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5-HT1B receptor

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Target id: 2

Nomenclature: 5-HT1B receptor

Family: 5-Hydroxytryptamine receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 390 6q14.1 HTR1B 5-hydroxytryptamine receptor 1B 19,19,25,47,57
Mouse 7 386 9 44.61 cM Htr1b 5-hydroxytryptamine (serotonin) receptor 1B 40
Rat 7 386 8q31 Htr1b 5-hydroxytryptamine receptor 1B 1,81
Previous and Unofficial Names Click here for help
5-HT1B | 5-HT1DB | HTR1D2 | 5-HT1B serotonin receptor | serotonin receptor 1B | 5-HT1Dβ [57,88] | 5-hydroxytryptamine (serotonin) receptor 1B, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRdb 5ht1b_human (Hs), 5ht1b_mouse (Mm), 5ht1b_rat (Rn)
Other databases
Alphafold P28222 (Hs), P28334 (Mm), P28564 (Rn)
ChEMBL Target CHEMBL1898 (Hs), CHEMBL3708691 (Mm), CHEMBL3459 (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)
Pharos P28222 (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 Click here for help
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:  82
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:  82
Natural/Endogenous Ligands Click here for help
5-HT-moduline
5-hydroxytryptamine
tryptamine
Comments: Endogenous ligand tryptamine is a weak agonist

