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5-HT6 receptor

Family: 5-Hydroxytryptamine receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Phenotypes, Alleles and Disease Models
Biologically Significant Variants
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 440 1p36-p35 HTR6 5-hydroxytryptamine (serotonin) receptor 6, G protein-coupled 17
Mouse 7 440 4 D3 Htr6 5-hydroxytryptamine (serotonin) receptor 6 16
Rat 7 436 5 Htr6 5-hydroxytryptamine (serotonin) receptor 6, G protein-coupled 22,31
Previous and Unofficial Names
5-HT6
5-HT6R
5-hydroxytryptamine (serotonin) receptor 6
5-HT-6
5-hydroxytryptamine receptor 6
ST-B17
serotonin receptor 6
Database Links
ChEMBL Target 10627 (Hs), 10628 (Rn)
DrugBank Target 1256 (Hs)
Ensembl ENSG00000158748 (Hs), ENSMUSG00000028747 (Mm)
Entrez Gene 3362 (Hs), 15565 (Mm), 64354 (Rn)
GeneCards HTR6 (Hs)
GenitoUrinary Development Molecular Anatomy Project Htr6 (Mm)
HomoloGene 673 (Hs)
Human Protein Reference Database 03066 (Hs)
InterPro P50406 (Hs), Q9R1C8 (Mm), P31388 (Rn)
KEGG Gene hsa:3362 (Hs), mmu:15565 (Mm), rno:64354 (Rn)
OMIM 601109 (Hs)
PharmGKB Gene PA29560 (Hs)
PhosphoSitePlus P50406 (Hs), Q9R1C8 (Mm), P31388 (Rn)
Protein Ontology (PRO) PRO:000001102 (Hs)
RefSeq Nucleotide NM_000871 (Hs), NM_021358 (Mm), NM_024365 (Rn)
RefSeq Protein NP_000862 (Hs), NP_067333 (Mm), NP_077341 (Rn)
TreeFam ENSG00000158748 (Hs), ENSMUSG00000028747 (Mm)
UniGene Hs. 22180 (Hs)
UniProt P50406 (Hs), Q9R1C8 (Mm), P31388 (Rn)
Wikipedia 5-HT6 receptor
5-Hydroxytryptamine receptors
Search for 3D structures on the PDB
Search by keyword: 5-Hydroxytryptamine receptors 5-HT6 receptor Search by accession number: P31388, P50406, Q9R1C8
Natural/Endogenous Ligand(s)
5-HT
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]LSD Hs Full agonist 8.7 pKd 4
[3H]LSD Rn Full agonist 8.6 – 8.7 pKd 3,20
5-HT Rn Full agonist 7.9 pKd 3
E-6801 Hs Partial agonist 8.7 pKi 13
WAY-181187 Hs Agonist 8.7 pKi 32
LSD Hs Full agonist 8.4 pKi 5
ergotamine Hs Full agonist 8.0 – 8.6 pKi 4-5
LSD Rn Full agonist 7.8 – 8.7 pKi 3,5
lisuride Hs Partial agonist 8.0 – 8.1 pKi 4-5
