5-HT<sub>1B</sub> receptor | 5-Hydroxytryptamine receptors | IUPHAR Guide to IMMUNOPHARMACOLOGY

Top ▲

5-HT1B receptor

  Target has curated data in GtoImmuPdb

Target id: 2

Nomenclature: 5-HT1B receptor

Family: 5-Hydroxytryptamine receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

Contents:

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 390 6q13 HTR1B 5-hydroxytryptamine receptor 1B 18,24,46,56,86
Mouse 7 386 9 E1 Htr1b 5-hydroxytryptamine (serotonin) receptor 1B 39
Rat 7 386 8q31 Htr1b 5-hydroxytryptamine receptor 1B 1,79
Previous and Unofficial Names
5-HT1B | 5-HT1DB | HTR1D2 | 5-HT1B serotonin receptor | serotonin receptor 1B | 5-HT1Dβ [56,86] | 5-hydroxytryptamine (serotonin) receptor 1B, G protein-coupled
Database Links
Specialist databases
GPCRDB 5ht1b_human (Hs), 5ht1b_mouse (Mm), 5ht1b_rat (Rn)
Other databases
ChEMBL Target 106 (Hs), 10577 (Rn)
DrugBank Target P28222 (Hs)
Ensembl Gene ENSG00000135312 (Hs), ENSMUSG00000049511 (Mm), ENSRNOG00000013042 (Rn)
Entrez Gene 3351 (Hs), 15551 (Mm), 25075 (Rn)
Human Protein Atlas ENSG00000135312 (Hs)
KEGG Gene hsa:3351 (Hs), mmu:15551 (Mm), rno:25075 (Rn)
OMIM 182131 (Hs)
RefSeq Nucleotide NM_000863 (Hs), NM_010482 (Mm), NM_022225 (Rn)
RefSeq Protein NP_000854 (Hs), NP_034612 (Mm), NP_071561 (Rn)
UniProtKB P28222 (Hs), P28334 (Mm), P28564 (Rn)
Wikipedia HTR1B (Hs)
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the chimeric protein of 5-HT1B-BRIL in complex with dihydroergotamine
PDB Id:  4IAQ
Ligand:  dihydroergotamine
Resolution:  2.8Å
Species:  Human
References:  80
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the chimeric protein of 5-HT1B-BRIL in complex with ergotamine
PDB Id:  4IAR
Ligand:  ergotamine
Resolution:  2.7Å
Species:  Human
References:  80
Natural/Endogenous Ligands
5-hydroxytryptamine
Comments: Endogenous ligand tryptamine is a weak agonist