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]N-methyl-AZ10419369 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Partial agonist 9.4 pKd 37
⤷ pKd 9.4 (Kd 3.7x10-10 M) [37]
[3H]8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.9 pKd 52
⤷ pKd 8.9 [52]
[125I]GTI Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Agonist 8.9 pKd 9-10
⤷ pKd 8.9 (Kd 1.3x10-9 M) [9-10]
[3H]alniditan Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.6 – 9.0 pKd 32
⤷ pKd 8.6 – 9.0 (Kd 2.51x10-9 – 1x10-9 M) [32]
[3H]eletriptan Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Partial agonist 8.5 pKd 50
⤷ pKd 8.5 (Kd 3x10-9 M) [50]
[3H]sumatriptan Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Partial agonist 8.0 pKd 50
⤷ pKd 8.0 (Kd 1.1x10-8 M) [50]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.5 – 8.4 pKd 55,88
⤷ pKd 7.5 – 8.4 [55,88]
donitriptan Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 9.7 pKi 26
⤷ pKi 9.7 [26]
oxymetazoline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.5 pKi 30
⤷ pKi 9.5 [30]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 9.0 – 9.8 pKi 17,28,61,70,87
⤷ pKi 9.0 – 9.8 [17,28,61,70,87]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.4 pKi 26
⤷ pKi 9.4 [26]
L-694,247 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.2 pKi 18
⤷ pKi 9.2 (Ki 6.3x10-10 M) [18]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 9.0 pKi 61
⤷ pKi 9.0 [61]
alniditan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.8 – 9.0 pKi 33
⤷ pKi 8.8 – 9.0 [33]
7-methoxy-1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.7 pKi 28
⤷ pKi 8.7 [28]
CP94253 Small molecule or natural product Hs Full agonist 8.7 pKi 29
⤷ pKi 8.7 (Ki 2x10-9 M) [29]
dihydroergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.0 – 9.2 pKi 33,55
⤷ pKi 8.0 – 9.2 [33,55]
CGS-12066 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.1 – 8.7 pKi 18,88
⤷ pKi 8.1 – 8.7 [18,88]
ziprasidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.3 pKi 69
⤷ pKi 8.3 [69]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.7 – 8.8 pKi 55,88
⤷ pKi 7.7 – 8.8 [55,88]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 7.4 – 9.0 pKi 13,51-52,70,87-88
⤷ pKi 7.4 – 9.0 [13,51-52,70,87-88]
5-(nonyloxy)-tryptamine Small molecule or natural product Hs Full agonist 8.2 pKi 18
⤷ pKi 8.2 [18]
lysergol Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 – 8.9 pKi 55,88
⤷ pKi 7.5 – 8.9 [55,88]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Full agonist 8.1 pKi 40
⤷ pKi 8.1 [40]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Mm Full agonist 8.1 pKi 40
⤷ pKi 8.1 [40]
asenapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.1 pKi 69
⤷ pKi 8.1 [69]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.1 pKi 40
⤷ pKi 8.1 [40]
naratriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 8.1 pKi 50
⤷ pKi 8.1 [50]
eletriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 8.0 pKi 50
⤷ pKi 8.0 (Ki 1x10-8 M) [50]
frovatriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Agonist 8.0 pKi 91
⤷ pKi 8.0 (Ki 1.03x10-8 M) [91]
BMS 181,101 Small molecule or natural product Hs Partial agonist 7.6 – 8.1 pKi 51
⤷ pKi 7.6 – 8.1 [51]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.7 – 7.9 pKi 28,55,88
⤷ pKi 7.7 – 7.9 [28,55,88]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.7 pKi 44
⤷ pKi 7.7 [44]
zolmitriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 7.7 pKi 50
⤷ pKi 7.7 [50]
avitriptan Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.7 pKi 68
⤷ pKi 7.7 (Ki 2.09x10-8 M) [68]
vortioxetine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Partial agonist 7.5 pKi 4
⤷ pKi 7.5 (Ki 3.3x10-8 M) [4]
avitriptan Small molecule or natural product Click here for species-specific activity table Rn Agonist 7.4 pKi 68
⤷ pKi 7.4 (Ki 3.63x10-8 M) [68]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.3 – 7.5 pKi 55,88
⤷ pKi 7.3 – 7.5 [55,88]
dipropyl-5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 88
⤷ pKi 7.4 [88]
sumatriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 6.5 – 8.1 pKi 18,33,45,50-51,55,88
⤷ pKi 6.5 – 8.1 (Ki 3.16x10-7 – 7.94x10-9 M) [18,33,45,50-51,55,88]
xanomeline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.3 pKi 85
⤷ pKi 7.3 [85]
rizatriptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 6.9 pKi 50
⤷ pKi 6.9 [50]
L-775,606 Small molecule or natural product Hs Partial agonist 6.3 – 6.9 pKi 51
⤷ pKi 6.3 – 6.9 [51]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.6 pKi 44
⤷ pKi 6.6 [44]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 6.6 pKi 44
⤷ pKi 6.6 [44]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.2 – 6.9 pKi 55,88
⤷ pKi 6.2 – 6.9 [55,88]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 6.5 pKi 44
⤷ pKi 6.5 [44]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.3 pKi 58
⤷ pKi 6.3 [58]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.3 pKi 44
⤷ pKi 6.3 [44]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.3 pKi 69
⤷ pKi 6.3 [69]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 6.3 pKi 88
⤷ pKi 6.3 [88]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.2 pKi 69
⤷ pKi 6.2 [69]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 6.1 pKi 61
⤷ pKi 6.1 [61]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.1 pKi 72
⤷ pKi 6.1 [72]
2-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.1 pKi 88
⤷ pKi 6.1 [88]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.8 – 6.0 pKi 44,52
⤷ pKi 5.8 – 6.0 [44,52]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.3 pKi 49
⤷ pKi 5.3 [49]
almotriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist 7.9 pIC50 8
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [8]
Description: Affinity of almotriptan at recombinant h5-HT1B receptors expressed in HeLa cells, determined in a radioligand displacement assay using [125I]GTI as tracer.
CP-122288 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.6 pIC50 15
⤷ pIC50 7.6 [15]
L-772,405 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.8 pIC50 65
⤷ pIC50 6.8 [65]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.2 pIC50 15
⤷ pIC50 6.2 [15]
[11C]AZ10419369 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Partial agonist - - 80
⤷ [80]
View species-specific agonist tables
Agonist Comments
Frovatriptan is selective for 1B and 1D 5-HT receptor subtypes compared to the 1A subtype [91].
BRL-15572 can be used to distinguish between 5-HT1D and 5-HT1B receptors, being approximately 60-fold selective for the 1D subtype [61].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GR-55562 Small molecule or natural product Hs Antagonist 7.4 pKB 23
⤷ pKB 7.4 [23]
[3H]GR 125,743 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 8.6 – 9.2 pKd 18,90
⤷ pKd 8.6 – 9.2 (Kd 2.6x10-9 – 7.1x10-10 M) [18,90]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.2 pKi 18
⤷ pKi 9.2 [18]
5-OH-DPAT Small molecule or natural product Mm Antagonist 8.4 pKi 40
⤷ pKi 8.4 [40]
SB 224289 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.2 – 8.6 pKi 17,51,70
⤷ pKi 8.2 – 8.6 (Ki 6.31x10-9 – 2.51x10-9 M) [17,51,70]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 8.3 pKi 40
⤷ pKi 8.3 [40]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 8.3 pKi 40
⤷ pKi 8.3 [40]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Mm Antagonist 8.3 pKi 40
⤷ pKi 8.3 [40]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Mm Antagonist 8.3 pKi 40
⤷ pKi 8.3 [40]
SB236057 Small molecule or natural product Hs Inverse agonist 8.2 pKi 42
⤷ pKi 8.2 (Ki 6.31x10-9 M) [42]
SB 272183 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.1 pKi 86
⤷ pKi 8.1 [86]
(-)-pindolol Small molecule or natural product Mm Antagonist 8.1 pKi 40
⤷ pKi 8.1 [40]
cyanopindolol Small molecule or natural product Mm Antagonist 8.1 pKi 40
⤷ pKi 8.1 [40]
SB 649915 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 pKi 84
⤷ pKi 8.0 [84]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 7.1 – 8.5 pKi 18,51,55,87
⤷ pKi 7.1 – 8.5 [18,51,55,87]
GR-55562 Small molecule or natural product Hs Antagonist 7.5 pKi 18
⤷ pKi 7.5 [18]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.8 – 7.6 pKi 45,88
⤷ pKi 6.8 – 7.6 [45,88]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.2 pKi 69
⤷ pKi 7.2 [69]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.2 pKi 55
⤷ pKi 7.2 [55]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.6 – 7.6 pKi 55,88
⤷ pKi 6.6 – 7.6 [55,88]
sertindole Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 pKi 69
⤷ pKi 7.0 [69]
risperidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.6 – 7.3 pKi 32,69,71
⤷ pKi 6.6 – 7.3 [32,69,71]
rauwolscine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 – 7.4 pKi 55,88
⤷ pKi 6.5 – 7.4 [55,88]
9-OH-risperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 69
⤷ pKi 6.8 [69]
SB 714786 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pKi 84
⤷ pKi 6.7 [84]
(S)-flurocarazolol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 63
⤷ pKi 6.5 [63]
pipamperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 69
⤷ pKi 6.2 [69]
(R)-flurocarazolol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 pKi 63
⤷ pKi 6.1 [63]
S33084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 pKi 43
⤷ pKi 6.1 [43]
(+)-WAY 100135 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.8 pKi 13
⤷ pKi 5.8 [13]
ocaperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.9 – 7.2 pIC50 32
⤷ pIC50 6.9 – 7.2 [32]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.0 – 6.5 pIC50 15,32
⤷ pIC50 6.0 – 6.5 [15,32]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.2 – 5.4 pIC50 15,32
⤷ pIC50 5.2 – 5.4 [15,32]
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 [37].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
5-HT-moduline Peptide Click here for species-specific activity table Ligand is endogenous in the given species Hs Negative 11.9 pIC50 64
⤷ pIC50 11.9 [64]
Immunopharmacology Comments
The expression of 5-HT1B receptors on immune cells indicates that it plays some part in immune/inflammatory responses [83].
Cell Type Associations
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   mature eosinophil (CL:0000041)
Comment:  Expressed by eosinophils.
References:  83
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
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
References:  34,92
Tissue Distribution Click here for help
Benign and malignant prostate tissue.
Species:  Human
Technique:  Western blotting.
References:  14
Brain: substantia nigra, globus pallidus > striatum > amygdala, hippocampus, septa region, hypothalamus.
Species:  Human
Technique:  Radioligand binding.
References:  78
Trigeminal ganglion.
Species:  Human
Technique:  immunocytochemistry.
References:  22
Cortical cerebral arteries (smooth muscle cell layer > endothelial cell layer).
Species:  Human
Technique:  immunocytochemistry.
References:  53
Coronary artery > atrium > ventricle, epicardium.
Species:  Human
Technique:  RT-PCR.
References:  54
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:  79
Suprachiasmatic nucleus.
Species:  Mouse
Technique:  Electron microscopic immunocytochemistry.
References:  6,59
Hypothalamus: magnocellular nuclei > supraoptic nucleus, paraventricular nucleus (dorsolateral) and accessory perifornical, circular and retrochiasmatic nuclei.
Species:  Rat
Technique:  Immunohistochemistry.
References:  38
Lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  60
Suprachiasmatic nucleus.
Species:  Rat
Technique:  Radioligand binding.
References:  39
Trigeminal ganglion.
Species:  Rat
Technique:  Immunohistochemistry.
References:  36
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  76
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:  66
Expression Datasets Click here for help