lisuride Rn Partial agonist 7.5 – 8.3 pKi 2-3,5,22
EMDT Hs Full agonist 7.8 pKi 11
ergotamine Rn Full agonist 7.0 – 8.6 pKi 2-3,5
5-MeOT Rn Full agonist 6.9 – 8.4 pKi 2-3,22
S 16924 Rn Full agonist 7.6 pKi 21
bromocriptine Hs Full agonist 7.5 pKi 17
bromocriptine Rn Partial agonist 7.5 pKi 2
pergolide Rn Full agonist 7.5 pKi 22
5-MeOT Hs Full agonist 7.4 pKi 17
lergotrile Rn Full agonist 7.4 pKi 22
5-HT Rn Full agonist 6.6 – 7.9 pKi 2-3,5,22
dimethyltryptamine Hs Full agonist 7.2 pKi 17
5-HT Hs Full agonist 6.8 – 7.5 pKi 4-5,17
1-naphthylpiperazine Rn Full agonist 7.0 pKi 22
5-MeO-DMT Rn Full agonist 6.9 pKi 2
5-benzyloxytryptamine Rn Full agonist 6.5 – 7.2 pKi 2-3,22
aripiprazole Rn Full agonist 6.8 pKi 20
2-methyl-5-HT Rn Full agonist 6.2 – 7.3 pKi 3
DM 1451 Rn Full agonist 6.5 pKi 20
TFMPP Hs Full agonist 6.4 pKi 17
TFMPP Rn Full agonist 6.3 pKi 22
tryptamine Rn Full agonist 5.8 – 6.8 pKi 3,22
OPC 4392 Rn Full agonist 6.2 pKi 20
RU 24969 Hs Full agonist 6.2 pKi 17
5-CT Rn Full agonist 5.5 – 6.7 pKi 2-3,22
5-CT Hs Full agonist 6.1 pKi 17
CGS-12066 Rn Full agonist 6.1 pKi 22
LY 165,163 Rn Full agonist 6.1 pKi 22
BRL-15572 Hs Partial agonist 5.9 pKi 27
xanomeline Hs Full agonist 5.9 pKi 35
GR-127935 Hs Partial agonist 5.8 pKi 27
donitriptan Hs Partial agonist 5.6 pKi 14
m-CPP Rn Full agonist 5.6 pKi 22
SL65.0155 Hs Partial agonist 5.6 pKi 23
α-methyl-5-HT Rn Full agonist 5.5 pKi 2
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]Ro 63-0563 Hs Antagonist 8.3 pKd 5
SB399885 Hs Antagonist 9.0 pKi 12
SB 271046 Hs Antagonist 8.9 pKi 8
zotepine Rn Inverse agonist 8.9 pKi 30
methiothepin Hs Antagonist 8.2 – 9.4 pKi 4-5,17
SB357134 Hs Antagonist 8.5 pKi 9
methiothepin Rn Antagonist 7.5 – 9.4 pKi 2-3,5,22
chlorpromazine Rn Inverse agonist 8.4 pKi 30
zotepine Hs Inverse agonist 8.3 pKi 28
thioridazine Rn Inverse agonist 8.2 pKi 30
Ro 63-0563 Hs Antagonist 7.9 – 8.4 pKi 5,33
dihydroergotamine Rn Antagonist 7.9 – 8.3 pKi 2,22
olanzapine Rn Inverse agonist 7.6 – 8.6 pKi 18,30
ICI 169369 Hs Antagonist 8.0 pKi 17
olanzapine Hs Inverse agonist 8.0 pKi 17,28
