5-HT<sub>6</sub> receptor | 5-Hydroxytryptamine receptors

5-HT₆ receptor

Target not currently curated in GtoImmuPdb

Target id: 11

Nomenclature: 5-HT₆ receptor

Family: 5-Hydroxytryptamine receptors

Gene and Protein Information
Previous and Unofficial Names
Database Links
Natural/Endogenous Ligands
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Phenotypes, Alleles and Disease Models
Biologically Significant Variants
References
Contributors
How to cite this page

Gene and Protein Information
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
5-HT6 \| serotonin receptor 6 \| ST-B17 \| 5-hydroxytryptamine (serotonin) receptor 6, G protein-coupled

Previous and Unofficial Names

5-HT6 | serotonin receptor 6 | ST-B17 | 5-hydroxytryptamine (serotonin) receptor 6, G protein-coupled

Database Links
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
5-hydroxytryptamine

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]LSD		Hs	Full agonist	8.7	pK_d	4
⤷	pK_d 8.7 (K_d 2x10^-9 M) [4]
[³H]LSD		Rn	Full agonist	8.6 – 8.7	pK_d	5,25
⤷	pK_d 8.6 – 8.7 [5,25]
5-hydroxytryptamine		Rn	Full agonist	7.9	pK_d	5
⤷	pK_d 7.9 [5]
E6801		Hs	Partial agonist	8.7	pK_i	17
⤷	pK_i 8.7 (K_i 1.9x10^-9 M) [17]
WAY-181187		Hs	Agonist	8.7	pK_i	39
⤷	pK_i 8.7 [39]
Lysergide		Hs	Full agonist	8.4	pK_i	7
⤷	pK_i 8.4 [7]
WAY-208466		Hs	Agonist	8.3	pK_i	3
⤷	pK_i 8.3 (K_i 4.8x10^-9 M) [3]
ergotamine		Hs	Full agonist	8.0 – 8.6	pK_i	4,7
⤷	pK_i 8.0 – 8.6 [4,7]
Lysergide		Rn	Full agonist	7.8 – 8.7	pK_i	5,7
⤷	pK_i 7.8 – 8.7 [5,7]
lisuride		Hs	Partial agonist	8.0 – 8.1	pK_i	4,7
⤷	pK_i 8.0 – 8.1 [4,7]
lisuride		Rn	Partial agonist	7.5 – 8.3	pK_i	5-7,28
⤷	pK_i 7.5 – 8.3 [5-7,28]
EMDT		Hs	Full agonist	7.8	pK_i	14
⤷	pK_i 7.8 [14]
ergotamine		Rn	Full agonist	7.0 – 8.6	pK_i	5-7
⤷	pK_i 7.0 – 8.6 [5-7]
5-MeOT		Rn	Full agonist	6.9 – 8.4	pK_i	5-6,28
⤷	pK_i 6.9 – 8.4 [5-6,28]
S 16924		Rn	Full agonist	7.6	pK_i	27
⤷	pK_i 7.6 [27]
bromocriptine		Hs	Full agonist	7.5	pK_i	21
⤷	pK_i 7.5 [21]
bromocriptine		Rn	Partial agonist	7.5	pK_i	6
⤷	pK_i 7.5 [6]
pergolide		Rn	Full agonist	7.5	pK_i	28
⤷	pK_i 7.5 [28]
