO178C, S-20098,Valdoxan, Thymanax
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

Specific Action of the Ligand	Agonist
Endogenous Drug?	False
Direct Interaction?	False

Direct Interaction	yes
Mechanism of Interaction	Serotonin 2b (5-HT2b) receptor partial agonist

Direct Interaction	yes
Mechanism of Interaction	Serotonin 2b (5-HT2b) receptor antagonist

Specific Action of the Ligand	Partial agonist
Endogenous Drug?	False

Details of the Assay for Interaction	Biased for β-arrestin signalling.
Specific Action of the Ligand	Biased agonist
Endogenous Drug?	False

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Partial agonist

Trial Name	Silenor (SO-101)
Novel drug target	Established target

Trial Name	terguride
Novel drug target	Established target
Specific Action of the Ligand	Antagonist

5-HYDROXYTRYPTAMINE RECEPTOR 2B	Uniprot Protein Name
P41595	Uniprot Accession
5HT2B_HUMAN	Uniprot Id

ENSG00000135914	Ensembl Gene Id
HTR2B	Display Id
5-HYDROXYTRYPTAMINE 2B RECEPTOR (5-HT-2B) (SEROTONIN RECEPTOR 2B). [SOURCE:UNIPROT/SWISSPROT;ACC:P41595]	Description

5294	HUGO Gene ID
5294	HUGO Gene Symbol
5-hydroxytryptamine receptor 2B	HUGO Gene Name

HTR2B	DrugBank Gene Name
P41595	UniProt Accession
3357	Entrez Gene Id

HTR2B	GENE_SYMBOL
5-hydroxytryptamine receptor 2B	UNIPROT
Serotonin receptor 2B	UNIPROT

HTR2B Gene Record

HTR2B 3357 Druggable GenomeDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name PRX-08066 Novel drug target Established target

PMIDs: 20430844

Sources: TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19773162

Sources: DTC

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 12761331 10617681 14659797 16960982 17202450 11104741

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 11752352 17139284 497523 17016423

Sources: TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: 16495076 15466450 16629860

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752352 17139284 2975224 1361012 17016423

Sources: TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Biased agonist

PMIDs: 14659797

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 2871581

Sources: TTD DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False

PMIDs: 18703043 18691132 10641988 21440001 18096760

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Full agonist

PMIDs: 18691132 18992242 20426763 10641988 19570945

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name agomelatine, AGO178C, S-20098,Valdoxan, Thymanax Novel drug target Established target Specific Action of the Ligand Antagonist

PMIDs: None found

Sources: TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Specific Action of the Ligand Agonist Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: partial agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serotonin 2b (5-HT2b) receptor partial agonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name PRX-08066

Novel drug target Established target

PMIDs:
20430844

Sources:
TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
19773162

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

PMIDs:
12761331 10617681 14659797 16960982 17202450 11104741

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11752352 17139284 497523 17016423

Sources:
TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
16495076 15466450 16629860

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752352 17139284 2975224 1361012 17016423

Sources:
TEND TdgClinicalTrial TTD DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Biased agonist

PMIDs:
14659797

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

PMIDs:
2871581

Sources:
TTD DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
18703043 18691132 10641988 21440001 18096760

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
18691132 18992242 20426763 10641988 19570945

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name agomelatine, AGO178C, S-20098,Valdoxan, Thymanax

Novel drug target Established target

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 2b (5-HT2b) receptor partial agonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology