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5-HT6 receptor

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Target id: 11

Nomenclature: 5-HT6 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 7 440 1p36.13 HTR6 5-hydroxytryptamine receptor 6 21
Mouse 7 440 4 70.57 cM Htr6 5-hydroxytryptamine (serotonin) receptor 6 20
Rat 7 436 5q36 Htr6 5-hydroxytryptamine receptor 6 28,38
Previous and Unofficial Names Click here for help
5-HT6 | serotonin receptor 6 | ST-B17 | 5-hydroxytryptamine (serotonin) receptor 6, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRdb 5ht6r_human (Hs), 5ht6r_mouse (Mm), 5ht6r_rat (Rn)
Other databases
Alphafold P50406 (Hs), Q9R1C8 (Mm), P31388 (Rn)
ChEMBL Target CHEMBL3371 (Hs), CHEMBL1075268 (Mm), CHEMBL3372 (Rn)
DrugBank Target P50406 (Hs)
Ensembl Gene ENSG00000158748 (Hs), ENSMUSG00000028747 (Mm), ENSRNOG00000049761 (Rn)
Entrez Gene 3362 (Hs), 15565 (Mm), 64354 (Rn)
Human Protein Atlas ENSG00000158748 (Hs)
KEGG Gene hsa:3362 (Hs), mmu:15565 (Mm), rno:64354 (Rn)
OMIM 601109 (Hs)
Pharos P50406 (Hs)
RefSeq Nucleotide NM_000871 (Hs), NM_021358 (Mm), NM_024365 (Rn)
RefSeq Protein NP_000862 (Hs), NP_067333 (Mm), NP_077341 (Rn)
UniProtKB P50406 (Hs), Q9R1C8 (Mm), P31388 (Rn)
Wikipedia HTR6 (Hs)
Natural/Endogenous Ligands Click here for help
5-hydroxytryptamine

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.7 pKd 4
⤷ pKd 8.7 (Kd 2x10-9 M) [4]
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Full agonist 8.6 – 8.7 pKd 5,25
⤷ pKd 8.6 – 8.7 [5,25]
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 Rn Full agonist 7.9 pKd 5
⤷ pKd 7.9 [5]
E6801 Small molecule or natural product Hs Partial agonist 8.7 pKi 17
⤷ pKi 8.7 (Ki 1.9x10-9 M) [17]
WAY-181187 Small molecule or natural product Hs Agonist 8.7 pKi 39
⤷ pKi 8.7 [39]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.4 pKi 7
⤷ pKi 8.4 [7]
WAY-208466 Small molecule or natural product Primary target of this compound Hs Agonist 8.3 pKi 3
⤷ pKi 8.3 (Ki 4.8x10-9 M) [3]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.0 – 8.6 pKi 4,7
⤷ pKi 8.0 – 8.6 [4,7]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.8 – 8.7 pKi 5,7
⤷ pKi 7.8 – 8.7 [5,7]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.0 – 8.1 pKi 4,7
⤷ pKi 8.0 – 8.1 [4,7]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.5 – 8.3 pKi 5-7,28
⤷ pKi 7.5 – 8.3 [5-7,28]
EMDT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 14
⤷ pKi 7.8 [14]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.0 – 8.6 pKi 5-7
⤷ pKi 7.0 – 8.6 [5-7]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 6.9 – 8.4 pKi 5-6,28
⤷ pKi 6.9 – 8.4 [5-6,28]
S 16924 Small molecule or natural product Rn Full agonist 7.6 pKi 27
⤷ pKi 7.6 [27]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.5 pKi 21
⤷ pKi 7.5 [21]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.5 pKi 6
⤷ pKi 7.5 [6]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Rn Full agonist 7.5 pKi 28
⤷ pKi 7.5 [28]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.4 pKi 21
⤷ pKi 7.4 [21]
lergotrile Small molecule or natural product Rn Full agonist 7.4 pKi 28
⤷ pKi 7.4 [28]
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 Rn Full agonist 6.6 – 7.9 pKi 5-7,28
⤷ pKi 6.6 – 7.9 [5-7,28]
dimethyltryptamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pKi 21
⤷ pKi 7.2 [21]
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 6.8 – 7.5 pKi 4,7,21
⤷ pKi 6.8 – 7.5 [4,7,21]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.0 pKi 28
⤷ pKi 7.0 [28]
5-MeO-DMT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.9 pKi 6
