DGIdb - HTR1B Gene Record

HTR1B 3351 Druggable Genome

Alternate Names:

3351
5-HYDROXYTRYPTAMINE RECEPTOR 1B
HTR1B
5-HT-1B
5-HT-1D-beta
5-HT1B
5-HT1DB
HTR1D2
HTR1DB
S12
182131
5287
ENSG00000135312
OTTHUMG00000015066
Serotonin 1D beta receptor
Serotonin receptor 1B
5-HYDROXYTRYPTAMINE 1B RECEPTOR (5-HT-1B) (SEROTONIN RECEPTOR 1B) (5- HT1B) (5-HT-1D-BETA) (SEROTONIN 1D BETA RECEPTOR) (S12). [SOURCE:UNIPROT/SWISSPROT;ACC:P28222]
P28222
5HT1B_HUMAN
2
5-HT<sub>1B</sub> receptor
PA29549
5-HT 1B receptor
T07806
NM_000863
NP_000854

Gene Info:

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

(7 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Willems et al., 1999, Pharmacological evidence that alpha1-and alpha2-adrenoceptors mediate vasoconstriction of carotid arteriovenous anastomoses in anaesthetized pigs., Br. J. Pharmacol.
Villalón et al., 2004, 5-HT1B receptors and alpha 2A/2C-adrenoceptors mediate external carotid vasoconstriction to dihydroergotamine., Eur. J. Pharmacol.
Buzzi et al., 1991, Evidence for 5-HT1B/1D receptors mediating the antimigraine effect of sumatriptan and dihydroergotamine., Cephalalgia
Pauwels et al., 1998, Interaction of 5-HT1B/D ligands with recombinant h 5-HT1A receptors: intrinsic activity and modulation by G-protein activation state., Naunyn Schmiedebergs Arch. Pharmacol.
Yu et al., 1996, 5-Carboxamido-tryptamine, CP-122,288 and dihydroergotamine but not sumatriptan, CP-93,129, and serotonin-5-O-carboxymethyl-glycyl -tyrosinamide block dural plasma protein extravasation in knockout mice that lack 5-hydroxytryptamine1B receptors., Mol. Pharmacol.
Bang-Andersen et al., 2011, Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder., J. Med. Chem.
Tfelt-Hansen et al., 2000, Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy., Drugs
Comer, 2002, Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan., Headache
Markus et al., 2007, Frovatriptan review., Expert Opin Pharmacother
Parsons et al., 1998, Effects of the novel high-affinity 5-HT(1B/1D)-receptor ligand frovatriptan in human isolated basilar and coronary arteries., J. Cardiovasc. Pharmacol.
Elkind et al., 2004, Pharmacokinetics of frovatriptan in adolescent migraineurs., J Clin Pharmacol
Buchan et al., 2002, Frovatriptan: a review of drug-drug interactions., Headache
Dodick et al., 2007, Use of the sustained pain-free plus no adverse events endpoint in clinical trials of triptans in acute migraine., CNS Drugs
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Balbisi, 2006, Frovatriptan: a review of pharmacology, pharmacokinetics and clinical potential in the treatment of menstrual migraine., Ther Clin Risk Manag
Easthope et al., 2001, Frovatriptan., CNS Drugs
Deleu et al., 2000, Current and emerging second-generation triptans in acute migraine therapy: a comparative review., J Clin Pharmacol
Balbisi, 2004, Frovatriptan succinate, a 5-HT1B/1D receptor agonist for migraine., Int. J. Clin. Pract.
Napier et al., 1999, Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors., Eur. J. Pharmacol.
van den Broek et al., 2000, Pharmacological analysis of contractile effects of eletriptan and sumatriptan on human isolated blood vessels., Eur. J. Pharmacol.
Lambert et al., 2002, Suppression by eletriptan of the activation of trigeminovascular sensory neurons by glyceryl trinitrate., Brain Res.
Johnson et al., 2001, Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain., Eur. J. Pharmacol.
Knyihár-Csillik et al., 2000, Effects of eletriptan on the peptidergic innervation of the cerebral dura mater and trigeminal ganglion, and on the expression of c-fos and c-jun in the trigeminal complex of the rat in an experimental migraine model., Eur. J. Neurosci.
Martin, 1997, Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine., Cephalalgia
Pascual, 1998, [Mechanism of action of zolmitriptan]., Neurologia
Hargreaves et al., 1999, Pathophysiology of migraine--new insights., Can J Neurol Sci
de Almeida et al., 2001, Zolmitriptan--a 5-HT1B/D agonist, alcohol, and aggression in mice., Psychopharmacology (Berl.)
Gowin et al., 2010, Zolmitriptan and human aggression: interaction with alcohol., Psychopharmacology (Berl.)
Whale et al., 1999, Zolmitriptan-induced growth hormone release in humans: mediation by 5-HT1D receptors?, Psychopharmacology (Berl.)
Reuter et al., 2004, Effects of chronic sumatriptan and zolmitriptan treatment on 5-HT receptor expression and function in rats., Cephalalgia
Le Grand et al., 2000, Zolmitriptan stimulates a Ca(2+)-dependent K(+) current in C6 glioma cells stably expressing recombinant human 5-HT(1B) receptors., Eur. J. Pharmacol.
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
Perroud N et al., 2011, Clinical and genetic correlates of suicidal ideation during antidepressant treatment in a depressed outpatient sample., Pharmacogenomics
Grånäs et al., 1999, Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT(1B) receptor., Eur. J. Pharmacol.