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
[3H]N-methyl-AZ10419369 Hs Partial agonist 9.4 pKd 36
pKd 9.4 (Kd 3.7x10-10 M) [36]
[3H]8-OH-DPAT Hs Full agonist 8.9 pKd 51
pKd 8.9 [51]
[125I]GTI Rn Agonist 8.9 pKd 8-9
pKd 8.9 (Kd 1.3x10-9 M) [8-9]
[3H]alniditan Hs Full agonist 8.6 – 9.0 pKd 31
pKd 8.6 – 9.0 (Kd 2.51x10-9 – 1x10-9 M) [31]
[3H]eletriptan Hs Partial agonist 8.5 pKd 49
pKd 8.5 (Kd 3x10-9 M) [49]
[3H]sumatriptan Hs Partial agonist 8.0 pKd 49
pKd 8.0 (Kd 1.1x10-8 M) [49]
5-hydroxytryptamine Hs Full agonist 7.5 – 8.4 pKd 54,86
pKd 7.5 – 8.4 [54,86]
donitriptan Rn Partial agonist 9.7 pKi 25
pKi 9.7 [25]
oxymetazoline Hs Full agonist 9.5 pKi 29
pKi 9.5 [29]
GR 127935 Hs Partial agonist 9.0 – 9.8 pKi 16,27,60,68,85
pKi 9.0 – 9.8 [16,27,60,68,85]
donitriptan Hs Full agonist 9.4 pKi 25
pKi 9.4 [25]
L-694,247 Hs Full agonist 9.2 pKi 17
pKi 9.2 (Ki 6.3x10-10 M) [17]
SB 216641 Hs Partial agonist 9.0 pKi 60
pKi 9.0 [60]
alniditan Hs Full agonist 8.8 – 9.0 pKi 32
pKi 8.8 – 9.0 [32]
7-methoxy-1-naphthylpiperazine Hs Full agonist 8.7 pKi 27
pKi 8.7 [27]
CP94253 Hs Full agonist 8.7 pKi 28
pKi 8.7 (Ki 2x10-9 M) [28]
dihydroergotamine Hs Full agonist 8.0 – 9.2 pKi 32,54
pKi 8.0 – 9.2 [32,54]
CGS-12066 Hs Full agonist 8.1 – 8.7 pKi 17,86
pKi 8.1 – 8.7 [17,86]
ziprasidone Hs Full agonist 8.3 pKi 67
pKi 8.3 [67]
5-CT Hs Full agonist 7.7 – 8.8 pKi 54,86
pKi 7.7 – 8.8 [54,86]
5-hydroxytryptamine Hs Full agonist 7.4 – 9.0 pKi 12,50-51,68,85-86
pKi 7.4 – 9.0 [12,50-51,68,85-86]
5-(nonyloxy)-tryptamine Hs Full agonist 8.2 pKi 17
pKi 8.2 [17]
lysergol Hs Full agonist 7.5 – 8.9 pKi 54,86
pKi 7.5 – 8.9 [54,86]
5-CT Mm Full agonist 8.1 pKi 39
pKi 8.1 [39]
5-hydroxytryptamine Mm Full agonist 8.1 pKi 39
pKi 8.1 [39]
asenapine Hs Full agonist 8.1 pKi 67
pKi 8.1 [67]
RU 24969 Hs Full agonist 8.1 pKi 39
pKi 8.1 [39]
naratriptan Hs Partial agonist 8.1 pKi 49
pKi 8.1 [49]
eletriptan Hs Full agonist 8.0 pKi 49
pKi 8.0 (Ki 1x10-8 M) [49]
frovatriptan Hs Agonist 8.0 pKi 89
pKi 8.0 (Ki 1.03x10-8 M) [89]
BMS 181,101 Hs Partial agonist 7.6 – 8.1 pKi 50
pKi 7.6 – 8.1 [50]
1-naphthylpiperazine Hs Full agonist 7.7 – 7.9 pKi 27,54,86
pKi 7.7 – 7.9 [27,54,86]
lisuride Hs Partial agonist 7.7 pKi 43
pKi 7.7 [43]
zolmitriptan Hs Partial agonist 7.7 pKi 49
pKi 7.7 [49]
vortioxetine Hs Partial agonist 7.5 pKi 4
pKi 7.5 (Ki 3.3x10-8 M) [4]
5-MeOT Hs Full agonist 7.3 – 7.5 pKi 54,86
pKi 7.3 – 7.5 [54,86]
dipropyl-5-CT Hs Full agonist 7.4 pKi 86
pKi 7.4 [86]
sumatriptan Hs Partial agonist 6.5 – 8.1 pKi 17,32,44,49-50,54,86
pKi 6.5 – 8.1 (Ki 3.16x10-7 – 7.94x10-9 M) [17,32,44,49-50,54,86]
xanomeline Hs Full agonist 7.3 pKi 83
pKi 7.3 [83]
rizatriptan Hs Partial agonist 6.9 pKi 49
pKi 6.9 [49]
L-775,606 Hs Partial agonist 6.3 – 6.9 pKi 50
pKi 6.3 – 6.9 [50]
pergolide Hs Full agonist 6.6 pKi 43
pKi 6.6 [43]
terguride Hs Partial agonist 6.6 pKi 43
pKi 6.6 [43]
TFMPP Hs Full agonist 6.2 – 6.9 pKi 54,86
pKi 6.2 – 6.9 [54,86]
bromocriptine Hs Partial agonist 6.5 pKi 43
pKi 6.5 [43]