5-MeOT		Hs	Full agonist	7.4	pK_i	21
⤷	pK_i 7.4 [21]
lergotrile		Rn	Full agonist	7.4	pK_i	28
⤷	pK_i 7.4 [28]
5-hydroxytryptamine		Rn	Full agonist	6.6 – 7.9	pK_i	5-7,28
⤷	pK_i 6.6 – 7.9 [5-7,28]
dimethyltryptamine		Hs	Full agonist	7.2	pK_i	21
⤷	pK_i 7.2 [21]
5-hydroxytryptamine		Hs	Full agonist	6.8 – 7.5	pK_i	4,7,21
⤷	pK_i 6.8 – 7.5 [4,7,21]
1-naphthylpiperazine		Rn	Full agonist	7.0	pK_i	28
⤷	pK_i 7.0 [28]
5-MeO-DMT		Rn	Full agonist	6.9	pK_i	6
⤷	pK_i 6.9 [6]
5-benzyloxytryptamine		Rn	Full agonist	6.5 – 7.2	pK_i	5-6,28
⤷	pK_i 6.5 – 7.2 [5-6,28]
2-methyl-5-HT		Rn	Full agonist	6.2 – 7.3	pK_i	5
⤷	pK_i 6.2 – 7.3 [5]
DM-1451		Rn	Full agonist	6.5	pK_i	25
⤷	pK_i 6.5 [25]
TFMPP		Hs	Full agonist	6.4	pK_i	21
⤷	pK_i 6.4 [21]
TFMPP		Rn	Full agonist	6.3	pK_i	28
⤷	pK_i 6.3 [28]
tryptamine		Rn	Full agonist	5.8 – 6.8	pK_i	5,28
⤷	pK_i 5.8 – 6.8 [5,28]
RU 24969		Hs	Full agonist	6.2	pK_i	21
⤷	pK_i 6.2 [21]
OPC 4392		Rn	Full agonist	6.2	pK_i	25
⤷	pK_i 6.2 [25]
5-CT		Hs	Full agonist	6.1	pK_i	21
⤷	pK_i 6.1 [21]
5-CT		Rn	Full agonist	5.5 – 6.7	pK_i	5-6,28
⤷	pK_i 5.5 – 6.7 [5-6,28]
LY 165,163		Rn	Full agonist	6.1	pK_i	28
⤷	pK_i 6.1 [28]
CGS-12066		Rn	Full agonist	6.1	pK_i	28
⤷	pK_i 6.1 [28]
BRL-15572		Hs	Partial agonist	5.9	pK_i	34
⤷	pK_i 5.9 [34]
xanomeline		Hs	Full agonist	5.9	pK_i	42
⤷	pK_i 5.9 [42]
GR 127935		Hs	Partial agonist	5.8	pK_i	34
⤷	pK_i 5.8 [34]
capeserod		Hs	Partial agonist	5.6	pK_i	29
⤷	pK_i 5.6 [29]
donitriptan		Hs	Partial agonist	5.6	pK_i	18
⤷	pK_i 5.6 [18]
m-chlorophenylpiperazine		Rn	Full agonist	5.6	pK_i	28
⤷	pK_i 5.6 [28]
α-methyl-5-HT		Rn	Full agonist	5.5	pK_i	6
⤷	pK_i 5.5 [6]
EMD-386088		Hs	Agonist	8.1	pIC₅₀	26
⤷	pIC₅₀ 8.1 (IC₅₀ 7.4x10^-9 M) [26]
[³H]5-CT		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		Hs	Antagonist	9.0	pK_d	16
⤷	pK_d 9.0 (K_d 1x10^-9 M) [16]
[³H]Ro 63-0563		Hs	Antagonist	8.3	pK_d	7
⤷	pK_d 8.3 (K_d 5x10^-9 M) [7]
[¹¹C]GSK215083		Hs	Antagonist	9.8	pK_i	31
⤷	pK_i 9.8 (K_i 1.6x10^-10 M) [31]
intepirdine		Hs	Antagonist	9.8	pK_i	23
⤷	pK_i 9.8 (K_i 1.7x10^-10 M) [23] Description: HeLa cell membrane assay, displacing [³H]LSD
idalopirdine		Hs	Antagonist	9.1	pK_i	23