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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]

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Functional Assays Click here for help
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:  57
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:  40
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:  88
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:  57
Physiological Functions Click here for help
Vasoconstriction.
Species:  Human
Tissue:  Coronary artery.
References:  54
Vasocontriction.
Species:  Human
Tissue:  Cortical cerebral artery.
References:  53
Mediation of impulsivity and prefrontal cortex-dependent learning and memory.
Species:  Mouse
Tissue:  In vivo.
References:  56
Regulation of hippocampal functions.
Species:  Rat
Tissue:  In vivo.
References:  11
Inhibition of food intake.
Species:  Rat
Tissue:  In vivo.
References:  31
Presynaptic inhibition of GABA release onto GABAB receptors but not GABAA.
Species:  Rat
Tissue:  Dopamine-containing neurons of the midbrain.
References:  27
Inhibition of GABA release.
Species:  Rat
Tissue:  Globus pallidus.
References:  12
Relief from akinesia.
Species:  Rat
Tissue:  In vivo.
References:  12
Lowering of hippocampal excitatory synaptic transmission.
Species:  Rat
Tissue:  CA1 pyramidal neurons.
References:  46
Inhibition of glutamatergic synaptic transmission.
Species:  Rat
Tissue:  Hypoglossal motoneurons.
References:  74
Presynaptic inhibition of 5-HT (autoreceptor function), GABA and glutamate release (heteroreceptor function).
Species:  Mouse
Tissue:  Dorsal raphe, ventral midbrain and nucleus accumbens.
References:  48
Presynaptic decrease in retinal input to the circadian system.
Species:  Mouse
Tissue:  in vivo (retinal axons in the suprachiasmatic nucleus).
References:  59
Antinociception.
Species:  Mouse
Tissue:  Ventrolateral periaqueductal gray.
References:  5
Regulation of aggressive behaviour.
Species:  Mouse
Tissue:  In vivo.
References:  67
Presynaptic inhibition of 5-HT release.
Species:  Mouse
Tissue:  in vivo (frontal cortex and ventral hippocampus).
References:  77
Presynaptic inhibition of acetylcholine release.
Species:  Rat
Tissue:  Hippocampus.
References:  41
Presynaptic inhibition of dopamine release.
Species:  Rat
Tissue:  In vivo.
References:  3
Physiological Consequences of Altering Gene Expression Click here for help
5-HT1B receptor knockout mice exhibit altered decision making abilities and response inhibition.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  56
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:  89
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:  16
5-HT1B receptor knockout mice lack inhibition of 5-HT, GABA and glutamate release in the CNS.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  48
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:  35
5-HT1B knockout mice exhibit increased aggressive behaviour.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  67
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:  77
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:  73
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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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 Click here for help
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:  21,62
Type:  Single nucleotide polymorphism
Species:  Human
Description:  861 G -> C polymorphism: 861C allele linked to the development of alcohol-dependence.
References:  20
Type:  Single nucleotide polymorphism
Species:  Human
Description:  861 G -> C polymorphism: 861C allele linked with substance abuse disorder and major depression.
References:  24
Type:  Single nucleotide polymorphism
Species:  Human
Description:  861 G -> C polymorphism: 861G allele linked to antisocial personality and conduct disorder in alcoholics.
References:  75

References

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