LY344864 Hs Full agonist 6.3 pKi 57
pKi 6.3 [57]
cabergoline Hs Full agonist 6.3 pKi 43
pKi 6.3 [43]
olanzapine Hs Full agonist 6.3 pKi 67
pKi 6.3 [67]
tryptamine Hs Full agonist 6.3 pKi 86
pKi 6.3 [86]
clozapine Hs Full agonist 6.2 pKi 67
pKi 6.2 [67]
BRL-15572 Hs Partial agonist 6.1 pKi 60
pKi 6.1 [60]
aripiprazole Hs Full agonist 6.1 pKi 70
pKi 6.1 [70]
2-methyl-5-HT Hs Full agonist 6.1 pKi 86
pKi 6.1 [86]
roxindole Hs Partial agonist 5.8 – 6.0 pKi 43,51
pKi 5.8 – 6.0 [43,51]
capeserod Hs Partial agonist 5.3 pKi 48
pKi 5.3 [48]
CP-122288 Hs Full agonist 7.6 pIC50 14
pIC50 7.6 [14]
L-772,405 Hs Full agonist 6.8 pIC50 64
pIC50 6.8 [64]
8-OH-DPAT Hs Full agonist 6.2 pIC50 14
pIC50 6.2 [14]
[11C]AZ10419369 Hs Partial agonist - - 78
[78]
View species-specific agonist tables
Agonist Comments
Frovatriptan is selective for 1B and 1D 5-HT receptor subtypes compared to the 1A subtype [89].
BRL-15572 can be used to distinguish between 5-HT1D and 5-HT1B receptors, being approximately 60-fold selective for the 1D subtype [60].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
GR-55562 Hs Antagonist 7.4 pKB 22
pKB 7.4 [22]
[3H]GR 125,743 Hs Antagonist 8.6 – 9.2 pKd 17,88
pKd 8.6 – 9.2 (Kd 2.6x10-9 – 7.1x10-10 M) [17,88]
GR 127935 Hs Antagonist 9.2 pKi 17
pKi 9.2 [17]
5-OH-DPAT Mm Antagonist 8.4 pKi 39
pKi 8.4 [39]
SB 224289 Hs Inverse agonist 8.2 – 8.6 pKi 16,50,68
pKi 8.2 – 8.6 (Ki 6.31x10-9 – 2.51x10-9 M) [16,50,68]
ketanserin Mm Antagonist 8.3 pKi 39
pKi 8.3 [39]
spiperone Mm Antagonist 8.3 pKi 39
pKi 8.3 [39]
yohimbine Mm Antagonist 8.3 pKi 39
pKi 8.3 [39]
mianserin Mm Antagonist 8.3 pKi 39
pKi 8.3 [39]
SB236057 Hs Inverse agonist 8.2 pKi 41
pKi 8.2 (Ki 6.31x10-9 M) [41]
SB 272183 Hs Antagonist 8.1 pKi 84
pKi 8.1 [84]
(-)-pindolol Mm Antagonist 8.1 pKi 39
pKi 8.1 [39]
cyanopindolol Mm Antagonist 8.1 pKi 39
pKi 8.1 [39]
SB 649915 Hs Antagonist 8.0 pKi 82
pKi 8.0 [82]
methiothepin Hs Inverse agonist 7.1 – 8.5 pKi 17,50,54,85
pKi 7.1 – 8.5 [17,50,54,85]
GR-55562 Hs Antagonist 7.5 pKi 17
pKi 7.5 [17]
yohimbine Hs Antagonist 6.8 – 7.6 pKi 44,86
pKi 6.8 – 7.6 [44,86]
zotepine Hs Antagonist 7.2 pKi 67
pKi 7.2 [67]
metergoline Hs Antagonist 7.2 pKi 54
pKi 7.2 [54]
methysergide Hs Antagonist 6.6 – 7.6 pKi 54,86
pKi 6.6 – 7.6 [54,86]
sertindole Hs Antagonist 7.0 pKi 67
pKi 7.0 [67]
risperidone Hs Antagonist 6.6 – 7.3 pKi 31,67,69
pKi 6.6 – 7.3 [31,67,69]
rauwolscine Hs Antagonist 6.5 – 7.4 pKi 54,86
pKi 6.5 – 7.4 [54,86]
9-OH-risperidone Hs Antagonist 6.8 pKi 67
pKi 6.8 [67]
SB 714786 Hs Antagonist 6.7 pKi 82
pKi 6.7 [82]
(S)-flurocarazolol Hs Antagonist 6.5 pKi 62
pKi 6.5 [62]
pipamperone Hs Antagonist 6.2 pKi 67
pKi 6.2 [67]
(R)-flurocarazolol Hs Antagonist 6.1 pKi 62
pKi 6.1 [62]
S33084 Hs Antagonist 6.1 pKi 42
pKi 6.1 [42]
(+)-WAY 100135 Hs Antagonist 5.8 pKi 12
pKi 5.8 [12]
ocaperidone Hs Antagonist 6.9 – 7.2 pIC50 31
pIC50 6.9 – 7.2 [31]
ritanserin Hs Antagonist 6.0 – 6.5 pIC50 14,31
pIC50 6.0 – 6.5 [14,31]
ketanserin Hs Antagonist 5.2 – 5.4 pIC50 14,31