⤷	pK_i 9.1 (K_i 8.3x10^-10 M) [23]
SB399885		Hs	Antagonist	9.0	pK_i	16
⤷	pK_i 9.0 (K_i 1x10^-9 M) [16]
zotepine		Rn	Inverse agonist	8.9	pK_i	37
⤷	pK_i 8.9 [37]
SB 271046		Hs	Antagonist	8.9	pK_i	10
⤷	pK_i 8.9 (K_i 1.26x10^-9 M) [10]
cerlapirdine		Hs	Antagonist	8.9	pK_i	13
⤷	pK_i 8.9 (K_i 1.3x10^-9 M) [13]
methiothepin		Hs	Antagonist	8.2 – 9.4	pK_i	4,7,21
⤷	pK_i 8.2 – 9.4 [4,7,21]
SB258585		Hs	Antagonist	8.5	pK_i	15
⤷	pK_i 8.5 [15]
SB357134		Hs	Antagonist	8.5	pK_i	11
⤷	pK_i 8.5 [11]
methiothepin		Rn	Antagonist	7.5 – 9.4	pK_i	5-7,28
⤷	pK_i 7.5 – 9.4 [5-7,28]
chlorpromazine		Rn	Inverse agonist	8.4	pK_i	37
⤷	pK_i 8.4 [37]
zotepine		Hs	Inverse agonist	8.3	pK_i	35
⤷	pK_i 8.3 [35]
thioridazine		Rn	Inverse agonist	8.2	pK_i	37
⤷	pK_i 8.2 [37]
Ro 63-0563		Hs	Antagonist	7.9 – 8.4	pK_i	7,40
⤷	pK_i 7.9 – 8.4 (K_i 1.26x10^-8 – 3.98x10^-9 M) [7,40]
olanzapine		Rn	Inverse agonist	7.6 – 8.6	pK_i	22,37
⤷	pK_i 7.6 – 8.6 [22,37]
dihydroergotamine		Rn	Antagonist	7.9 – 8.3	pK_i	6,28
⤷	pK_i 7.9 – 8.3 [6,28]
olanzapine		Hs	Inverse agonist	8.0	pK_i	21,35
⤷	pK_i 8.0 [21,35]
ICI 169369		Hs	Antagonist	8.0	pK_i	21
⤷	pK_i 8.0 [21]
clozapine		Hs	Inverse agonist	7.8 – 8.1	pK_i	4,7,21,35
⤷	pK_i 7.8 – 8.1 [4,7,21,35]
clozapine		Rn	Inverse agonist	7.5 – 8.4	pK_i	5-7,22,27-28,37
⤷	pK_i 7.5 – 8.4 [5-7,22,27-28,37]
Ro 63-0563		Rn	Antagonist	7.8 – 8.0	pK_i	7,40
⤷	pK_i 7.8 – 8.0 [7,40]
amoxapine		Rn	Antagonist	7.5 – 8.2	pK_i	28,37
⤷	pK_i 7.5 – 8.2 [28,37]
fluphenazine		Rn	Inverse agonist	7.8	pK_i	37
⤷	pK_i 7.8 [37]
perphenazine		Rn	Inverse agonist	7.8	pK_i	37
⤷	pK_i 7.8 [37]
2-bromo-LSD		Rn	Antagonist	7.8	pK_i	28
⤷	pK_i 7.8 [28]
fluperlapine		Rn	Inverse agonist	7.8	pK_i	37
⤷	pK_i 7.8 [37]
chlorpromazine		Hs	Inverse agonist	7.7 – 7.8	pK_i	21,35
⤷	pK_i 7.7 – 7.8 [21,35]
MPDT		Hs	Antagonist	7.7	pK_i	14
⤷	pK_i 7.7 [14]
bufotenine		Rn	Antagonist	7.0 – 8.4	pK_i	5
⤷	pK_i 7.0 – 8.4 [5]
Ro 04-6790		Hs	Antagonist	7.3 – 7.9	pK_i	7,40
⤷	pK_i 7.3 – 7.9 [7,40]
loxapine		Hs	Inverse agonist	7.4 – 7.6	pK_i	21,35
⤷	pK_i 7.4 – 7.6 [21,35]
loxapine		Rn	Inverse agonist	7.2 – 7.8	pK_i	28,37
⤷	pK_i 7.2 – 7.8 [28,37]