⤷ pKi 6.9 [6]
5-benzyloxytryptamine Small molecule or natural product Rn Full agonist 6.5 – 7.2 pKi 5-6,28
⤷ pKi 6.5 – 7.2 [5-6,28]
2-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.2 – 7.3 pKi 5
⤷ pKi 6.2 – 7.3 [5]
DM-1451 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.5 pKi 25
⤷ pKi 6.5 [25]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.4 pKi 21
⤷ pKi 6.4 [21]
TFMPP Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.3 pKi 28
⤷ pKi 6.3 [28]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 5.8 – 6.8 pKi 5,28
⤷ pKi 5.8 – 6.8 [5,28]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.2 pKi 21
⤷ pKi 6.2 [21]
OPC 4392 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.2 pKi 25
⤷ pKi 6.2 [25]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.1 pKi 21
⤷ pKi 6.1 [21]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 5.5 – 6.7 pKi 5-6,28
⤷ pKi 5.5 – 6.7 [5-6,28]
LY 165,163 Small molecule or natural product Rn Full agonist 6.1 pKi 28
⤷ pKi 6.1 [28]
CGS-12066 Small molecule or natural product Rn Full agonist 6.1 pKi 28
⤷ pKi 6.1 [28]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 5.9 pKi 34
⤷ pKi 5.9 [34]
xanomeline Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.9 pKi 42
⤷ pKi 5.9 [42]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.8 pKi 34
⤷ pKi 5.8 [34]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.6 pKi 29
⤷ pKi 5.6 [29]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.6 pKi 18
⤷ pKi 5.6 [18]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.6 pKi 28
⤷ pKi 5.6 [28]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.5 pKi 6
⤷ pKi 5.5 [6]
EMD-386088 Small molecule or natural product Primary target of this compound Hs Agonist 8.1 pIC50 26
⤷ pIC50 8.1 (IC50 7.4x10-9 M) [26]
[3H]5-CT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist - -
⤷
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]SB258585 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.0 pKd 16
⤷ pKd 9.0 (Kd 1x10-9 M) [16]
[3H]Ro 63-0563 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.3 pKd 7
⤷ pKd 8.3 (Kd 5x10-9 M) [7]
[11C]GSK215083 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.8 pKi 31
⤷ pKi 9.8 (Ki 1.6x10-10 M) [31]
intepirdine Small molecule or natural product Primary target of this compound Hs Antagonist 9.8 pKi 23
⤷ pKi 9.8 (Ki 1.7x10-10 M) [23]
Description: HeLa cell membrane assay, displacing [3H]LSD
idalopirdine Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.1 pKi 23
⤷ pKi 9.1 (Ki 8.3x10-10 M) [23]
SB399885 Small molecule or natural product Hs Antagonist 9.0 pKi 16
⤷ pKi 9.0 (Ki 1x10-9 M) [16]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.9 pKi 37
⤷ pKi 8.9 [37]
SB 271046 Small molecule or natural product Hs Antagonist 8.9 pKi 10
⤷ pKi 8.9 (Ki 1.26x10-9 M) [10]
cerlapirdine Small molecule or natural product Primary target of this compound Hs Antagonist 8.9 pKi 13
⤷ pKi 8.9 (Ki 1.3x10-9 M) [13]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 9.4 pKi 4,7,21
⤷ pKi 8.2 – 9.4 [4,7,21]
SB258585 Small molecule or natural product Hs Antagonist 8.5 pKi 15
⤷ pKi 8.5 [15]
SB357134 Small molecule or natural product Hs Antagonist 8.5 pKi 11
⤷ pKi 8.5 [11]
methiothepin Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.5 – 9.4 pKi 5-7,28
⤷ pKi 7.5 – 9.4 [5-7,28]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.4 pKi 37
⤷ pKi 8.4 [37]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.3 pKi 35
⤷ pKi 8.3 [35]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 8.2 pKi 37
⤷ pKi 8.2 [37]