clozapine Hs Inverse agonist 7.8 – 8.1 pKi 4-5,17,28
clozapine Rn Inverse agonist 7.5 – 8.4 pKi 2-3,5,18,21-22,30
Ro 63-0563 Rn Antagonist 7.8 – 8.0 pKi 5,33
amoxapine Rn Antagonist 7.5 – 8.2 pKi 22,30
2-Br-LSD Rn Antagonist 7.8 pKi 22
fluperlapine Rn Inverse agonist 7.8 pKi 30
fluphenazine Rn Inverse agonist 7.8 pKi 30
perphenazine Rn Inverse agonist 7.8 pKi 30
chlorpromazine Hs Inverse agonist 7.7 – 7.8 pKi 17,28
bufotenine Rn Antagonist 7.0 – 8.4 pKi 3
MPDT Hs Antagonist 7.7 pKi 11
Ro 04-6790 Hs Antagonist 7.3 – 7.9 pKi 5,33
loxapine Hs Inverse agonist 7.4 – 7.6 pKi 17,28
loxapine Rn Inverse agonist 7.2 – 7.8 pKi 22,30
Ro 04-6790 Rn Antagonist 7.4 – 7.6 pKi 5,33
fluperlapine Hs Inverse agonist 7.3 – 7.5 pKi 17,28
iloperidone Rn Antagonist 7.4 pKi 18
fluphenazine Hs Inverse agonist 7.3 – 7.4 pKi 28
α-ergocryptine Rn Antagonist 7.3 pKi 2
amoxapine Hs Antagonist 7.3 pKi 17
dihydroergocristine Rn Antagonist 7.2 pKi 2
iloperidone Hs Antagonist 7.2 pKi 15
pimozide Rn Antagonist 7.2 pKi 30
ritanserin Hs Antagonist 7.0 – 7.4 pKi 4-5,17
thioridazine Hs Inverse agonist 7.2 pKi 28
mianserin Rn Antagonist 6.9 – 7.4 pKi 3,5,22
ritanserin Rn Antagonist 6.5 – 7.8 pKi 2-3,5,22
mianserin Hs Antagonist 6.9 – 7.3 pKi 4-5,17
perphenazine Hs Inverse agonist 7.1 pKi 28
tiospirone Rn Antagonist 7.1 pKi 30
amitriptyline Hs Antagonist 6.9 – 7.2 pKi 4-5,17
metergoline Rn Antagonist 6.6 – 7.5 pKi 2-3,5,22
cyproheptadine Rn Antagonist 6.9 pKi 22
metergoline Hs Antagonist 6.4 – 7.4 pKi 4-5,17
amitriptyline Rn Antagonist 6.5 – 7.2 pKi 3,5,22
cyproheptadine Hs Antagonist 6.8 pKi 17
methysergide Hs Antagonist 6.5 – 6.8 pKi 4-5,17
methysergide Rn Antagonist 6.4 – 6.6 pKi 2-3,5,22
duloxetine Hs Antagonist 6.4 pKi 10
risperidone Rn Inverse agonist 6.0 – 6.4 pKi 18,30
tiospirone Hs Antagonist 6.0 pKi 17
fluoxetine Rn Antagonist 5.8 pKi 22
spiperone Rn Antagonist 5.8 pKi 30
risperidone Hs Antagonist 5.6 pKi 17
sumatriptan Hs Antagonist 5.6 pKi 17
mesulergine Hs Antagonist 5.4 – 5.7 pKi 4-5,17
mesulergine Rn Antagonist 5.1 – 5.8 pKi 3,5,22
sumatriptan Rn Antagonist 5.2 pKi 2
View species-specific antagonist tables