Ro 04-6790		Rn	Antagonist	7.4 – 7.6	pK_i	7,40
⤷	pK_i 7.4 – 7.6 [7,40]
iloperidone		Rn	Antagonist	7.4	pK_i	22
⤷	pK_i 7.4 [22]
fluperlapine		Hs	Inverse agonist	7.3 – 7.5	pK_i	21,35
⤷	pK_i 7.3 – 7.5 [21,35]
fluphenazine		Hs	Inverse agonist	7.3 – 7.4	pK_i	35
⤷	pK_i 7.3 – 7.4 [35]
amoxapine		Hs	Antagonist	7.3	pK_i	21
⤷	pK_i 7.3 [21]
α-ergocryptine		Rn	Antagonist	7.3	pK_i	6
⤷	pK_i 7.3 [6]
iloperidone		Hs	Antagonist	7.2	pK_i	19
⤷	pK_i 7.2 [19]
pimozide		Rn	Antagonist	7.2	pK_i	37
⤷	pK_i 7.2 [37]
ritanserin		Hs	Antagonist	7.0 – 7.4	pK_i	4,7,21
⤷	pK_i 7.0 – 7.4 [4,7,21]
thioridazine		Hs	Inverse agonist	7.2	pK_i	35
⤷	pK_i 7.2 [35]
dihydroergocristine		Rn	Antagonist	7.2	pK_i	6
⤷	pK_i 7.2 [6]
ritanserin		Rn	Antagonist	6.5 – 7.8	pK_i	5-7,28
⤷	pK_i 6.5 – 7.8 [5-7,28]
mianserin		Rn	Antagonist	6.9 – 7.4	pK_i	5,7,28
⤷	pK_i 6.9 – 7.4 [5,7,28]
mianserin		Hs	Antagonist	6.9 – 7.3	pK_i	4,7,21
⤷	pK_i 6.9 – 7.3 [4,7,21]
tiospirone		Rn	Antagonist	7.1	pK_i	37
⤷	pK_i 7.1 [37]
perphenazine		Hs	Inverse agonist	7.1	pK_i	35
⤷	pK_i 7.1 [35]
metergoline		Rn	Antagonist	6.6 – 7.5	pK_i	5-7,28
⤷	pK_i 6.6 – 7.5 [5-7,28]
amitriptyline		Hs	Antagonist	6.9 – 7.2	pK_i	4,7,21
⤷	pK_i 6.9 – 7.2 [4,7,21]
metergoline		Hs	Antagonist	6.4 – 7.4	pK_i	4,7,21
⤷	pK_i 6.4 – 7.4 [4,7,21]
cyproheptadine		Rn	Antagonist	6.9	pK_i	28
⤷	pK_i 6.9 [28]
amitriptyline		Rn	Antagonist	6.5 – 7.2	pK_i	5,7,28
⤷	pK_i 6.5 – 7.2 [5,7,28]
aripiprazole		Rn	Antagonist	6.8	pK_i	25
⤷	pK_i 6.8 [25]
cyproheptadine		Hs	Antagonist	6.8	pK_i	21
⤷	pK_i 6.8 [21]
methysergide		Hs	Antagonist	6.5 – 6.8	pK_i	4,7,21
⤷	pK_i 6.5 – 6.8 [4,7,21]
methysergide		Rn	Antagonist	6.4 – 6.6	pK_i	5-7,28
⤷	pK_i 6.4 – 6.6 [5-7,28]
vortioxetine		Hs	Antagonist	6.5	pK_i	1
⤷	pK_i 6.5 (K_i 3.3x10^-7 M) [1]
duloxetine		Hs	Antagonist	6.4	pK_i	12
⤷	pK_i 6.4 [12]
risperidone		Rn	Inverse agonist	6.0 – 6.4	pK_i	22,37
⤷	pK_i 6.0 – 6.4 [22,37]
tiospirone		Hs	Antagonist	6.0	pK_i	21
⤷	pK_i 6.0 [21]
spiperone		Rn	Antagonist	5.8	pK_i	37
⤷	pK_i 5.8 [37]
fluoxetine		Rn	Antagonist	5.8	pK_i	28
⤷	pK_i 5.8 [28]
sumatriptan		Hs	Antagonist	5.6	pK_i	21
⤷	pK_i 5.6 [21]
risperidone

5-HT6 receptor

Contents:

5-HT₆ receptor