Ro 63-0563 Small molecule or natural product Hs Antagonist 7.9 – 8.4 pKi 7,40
⤷ pKi 7.9 – 8.4 (Ki 1.26x10-8 – 3.98x10-9 M) [7,40]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.6 – 8.6 pKi 22,37
⤷ pKi 7.6 – 8.6 [22,37]
dihydroergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.9 – 8.3 pKi 6,28
⤷ pKi 7.9 – 8.3 [6,28]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 8.0 pKi 21,35
⤷ pKi 8.0 [21,35]
ICI 169369 Small molecule or natural product Hs Antagonist 8.0 pKi 21
⤷ pKi 8.0 [21]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.8 – 8.1 pKi 4,7,21,35
⤷ pKi 7.8 – 8.1 [4,7,21,35]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.5 – 8.4 pKi 5-7,22,27-28,37
⤷ pKi 7.5 – 8.4 [5-7,22,27-28,37]
Ro 63-0563 Small molecule or natural product Rn Antagonist 7.8 – 8.0 pKi 7,40
⤷ pKi 7.8 – 8.0 [7,40]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.5 – 8.2 pKi 28,37
⤷ pKi 7.5 – 8.2 [28,37]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.8 pKi 37
⤷ pKi 7.8 [37]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.8 pKi 37
⤷ pKi 7.8 [37]
2-bromo-LSD Small molecule or natural product Rn Antagonist 7.8 pKi 28
⤷ pKi 7.8 [28]
fluperlapine Small molecule or natural product Click here for species-specific activity table Rn Inverse agonist 7.8 pKi 37
⤷ pKi 7.8 [37]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 7.7 – 7.8 pKi 21,35
⤷ pKi 7.7 – 7.8 [21,35]
MPDT Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 14
⤷ pKi 7.7 [14]
bufotenine Small molecule or natural product Rn Antagonist 7.0 – 8.4 pKi 5
⤷ pKi 7.0 – 8.4 [5]
Ro 04-6790 Small molecule or natural product Hs Antagonist 7.3 – 7.9 pKi 7,40
⤷ pKi 7.3 – 7.9 [7,40]
loxapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.4 – 7.6 pKi 21,35
⤷ pKi 7.4 – 7.6 [21,35]
loxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.2 – 7.8 pKi 28,37
⤷ pKi 7.2 – 7.8 [28,37]
Ro 04-6790 Small molecule or natural product Rn Antagonist 7.4 – 7.6 pKi 7,40
⤷ pKi 7.4 – 7.6 [7,40]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.4 pKi 22
⤷ pKi 7.4 [22]
fluperlapine Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 7.3 – 7.5 pKi 21,35
⤷ pKi 7.3 – 7.5 [21,35]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.3 – 7.4 pKi 35
⤷ pKi 7.3 – 7.4 [35]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 pKi 21
⤷ pKi 7.3 [21]
α-ergocryptine Small molecule or natural product Rn Antagonist 7.3 pKi 6
⤷ pKi 7.3 [6]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.2 pKi 19
⤷ pKi 7.2 [19]
pimozide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.2 pKi 37
⤷ pKi 7.2 [37]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 – 7.4 pKi 4,7,21
⤷ pKi 7.0 – 7.4 [4,7,21]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.2 pKi 35
⤷ pKi 7.2 [35]
dihydroergocristine Small molecule or natural product Rn Antagonist 7.2 pKi 6
⤷ pKi 7.2 [6]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.5 – 7.8 pKi 5-7,28
⤷ pKi 6.5 – 7.8 [5-7,28]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.9 – 7.4 pKi 5,7,28
⤷ pKi 6.9 – 7.4 [5,7,28]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.9 – 7.3 pKi 4,7,21
⤷ pKi 6.9 – 7.3 [4,7,21]
tiospirone Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.1 pKi 37
⤷ pKi 7.1 [37]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.1 pKi 35
⤷ pKi 7.1 [35]
metergoline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.6 – 7.5 pKi 5-7,28
⤷ pKi 6.6 – 7.5 [5-7,28]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.9 – 7.2 pKi 4,7,21
⤷ pKi 6.9 – 7.2 [4,7,21]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 – 7.4 pKi 4,7,21