Roy et al., 2000, Expression of 5-hydroxytryptamine receptor subtype messenger RNA in interstitial cells from human heart valves., J. Heart Valve Dis.
Mitsikostas et al., 1999, Both 5-HT1B and 5-HT1F receptors modulate c-fos expression within rat trigeminal nucleus caudalis., Eur. J. Pharmacol.
Nikai et al., 2008, Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan., Pain
Razzaque et al., 2002, 5-HT1B-receptors and vascular reactivity in human isolated blood vessels: assessment of the potential craniovascular selectivity of sumatriptan., Br J Clin Pharmacol
Cohen et al., 1999, Multiple microvascular and astroglial 5-hydroxytryptamine receptor subtypes in human brain: molecular and pharmacologic characterization., J. Cereb. Blood Flow Metab.
Akin et al., 2002, Involvement of 5-HT1B and 5-HT1D receptors in sumatriptan mediated vasocontractile response in rabbit common carotid artery., Br. J. Pharmacol.
Mitsikostas et al., 2002, 5-Hydroxytryptamine(1B/1D) and 5-hydroxytryptamine1F receptors inhibit capsaicin-induced c-fos immunoreactivity within mouse trigeminal nucleus caudalis., Cephalalgia
Cohen et al., 1999, 5-Hydroxytryptamine(1A) receptor activation enhances norepinephrine release from nerves in the rabbit saphenous vein., J. Pharmacol. Exp. Ther.
Dupuis et al., 1999, Magnitude of 5-HT1B and 5-HT1A receptor activation in guinea-pig and rat brain: evidence from sumatriptan dimer-mediated [35S]GTPgammaS binding responses., Brain Res. Mol. Brain Res.
Kvernmo et al., 2008, Receptor-binding and pharmacokinetic properties of dopaminergic agonists., Curr Top Med Chem
Lam, 2000, Clinical pharmacology of dopamine agonists., Pharmacotherapy
Massiou, 2001, Naratriptan., Curr Med Res Opin
Hoskin et al., 2004, The 5-hydroxytryptamine1B/1D/1F receptor agonists eletriptan and naratriptan inhibit trigeminovascular input to the nucleus tractus solitarius in the cat., Brain Res.
Lambert, 2005, Preclinical neuropharmacology of naratriptan., CNS Drug Rev
Dulli, 1999, Naratriptan: an alternative for migraine., Ann Pharmacother
Akin et al., 2002, Agonist-directed trafficking explaining the difference between response pattern of naratriptan and sumatriptan in rabbit common carotid artery., Br. J. Pharmacol.
Johnston et al., 2010, Triptans for the management of migraine., Drugs
Boers et al., 2004, Naratriptan has a selective inhibitory effect on trigeminovascular neurones at central 5-HT1A and 5-HT(1B/1D) receptors in the cat: implications for migraine therapy., Cephalalgia
Wellington et al., 2002, Rizatriptan: an update of its use in the management of migraine., Drugs
Wellington et al., 2002, Spotlight on rizatriptan in migraine., CNS Drugs
Wackenfors et al., 2005, Triptans induce vasoconstriction of human arteries and veins from the thoracic wall., J. Cardiovasc. Pharmacol.
Williamson et al., 2001, The anti-migraine 5-HT(1B/1D) agonist rizatriptan inhibits neurogenic dural vasodilation in anaesthetized guinea-pigs., Br. J. Pharmacol.
Ikemoto et al., 2004, [Rizatriptan (Maxalt), a new entity of triptan for migraine: pharmacology and therapeutic relevance]., Nippon Yakurigaku Zasshi
Gassó P et al., 2017, Epigenetic and genetic variants in the HTR1B gene and clinical improvement in children and adolescents treated with fluoxetine., Prog Neuropsychopharmacol Biol Psychiatry
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
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
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
Bou et al., 2000, Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine., Eur. J. Pharmacol.
Fleishaker et al., 2000, Pharmacokinetic interaction between verapamil and almotriptan in healthy volunteers., Clin. Pharmacol. Ther.
Millan et al., 2000, Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states., Synapse
Kaumann, 1983, Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors., Naunyn Schmiedebergs Arch. Pharmacol.
Villalón et al., 1999, Canine external carotid vasoconstriction to methysergide, ergotamine and dihydroergotamine: role of 5-HT1B/1D receptors and alpha2-adrenoceptors., Br. J. Pharmacol.
Cohen et al., 2000, Contractile responses to sumatriptan and ergotamine in the rabbit saphenous vein: effect of selective 5-HT(1F) receptor agonists and PGF(2alpha)., Br. J. Pharmacol.
Valdivia et al., 2004, 5-HT1B receptors, alpha2A/2C- and, to a lesser extent, alpha1-adrenoceptors mediate the external carotid vasoconstriction to ergotamine in vagosympathectomised dogs., Naunyn Schmiedebergs Arch. Pharmacol.
Schmidt et al., 2001, Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile., Eur. J. Pharmacol.
Matsumoto et al., 1992, Characterization of 5-hydroxytryptamine1B receptors in rat spinal cord via [125I]iodocyanopindolol binding and inhibition of [3H]-5-hydroxytryptamine release., J. Pharmacol. Exp. Ther.
Amitai M et al., 2016, Pharmacogenetics of citalopram-related side effects in children with depression and/or anxiety disorders., J Neural Transm (Vienna)