pIC50 5.2 – 5.4 [14,31]
View species-specific antagonist tables
Antagonist Comments
It is possible that radioligand [3H]N-methyl-AZ10419369 may have properties as a partial agonist at the 5-HT1B receptor [36].
Allosteric Modulators
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
5-HT-moduline Hs Negative 11.9 pIC50 63
pIC50 11.9 [63]
Immunopharmacology Comments
The expression of 5-HT1B receptors on immune cells indicates that it plays some part in immune/inflammatory responses [81].
Cell Type Associations
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   mature eosinophil (CL:0000041)
Comment:  Expressed by eosinophils.
References:  81
Immuno Cell Type:  Dendritic cells
Cell Ontology Term:   dendritic cell (CL:0000451)
Comment:  Involved in DC chemotaxis.
References:  2
Immuno Cell Type:  T cells
Comment:  Involved in T cell proliferation.
References:  2
Immuno Process Associations
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0002031 G protein-coupled receptor internalization IEA
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  33,90
Tissue Distribution
Benign and malignant prostate tissue.
Species:  Human
Technique:  Western blotting.
References:  13
Brain: substantia nigra, globus pallidus > striatum > amygdala, hippocampus, septa region, hypothalamus.
Species:  Human
Technique:  Radioligand binding.
References:  76
Trigeminal ganglion.
Species:  Human
Technique:  immunocytochemistry.
References:  21
Cortical cerebral arteries (smooth muscle cell layer > endothelial cell layer).
Species:  Human
Technique:  immunocytochemistry.
References:  52
Coronary artery > atrium > ventricle, epicardium.
Species:  Human
Technique:  RT-PCR.
References:  53
Brain: substantia nigra, globus pallidus > caudate nucleus, putamen, nucleus accumbens, central gray, hippocampal formation > various cortical regions.
Species:  Human
Technique:  Radioligand binding.
References:  7
Brain: striatum, cortex, lateral geniculate nucleus, raphe nucleus.
Species:  Human
Technique:  in situ hybridisation.
References:  77
Suprachiasmatic nucleus.
Species:  Mouse
Technique:  Electron microscopic immunocytochemistry.
References:  6,58
Hypothalamus: magnocellular nuclei > supraoptic nucleus, paraventricular nucleus (dorsolateral) and accessory perifornical, circular and retrochiasmatic nuclei.
Species:  Rat
Technique:  Immunohistochemistry.
References:  37
Lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  59
Suprachiasmatic nucleus.
Species:  Rat
Technique:  Radioligand binding.
References:  38
Trigeminal ganglion.
Species:  Rat
Technique:  Immunohistochemistry.
References:  35
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  74
CNS: ventral pallidum, globus pallidus, dorsal subiculum, substantia nigra > caudate–putamen, entopeduncular nucleus, superficial gray layer of the superior colliculus, deep nuclei of the cerebellum > cerebral cortex, thalamus.
Species:  Rat
Technique:  immunocytochemistry.
References:  65
Expression Datasets