⤷ pKi 6.4 – 7.4 [4,7,21]
cyproheptadine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.9 pKi 28
⤷ pKi 6.9 [28]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.5 – 7.2 pKi 5,7,28
⤷ pKi 6.5 – 7.2 [5,7,28]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.8 pKi 25
⤷ pKi 6.8 [25]
cyproheptadine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.8 pKi 21
⤷ pKi 6.8 [21]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.5 – 6.8 pKi 4,7,21
⤷ pKi 6.5 – 6.8 [4,7,21]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.4 – 6.6 pKi 5-7,28
⤷ pKi 6.4 – 6.6 [5-7,28]
vortioxetine Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.5 pKi 1
⤷ pKi 6.5 (Ki 3.3x10-7 M) [1]
duloxetine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.4 pKi 12
⤷ pKi 6.4 [12]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 6.0 – 6.4 pKi 22,37
⤷ pKi 6.0 – 6.4 [22,37]
tiospirone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 21
⤷ pKi 6.0 [21]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 5.8 pKi 37
⤷ pKi 5.8 [37]
fluoxetine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 5.8 pKi 28
⤷ pKi 5.8 [28]
sumatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.6 pKi 21
⤷ pKi 5.6 [21]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.6 pKi 21
⤷ pKi 5.6 [21]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 – 5.7 pKi 4,7,21
⤷ pKi 5.4 – 5.7 [4,7,21]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.1 – 5.8 pKi 5,7,28
⤷ pKi 5.1 – 5.8 [5,7,28]
sumatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 5.2 pKi 6
⤷ pKi 5.2 [6]
View species-specific antagonist tables
Antagonist Comments
5-HT6 receptor antagonists have been developed as potential add-on, cognition-enhancing clinical candidate for Alzheimer's disease. However, none of these have yet shown efficacy in Phase 3 trials: Pfizer's PF-05212377 failed Phase 2 in October 2015, and Lundbeck reported failure of all of its Phase 3 trials of idalopirdine (2016/17). Axovant Science still has RVT-101 (intepirdine) in Phase 3 trial, with reporting expected in the second half of 2017.
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family Adenylyl cyclase stimulation
References:  45
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  45
Tissue Distribution Click here for help
Superior cervical ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  33
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  41
Brain: nucleus accumbens, olfactory tubercle, striatum, hippocampus, anterior corpus.
Species:  Rat
Technique:  in situ hybridisation.
References:  44
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 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:  45
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:  5,45
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:  20
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:  20
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:  38
Physiological Functions Click here for help
Role in spatial learning and memory.
Species:  Rat
Tissue:  In vivo.
References:  32,36,43
Modulation of acetlycholinergic neurotransmission.
Species:  Rat
Tissue:  In vivo.
References:  2,8-9,24
Modulation of dopaminergic neurotransmission.
Species:  Rat
Tissue:  In vivo.
References:  24
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
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 Click here for help
Type:  Splice variant
Species:  Human
Description:  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.
References:  30

References

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