FROVATRIPTAN HTR1B

Interaction Score: 5.23

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name frovatriptan,Frovelan, Frova

Novel drug target Established target

Specific Action of the Ligand Agonist

PMIDs:
11152011 12028320 18001261 9700983 15342617 12028322 17190530 11752352 18360605 11735616 10883409 15311727

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
ALMOTRIPTAN HTR1B

Interaction Score: 4.42

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
10193663 11050304 11134654 11752352 10824628 11069595

Sources:
TdgClinicalTrial TEND GuideToPharmacology
NARATRIPTAN HTR1B

Interaction Score: 2.75

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12463278 14725972 16389295 10410185 12010764 11752352 20687618 14728705 11152011 9650800

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
ZOLMITRIPTAN HTR1B

Interaction Score: 2.62

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Direct Interaction yes

Trial Name zolmitriptan,Zomig

PMIDs:
9399012 9859690 10563228 11513839 11594437 20407761 10463324 11752352 15096229 10844127 29352859

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD
RIZATRIPTAN HTR1B

Interaction Score: 1.96

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12093318 12269863 15821444 11487512 9650800 11752352 15056946

Sources:
TdgClinicalTrial TEND GuideToPharmacology
ELETRIPTAN HTR1B

Interaction Score: 1.47

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
10193663 11050304 12384251 11513839 11752352 11069595

Sources:
TEND GuideToPharmacology TTD
DIHYDROERGOTAMINE HTR1B

Interaction Score: 0.86

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name MT 300

Novel drug target Established target

Trial Name MAP-0004, TEMPO Migraine,Levadex

PMIDs:
10455274 14744615 1660351 9650800 8622623

Sources:
TdgClinicalTrial GuideToPharmacology
SUMATRIPTAN HTR1B

Interaction Score: 0.82

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name MT 400,Treximet

Novel drug target Established target

Trial Name NP101,Zelrix

PMIDs:
10513577 10772044 10225363 18723285 11874390 10458598 12010765 12110114 11752352 10454495 10101238