Show »

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

There should be a chart of expression data here, you may need to enable JavaScript!
Functional Assays
Measurement of cAMP levels in mouse adrenal Y-1 cells transfected with the 5-HT1B receptor.
Species:  Human
Tissue:  Y-1 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  86
Measurement of cAMP levels in rat C6 glial cells transfected with the human 5-HT1B receptor.
Species:  Human
Tissue:  C6 glial cells.
Response measured:  Inhibition of cAMP accumulation.
References:  56
Measurement of cell growth ([3H]thymidine incorporation) of rat C6 glial cells transfected with the 5-HT1B receptor.
Species:  Human
Tissue:  C6 glial cells.
Response measured:  Cell proliferation.
References:  56
Measurement of cAMP levels in COS-7 cells transfected with the rat 5-HT1B receptor.
Species:  Rat
Tissue:  COS-7 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  1
Measurement of cAMP levels in NIH3T3 cells endogenously expressing the 5-HT1B receptor.
Species:  Mouse
Tissue:  NIH3T3 cell line.
Response measured:  Inhibition of cAMP accumulation.
References:  39
Physiological Functions
Vasoconstriction.
Species:  Human
Tissue:  Coronary artery.
References:  53
Vasocontriction.
Species:  Human
Tissue:  Cortical cerebral artery.
References:  52
Mediation of impulsivity and prefrontal cortex-dependent learning and memory.
Species:  Mouse
Tissue:  In vivo.
References:  55
Regulation of hippocampal functions.
Species:  Rat
Tissue:  In vivo.
References:  10
Inhibition of food intake.
Species:  Rat
Tissue:  In vivo.
References:  30
Presynaptic inhibition of GABA release onto GABAB receptors but not GABAA.
Species:  Rat
Tissue:  Dopamine-containing neurons of the midbrain.
References:  26
Inhibition of GABA release.
Species:  Rat
Tissue:  Globus pallidus.
References:  11
Relief from akinesia.
Species:  Rat
Tissue:  In vivo.
References:  11
Lowering of hippocampal excitatory synaptic transmission.
Species:  Rat
Tissue:  CA1 pyramidal neurons.
References:  45
Inhibition of glutamatergic synaptic transmission.
Species:  Rat
Tissue:  Hypoglossal motoneurons.
References:  72
Presynaptic inhibition of 5-HT (autoreceptor function), GABA and glutamate release (heteroreceptor function).
Species:  Mouse
Tissue:  Dorsal raphe, ventral midbrain and nucleus accumbens.
References:  47
Presynaptic decrease in retinal input to the circadian system.
Species:  Mouse
Tissue:  in vivo (retinal axons in the suprachiasmatic nucleus).
References:  58
Antinociception.
Species:  Mouse
Tissue:  Ventrolateral periaqueductal gray.
References:  5
Regulation of aggressive behaviour.
Species:  Mouse
Tissue:  In vivo.
References:  66
Presynaptic inhibition of 5-HT release.
Species:  Mouse
Tissue:  in vivo (frontal cortex and ventral hippocampus).
References:  75
Presynaptic inhibition of acetylcholine release.
Species:  Rat
Tissue:  Hippocampus.
References:  40
Presynaptic inhibition of dopamine release.
Species:  Rat
Tissue:  In vivo.
References:  3
Physiological Consequences of Altering Gene Expression
5-HT1B receptor knockout mice exhibit altered decision making abilities and response inhibition.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  55
5-HT1B receptor knockout mice exhibit facilitated reference memory and impaired delay-dependent working memory.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  87
Juvenile 5-HT1B receptor knockout mice exhibit reduced anxiety and hyperactivity, reduced sensitivity to 5-HT1A receptor activity and reduced 5-HT1A receptor abundance in some brain regions.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  15
5-HT1B receptor knockout mice lack inhibition of 5-HT, GABA and glutamate release in the CNS.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  47
5-HT1B knockout mice exhibit a reduced effect of cocaine on the induction of the immediate-early gene c-fos, commonly used as a molecular marker for neuronal activation. Indicates that this receptor subtype is involved in mediating the stimulatory effects of cocaine.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  34
5-HT1B knockout mice exhibit increased aggressive behaviour.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  66
5-HT1B receptor knockout mice exhibit no inhibition of 5-HT release in the frontal cortex and ventral hippocampus.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  75
5-HT1B knockout mice exhibit altered monoamine metabolism in the CNS.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  3
5-HT1B receptor knockout mice exhibit elevated extracellular dopamine levels and dopamine release in the nucleus accumbens.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  71
Phenotypes, Alleles and Disease Models Mouse data from MGI

Show »