Explore drug-target interactions for this set of compounds using iPHACE

Primary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  38
Secondary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  38
Tissue Distribution
Superior cervical ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  26
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  34
Brain: nucleus accumbens, olfactory tubercle, striatum, hippocampus, anterior corpus.
Species:  Rat
Technique:  in situ hybridisation.
References:  37
Expression Datasets

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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
Measurement of intracellular Ca2+ levels in HEK 293 cells transfected with the human 5-HT6 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in intracellular Ca2+ levels.
References:  38
Measurement of cAMP levels in HEK 293 cells transfected with the human 5-HT6 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Stimulation of cAMP accumulation.
References:  3,38
Measurement of cAMP levels in JEG-3 cells transfected with the 5-HT6 receptor and using a cAMP response element (CRE)-coupled luciferase construct as the reporter.
Species:  Mouse
Tissue:  JEG-3 cells.
Response measured:  Increase in basal cAMP levels and cAMP accumulation.
References:  16
Measurement of cAMP levels in JEG-3 cells transfected with the 5-HT6 receptor and using a cAMP response element (CRE)-coupled luciferase construct as the reporter.
Species:  Mouse
Tissue:  COS-7 cells.
Response measured:  Increase in basal cAMP levels and cAMP accumulation.
References:  16
Measurement of cAMP levels in COS-7 cells transfected with the rat 5-HT6 receptor.
Species:  Rat
Tissue:  COS-7 cells.
Response measured:  Stimulation of cAMP accumulation.
References:  31
Physiological Functions
Role in spatial learning and memory.
Species:  Rat
Tissue:  In vivo.
References:  25,29,36
Modulation of acetlycholinergic neurotransmission.
Species:  Rat
Tissue:  In vivo.
References:  1,6-7,19
Modulation of dopaminergic neurotransmission.
Species:  Rat
Tissue:  In vivo.
References:  19
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Htr6tm1Arte Htr6tm1Arte/Htr6tm1Arte
involves: C57BL/6		 MGI:1196627  MP:0008961 abnormal basal metabolism PMID: 18755168 
Htr6tm1Lex Htr6tm1Lex/Htr6tm1Lex
involves: 129S5/SvEvBrd * C57BL/6J		 MGI:1196627  MP:0001258 decreased body length
Htr6tm1Lex Htr6tm1Lex/Htr6tm1Lex
involves: 129S5/SvEvBrd * C57BL/6J		 MGI:1196627  MP:0001262 decreased body weight
Htr6tm1Arte Htr6tm1Arte/Htr6tm1Arte
involves: C57BL/6		 MGI:1196627  MP:0001262 decreased body weight PMID: 18755168 
Htr6tm1Arte Htr6tm1Arte/Htr6tm1Arte
involves: C57BL/6		 MGI:1196627  MP:0003910 decreased eating behavior PMID: 18755168 
Htr6tm1Arte Htr6tm1Arte/Htr6tm1Arte
involves: C57BL/6		 MGI:1196627  MP:0010025 decreased total body fat amount PMID: 18755168 
Htr6tm1Tct Htr6tm1Tct/Htr6tm1Tct
involves: 129X1/SvJ * C57BL/6J		 MGI:1196627  MP:0002629 hyperactivity elicited by ethanol administration PMID: 16452990 
Htr6tm1Tct Htr6tm1Tct/Htr6tm1Tct
involves: 129X1/SvJ * C57BL/6J		 MGI:1196627  MP:0009755 impaired behavioral response to alcohol PMID: 16452990 
Biologically Significant Variants
A truncated, nonfunctional 5-HT6 receptor with a 289 bp deletion of the region coding for transmembrane IV and third intracellular loop has been identified in the caudate and substantia nigra of the human brain.
Type:  Splice variant.
Species:  Human
References:  24

REFERENCES

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1. Bentley, J. C., Bourson, A., Boess, F. G., Fone, K. C., Marsden, C. A., Petit, N. and Sleight, A. J. (1999) Investigation of stretching behaviour induced by the selective 5-HT6 receptor antagonist, Ro 04-6790, in rats. Br J Pharmacol, 126: 1537-1542. [PMID:10323584]

2. Boess, F. G., Monsma, F. J. and Sleight, A. J. (1998) Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor. J Neurochem, 71: 2169-2177. [PMID:9798944]

3. Boess, F. G., Monsma, F. J., Carolo, C., Meyer, V., Rudler, A., Zwingelstein, C. and Sleight, A. J. (1997) Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells. Neuropharmacology, 36: 713-720. [PMID:9225298]

4. Boess, F. G., Monsma, F. J., Meyer, V., Zwingelstein, C. and Sleight, A. J. (1997) Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor. Mol Pharmacol, 52: 515-523. [PMID:9284367]

5. Boess, F. G., Riemer, C., Bos, M., Bentley, J., Bourson, A. and Sleight, A. J. (1998) The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum. Mol Pharmacol, 54: 577-583. [PMID:9730917]

6. Bourson, A., Boess, F. G., Bos, M. and Sleight, A. J. (1998) Involvement of 5-HT6 receptors in nigro-striatal function in rodents. Br J Pharmacol, 125: 1562-1566. [PMID:9884085]

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To cite this database page, please use the following:

Rodrigo Andrade, Nicholas M. Barnes, Gordon Baxter, Joel Bockaert, Theresa Branchek, Marlene L. Cohen, Aline Dumuis, Richard M. Eglen, Manfred Göthert, Mark Hamblin, Michel Hamon, Paul R. Hartig, René Hen, Katharine Herrick-Davis, Rebecca Hills, Daniel Hoyer, Patrick P. A. Humphrey, Klaus Peter Latté, Luc Maroteaux, Graeme R. Martin, Derek N. Middlemiss, Ewan Mylecharane, Stephen J. Peroutka, Pramod R. Saxena, Andrew Sleight, Carlos M. Villalon, Frank Yocca.
5-Hydroxytryptamine receptors: 5-HT6 receptor. Last modified on 12/02/2013. Accessed on 23/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=11.


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