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
ERGOTAMINE HTR1B

Interaction Score: 0.65

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10455274 10188968 11015308 15224175

Sources:
TdgClinicalTrial TEND
TRELANSERIN HTR1B

Interaction Score: 0.65

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name trelanserin, SL 65.0472

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
ALNIDITAN HTR1B

Interaction Score: 0.49

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NARATRIPTAN HYDROCHLORIDE HTR1B

Interaction Score: 0.49

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RIZATRIPTAN BENZOATE HTR1B

Interaction Score: 0.49

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SUMATRIPTAN SUCCINATE HTR1B

Interaction Score: 0.49

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL159332 HTR1B

Interaction Score: 0.49

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
AVITRIPTAN HTR1B

Interaction Score: 0.49

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
FROVATRIPTAN SUCCINATE HTR1B

Interaction Score: 0.49

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
GR-55562 HTR1B

Interaction Score: 0.33

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
DONITRIPTAN HTR1B

Interaction Score: 0.33

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology TTD
ALMOTRIPTAN MALATE HTR1B

Interaction Score: 0.33

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ELETRIPTAN HYDROBROMIDE HTR1B

Interaction Score: 0.33

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
ELTOPRAZINE HTR1B

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
VORTIOXETINE HTR1B

Interaction Score: 0.33

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
21486038

Sources:
TdgClinicalTrial GuideToPharmacology
LIOTHYRONINE HTR1B

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21449676

Sources:
PharmGKB
GSK163090 HTR1B

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
YOHIMBINE HTR1B

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
10611634 6136920

Sources:
GuideToPharmacology
CABERGOLINE HTR1B

Interaction Score: 0.2

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
18691132 10641988

Sources:
GuideToPharmacology
PERGOLIDE HTR1B

Interaction Score: 0.2

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
18691132 10641988

Sources:
GuideToPharmacology
PIPAMPERONE HTR1B

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
ASENAPINE HTR1B

Interaction Score: 0.2

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Full agonist

Trial Name Asenapine

PMIDs:
18308814 21655346

Sources:
TdgClinicalTrial GuideToPharmacology
ARIPIPRAZOLE HTR1B

Interaction Score: 0.18

Interaction Types & Directionality:

ligand

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
17848919 26346901

Sources:
GuideToPharmacology
NEFAZODONE HTR1B

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21449676

Sources:
PharmGKB
OCAPERIDONE HTR1B

Interaction Score: 0.16

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CLOMIPRAMINE HTR1B

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21449676

Sources:
PharmGKB
ZIPRASIDONE HTR1B

Interaction Score: 0.14

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
17848919 11513838

Sources:
GuideToPharmacology
RAUWOLSCINE HTR1B

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
VENLAFAXINE HTR1B

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21449676

Sources:
PharmGKB
LISURIDE HTR1B

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
18691132

Sources:
GuideToPharmacology
METHYSERGIDE HTR1B

Interaction Score: 0.12

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
1738111

Sources:
GuideToPharmacology
CAPESEROD HTR1B

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BRL-15,572 HTR1B

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
None found

Sources:
GuideToPharmacology
BROMOCRIPTINE HTR1B

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
18691132 10641988

Sources:
GuideToPharmacology
8-OH-DPAT HTR1B

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
OXYMETAZOLINE HTR1B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ERGOLOID MESYLATES HTR1B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRYPTAMINE HTR1B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? True