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Htr1btm1Rhn|Slc6a4tm1Kpl Htr1btm1Rhn/Htr1btm1Rhn,Slc6a4tm1Kpl/Slc6a4tm1Kpl
involves: 129S1/Sv * 129S2/SvPas * 129X1/SvJ * C57BL/6		 MGI:96274  MGI:96285  MP:0000285 abnormal heart valve morphology PMID: 16380550 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0003313 abnormal locomotor activation PMID: 12798274 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas * 129S6/SvEvTac		 MGI:96274  MP:0002803 abnormal operant conditional behavior PMID: 12742250 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0005006 abnormal osteoblast physiology PMID: 19041748 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0000057 abnormal osteogenesis PMID: 19041748 
Htr1b+|Htr1btm1Rhn Htr1btm1Rhn/Htr1b+
involves: 129S2/SvPas		 MGI:96274  MP:0000057 abnormal osteogenesis PMID: 19041748 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0001463 abnormal spatial learning PMID: 12798274 
Htr1btm1Rhn|Slc6a4tm1Kpl Htr1btm1Rhn/Htr1btm1Rhn,Slc6a4tm1Kpl/Slc6a4tm1Kpl
involves: 129S1/Sv * 129S2/SvPas * 129X1/SvJ * C57BL/6		 MGI:96274  MGI:96285  MP:0003141 cardiac fibrosis PMID: 16380550 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0001364 decreased anxiety-related response PMID: 10996411 
Htr1btm1Rhn|Slc6a4tm1Kpl Htr1btm1Rhn/Htr1btm1Rhn,Slc6a4tm1Kpl/Slc6a4tm1Kpl
involves: 129S1/Sv * 129S2/SvPas * 129X1/SvJ * C57BL/6		 MGI:96274  MGI:96285  MP:0005140 decreased cardiac muscle contractility PMID: 16380550 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0001489 decreased startle reflex PMID: 11164514 
Htr1btm1Rhn|Slc6a4tm1Kpl Htr1btm1Rhn/Htr1btm1Rhn,Slc6a4tm1Kpl/Slc6a4tm1Kpl
involves: 129S1/Sv * 129S2/SvPas * 129X1/SvJ * C57BL/6		 MGI:96274  MGI:96285  MP:0002795 dilated cardiomyopathy PMID: 16380550 
Htr1btm1Rhn|Slc6a4tm1Kpl Htr1btm1Rhn/Htr1btm1Rhn,Slc6a4tm1Kpl/Slc6a4tm1Kpl
involves: 129S1/Sv * 129S2/SvPas * 129X1/SvJ * C57BL/6		 MGI:96274  MGI:96285  MP:0003958 heart valve hyperplasia PMID: 16380550 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0001354 increased aggression towards males PMID: 8091214 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0001260 increased body weight PMID: 11164514  11790410 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0005605 increased bone mass PMID: 19041748 
Htr1b+|Htr1btm1Rhn Htr1btm1Rhn/Htr1b+
involves: 129S2/SvPas		 MGI:96274  MP:0005605 increased bone mass PMID: 19041748 
Htr1b+|Htr1btm1Rhn|Tg(Vil-cre)20Syr|Tph1+|Tph1tm1Kry Htr1btm1Rhn/Htr1b+,Tph1tm1Kry/Tph1+,Tg(Vil-cre)20Syr/0
involves: 129S2/SvPas * C57BL/6 * DBA/2		 MGI:3053809  MGI:96274  MGI:98796  MP:0005605 increased bone mass PMID: 19041748 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0003911 increased drinking behavior PMID: 11790410 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0004988 increased osteoblast cell number PMID: 19041748 
Htr1b+|Htr1btm1Rhn Htr1btm1Rhn/Htr1b+
involves: 129S2/SvPas		 MGI:96274  MP:0004988 increased osteoblast cell number PMID: 19041748 
Htr1btm1Rhn Htr1btm1Rhn/Htr1btm1Rhn
involves: 129S2/SvPas		 MGI:96274  MP:0001147 small testis PMID: 11790410 
Biologically Significant Variants
Type:  Single nucleotide polymorphism
Species:  Human
Description:  861 G -> C polymorphism of the HTR1B gene: 861G allele linked to the development of attention deficit hyperactivity disorder (ADHD).
References:  20,61
Type:  Single nucleotide polymorphism
Species:  Human
Description:  861 G -> C polymorphism: 861C allele linked to the development of alcohol-dependence.
References:  19
Type:  Single nucleotide polymorphism
Species:  Human
Description:  861 G -> C polymorphism: 861C allele linked with substance abuse disorder and major depression.
References:  23
Type:  Single nucleotide polymorphism
Species:  Human
Description:  861 G -> C polymorphism: 861G allele linked to antisocial personality and conduct disorder in alcoholics.
References:  73

References

Show »

1. Adham N, Romanienko P, Hartig P, Weinshank RL, Branchek T. (1992) The rat 5-hydroxytryptamine1B receptor is the species homologue of the human 5-hydroxytryptamine1D beta receptor. Mol Pharmacol, 41: 1-7. [PMID:1732716]

2. Ahern GP. (2011) 5-HT and the immune system. Curr Opin Pharmacol, 11 (1): 29-33. [PMID:21393060]

3. Ase AR, Reader TA, Hen R, Riad M, Descarries L. (2000) Altered serotonin and dopamine metabolism in the CNS of serotonin 5-HT(1A) or 5-HT(1B) receptor knockout mice. J Neurochem, 75: 2415-2426. [PMID:11080193]

4. Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A 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., 54 (9): 3206-21. [PMID:21486038]

5. Bartsch T, Knight YE, Goadsby PJ. (2004) Activation of 5-HT(1B/1D) receptor in the periaqueductal gray inhibits nociception. Ann Neurol, 56: 371-381. [PMID:15349864]

6. Belenky MA, Pickard GE. (2001) Subcellular distribution of 5-HT(1B) and 5-HT(7) receptors in the mouse suprachiasmatic nucleus. J Comp Neurol, 432: 371-388. [PMID:11246214]

7. Bonaventure P, Schotte A, Cras P, Leysen JE. (1997) Autoradiographic mapping of 5-HT1B- and 5-HT1D receptors in human brain using [3H]alniditan, a new radioligand. Recept. Channels, 5 (3-4): 225-30. [PMID:9606727]

8. Boulenguez P, Segu L, Chauveau J, Morel A, Lanoir J, Delaage M. (1992) Biochemical and pharmacological characterization of serotonin-O-carboxymethylglycyl[125I]iodotyrosinamide, a new radioiodinated probe for 5-HT1B and 5-HT1D binding sites. J. Neurochem., 58 (3): 951-9. [PMID:1738002]

9. Bruinvels AT, Palacios JM, Hoyer D. (1993) Autoradiographic characterisation and localisation of 5-HT1D compared to 5-HT1B binding sites in rat brain. Naunyn Schmiedebergs Arch. Pharmacol., 347 (6): 569-82. [PMID:8361548]

10. Buhot MC, Naili S. (1995) Changes in exploratory activity following stimulation of hippocampal 5-HT1A and 5-HT1B receptors in the rat. Hippocampus, 5: 198-208. [PMID:7550615]

11. Chadha A, Sur C, Atack J, Duty S. (2000) The 5HT(1B) receptor agonist, CP-93129, inhibits [(3)H]-GABA release from rat globus pallidus slices and reverses akinesia following intrapallidal injection in the reserpine-treated rat. Br J Pharmacol, 130: 1927-1932. [PMID:10952684]

12. Davidson C, Ho M, Price GW, Jones BJ, Stamford JA. (1997) (+)-WAY 100135, a partial agonist, at native and recombinant 5-HT1B/1D receptors. Br J Pharmacol, 121: 737-742. [PMID:9208142]

13. Dizeyi N, Bjartell A, Nilsson E, Hansson J, Gadaleanu V, Cross N, Abrahamsson PA. (2004) Expression of serotonin receptors and role of serotonin in human prostate cancer tissue and cell lines. Prostate, 59: 328-336. [PMID:15042609]

14. Domenech T, Beleta J, Palacios JM. (1997) Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol, 356: 328-334. [PMID:9303569]

15. El-Khodor BF, Dimmler MH, Amara DA, Hofer M, Hen R, Brunner D. (2004) Juvenile 5HT(1B) receptor knockout mice exhibit reduced pharmacological sensitivity to 5HT(1A) receptor activation. Int J Dev Neurosci, 22: 405-413. [PMID:15380839]

16. Gaster LM, Blaney FE, Davies S, Duckworth DM, Ham P, Jenkins S, Jennings AJ, Joiner GF, King FD, Mulholland KR, Wyman PA, Hagan JJ, Hatcher J, Jones BJ, Middlemiss DN, Price GW, Riley G, Roberts C, Routledge C, Selkirk J, Slade PD. (1998) The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J Med Chem, 41: 1218-1235. [PMID:9548813]

17. Granas C, Larhammar D. (1999) Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT(1B) receptor. Eur J Pharmacol, 380: 171-181. [PMID:10513577]

18. Hamblin MW, Metcalf MA, McGuffin RW, Karpells S.