Specific Action of the Ligand Full agonist

PMIDs:
None found

Sources:
GuideToPharmacology
PAROXETINE HTR1B

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21449676

Sources:
PharmGKB
TERGURIDE HTR1B

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
None found

Sources:
GuideToPharmacology
ROXINDOLE HTR1B

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
XANOMELINE HTR1B

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ZOTEPINE HTR1B

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
FLUPHENAZINE HTR1B

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
FLUOXETINE HTR1B

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28025020

Sources:
PharmGKB
CITALOPRAM HTR1B

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27324805

Sources:
PharmGKB
ESCITALOPRAM HTR1B

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
METERGOLINE HTR1B

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
SERTINDOLE HTR1B

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
SEROTONIN HTR1B

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? True

PMIDs:
None found

Sources:
GuideToPharmacology
KETANSERIN HTR1B

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
METITEPINE HTR1B

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
RITANSERIN HTR1B

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
OLANZAPINE HTR1B

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

Novel drug target Established target

Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

PMIDs:
17848919

Sources:
TdgClinicalTrial GuideToPharmacology
LITHIUM HTR1B

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21449676

Sources:
PharmGKB
CLOZAPINE HTR1B

Interaction Score: 0.03

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
17848919

Sources:
GuideToPharmacology
RISPERIDONE HTR1B

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology

Ensembl: ENSG00000135312
- Version: 101_38
Alternate Names:

HTR1B Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:

RussLampel: ENSG00000135312

Version: 26-July-2011

Alternate Names:

5-HYDROXYTRYPTAMINE 1B RECEPTOR (5-HT-1B) (SEROTONIN RECEPTOR 1B) (5- HT1B) (5-HT-1D-BETA) (SEROTONIN 1D BETA RECEPTOR) (S12). [SOURCE:UNIPROT/SWISSPROT;ACC:P28222] Description

ENSG00000135312 Ensembl Gene Id

HTR1B Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

TdgClinicalTrial: P28222
- Version: January-2014
Alternate Names:

HTR1B Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
TEND: P28222
- Version: 01-August-2011
Alternate Names:

P28222 Uniprot Accession

HTR1B Gene Symbol

ENSG00000135312 Ensembl Gene Id

Gene Info:

Target Main Class Receptors

Target Subclass Rhodopsin

Target Subclass GPCR

Publications:
HopkinsGroom: P28222
- Version: 11-September-2012
Alternate Names:

ENSG00000135312 Ensembl Gene Id

5-HYDROXYTRYPTAMINE RECEPTOR 1B Uniprot Protein Name

HTR1B Uniprot Gene Name

Gene Info:

Interpro Type Family

Interpro Acc IPR000276

Human Readable Name G PROTEIN COUPLED RECEPTOR

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
GuideToPharmacology: 3351
- Version: 29-September-2020
Alternate Names:

5287 HUGO Gene ID

5287 HUGO Gene Symbol

5-hydroxytryptamine receptor 1B HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name 5-Hydroxytryptamine receptors

GuideToPharmacology Gene Category ID 1

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

PharmGKB: HTR1B

Version: 18-August-2020

Alternate Names:

PA29549 PharmGKB ID

Gene Info:

Publications:

Perroud N et al., 2011, Clinical and genetic correlates of suicidal ideation during antidepressant treatment in a depressed outpatient sample., Pharmacogenomics

Gassó P et al., 2017, Epigenetic and genetic variants in the HTR1B gene and clinical improvement in children and adolescents treated with fluoxetine., Prog Neuropsychopharmacol Biol Psychiatry

Amitai M et al., 2016, Pharmacogenetics of citalopram-related side effects in children with depression and/or anxiety disorders., J Neural Transm (Vienna)

ChemblInteractions: HTR1DB
- Version: chembl_23
Alternate Names:

HTR1DB GENE_SYMBOL

HTR1B GENE_SYMBOL

5-hydroxytryptamine receptor 1B UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000135312
- Version: 31-May-2017
Alternate Names:

ENSG00000135312 Gene Symbol

HTR1B Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
dGene: HTR1B
- Version: 27-Jun-2013
Alternate Names:

3351 Gene ID

5-HT1B dGene Synonym

5-HT1DB dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: 5-HT 1B receptor
- Version: 2020.06.01
Alternate Names:

HTR1B TTD Gene Abbreviation

T07806 TTD Target ID

Gene Info:

Publications:

Trial Name	frovatriptan,Frovelan, Frova
Novel drug target	Established target
Specific Action of the Ligand	Agonist

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

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

Mechanism of Interaction	Serotonin 1b (5-HT1b) receptor agonist
Direct Interaction	yes
Trial Name	zolmitriptan,Zomig

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

Trial Name	MT 300
Novel drug target	Established target
Trial Name	MAP-0004, TEMPO Migraine,Levadex

Trial Name	MT 400,Treximet
Novel drug target	Established target
Trial Name	NP101,Zelrix

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Direct Interaction	yes
Mechanism of Interaction	Serotonin 1b (5-HT1b) receptor antagonist

Specific Action of the Ligand	Inverse agonist
Endogenous Drug?	False

Trial Name	olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv
Novel drug target	Established target
Trial Name	Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

5-HYDROXYTRYPTAMINE 1B RECEPTOR (5-HT-1B) (SEROTONIN RECEPTOR 1B) (5- HT1B) (5-HT-1D-BETA) (SEROTONIN 1D BETA RECEPTOR) (S12). [SOURCE:UNIPROT/SWISSPROT;ACC:P28222]	Description
ENSG00000135312	Ensembl Gene Id
HTR1B	Display Id

P28222	Uniprot Accession
HTR1B	Gene Symbol
ENSG00000135312	Ensembl Gene Id

5287	HUGO Gene ID
5287	HUGO Gene Symbol
5-hydroxytryptamine receptor 1B	HUGO Gene Name

HTR1DB	GENE_SYMBOL
HTR1B	GENE_SYMBOL
5-hydroxytryptamine receptor 1B	UNIPROT

HTR1B Gene Record

HTR1B 3351 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name frovatriptan,Frovelan, Frova Novel drug target Established target Specific Action of the Ligand Agonist

PMIDs: 11152011 12028320 18001261 9700983 15342617 12028322 17190530 11752352 18360605 11735616 10883409 15311727

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 10193663 11050304 11134654 11752352 10824628 11069595

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 12463278 14725972 16389295 10410185 12010764 11752352 20687618 14728705 11152011 9650800

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist Direct Interaction yes Trial Name zolmitriptan,Zomig

PMIDs: 9399012 9859690 10563228 11513839 11594437 20407761 10463324 11752352 15096229 10844127 29352859

Sources: TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 12093318 12269863 15821444 11487512 9650800 11752352 15056946

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 10193663 11050304 12384251 11513839 11752352 11069595

Sources: TEND GuideToPharmacology TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name MT 300 Novel drug target Established target Trial Name MAP-0004, TEMPO Migraine,Levadex

PMIDs: 10455274 14744615 1660351 9650800 8622623

Sources: TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name MT 400,Treximet Novel drug target Established target Trial Name NP101,Zelrix

PMIDs: 10513577 10772044 10225363 18723285 11874390 10458598 12010765 12110114 11752352 10454495 10101238

Sources: TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10455274 10188968 11015308 15224175

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name trelanserin, SL 65.0472 Mechanism of Interaction Serotonin 1b (5-HT1b) receptor antagonist

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions

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: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

PMIDs: None found

Sources: ChemblInteractions

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: agonist (activating)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serotonin 1b (5-HT1b) receptor 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: agonist (activating)

Interaction Info: Specific Action of the Ligand Full agonist Endogenous Drug? False Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name frovatriptan,Frovelan, Frova

Novel drug target Established target

Specific Action of the Ligand Agonist

PMIDs:
11152011 12028320 18001261 9700983 15342617 12028322 17190530 11752352 18360605 11735616 10883409 15311727

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
10193663 11050304 11134654 11752352 10824628 11069595

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12463278 14725972 16389295 10410185 12010764 11752352 20687618 14728705 11152011 9650800

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Direct Interaction yes

Trial Name zolmitriptan,Zomig

PMIDs:
9399012 9859690 10563228 11513839 11594437 20407761 10463324 11752352 15096229 10844127 29352859

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12093318 12269863 15821444 11487512 9650800 11752352 15056946

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
10193663 11050304 12384251 11513839 11752352 11069595

Sources:
TEND GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name MT 300

Novel drug target Established target

Trial Name MAP-0004, TEMPO Migraine,Levadex

PMIDs:
10455274 14744615 1660351 9650800 8622623

Sources:
TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name MT 400,Treximet

Novel drug target Established target

Trial Name NP101,Zelrix

PMIDs:
10513577 10772044 10225363 18723285 11874390 10458598 12010765 12110114 11752352 10454495 10101238

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10455274 10188968 11015308 15224175

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name trelanserin, SL 65.0472

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions

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:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions

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:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor 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:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 1b (5-HT1b) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions