Nomenclature: 5-HT6 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. 

Contents

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 18
Mouse 7 440 4 D3 Htr6 5-hydroxytryptamine (serotonin) receptor 6 17
Rat 7 436 5 Htr6 5-hydroxytryptamine (serotonin) receptor 6, G protein-coupled 23,32
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
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
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 3
pKd 8.7 (Kd 2x10-9 M) [3]
[3H]LSD Rn Full agonist 8.6 – 8.7 pKd 2,21
pKd 8.6 – 8.7 [2,21]
5-HT Rn Full agonist 7.9 pKd 2
pKd 7.9 [2]
E-6801 Hs Partial agonist 8.7 pKi 14
pKi 8.7 (Ki 1.9x10-9 M) [14]
WAY-181187 Hs Agonist 8.7 pKi 33
pKi 8.7 [33]
LSD Hs Full agonist 8.4 pKi 5
pKi 8.4 [5]
ergotamine Hs Full agonist 8.0 – 8.6 pKi 3,5
pKi 8.0 – 8.6 [3,5]
LSD Rn Full agonist 7.8 – 8.7 pKi 2,5
pKi 7.8 – 8.7 [2,5]
lisuride Hs Partial agonist 8.0 – 8.1 pKi 3,5
pKi 8.0 – 8.1 [3,5]
lisuride Rn Partial agonist 7.5 – 8.3 pKi 2,4-5,23
pKi 7.5 – 8.3 [2,4-5,23]
ergotamine Rn Full agonist 7.0 – 8.6 pKi 2,4-5
pKi 7.0 – 8.6 [2,4-5]
EMDT Hs Full agonist 7.8 pKi 12
pKi 7.8 [12]
5-MeOT Rn Full agonist 6.9 – 8.4 pKi 2,4,23
pKi 6.9 – 8.4 [2,4,23]
S 16924 Rn Full agonist 7.6 pKi 22
pKi 7.6 [22]
pergolide Rn Full agonist 7.5 pKi 23
pKi 7.5 [23]
bromocriptine Rn Partial agonist 7.5 pKi 4
pKi 7.5 [4]
bromocriptine Hs Full agonist 7.5 pKi 18
pKi 7.5 [18]
5-MeOT Hs Full agonist 7.4 pKi 18
pKi 7.4 [18]
lergotrile Rn Full agonist 7.4 pKi 23
pKi 7.4 [23]
5-HT Rn Full agonist 6.6 – 7.9 pKi 2,4-5,23
pKi 6.6 – 7.9 [2,4-5,23]
dimethyltryptamine Hs Full agonist 7.2 pKi 18
pKi 7.2 [18]
5-HT Hs Full agonist 6.8 – 7.5 pKi 3,5,18
pKi 6.8 – 7.5 [3,5,18]
1-naphthylpiperazine Rn Full agonist 7.0 pKi 23
pKi 7.0 [23]
5-MeO-DMT Rn Full agonist 6.9 pKi 4
pKi 6.9 [4]
5-benzyloxytryptamine Rn Full agonist 6.5 – 7.2 pKi 2,4,23
pKi 6.5 – 7.2 [2,4,23]
aripiprazole Rn Full agonist 6.8 pKi 21
pKi 6.8 [21]
2-methyl-5-HT Rn Full agonist 6.2 – 7.3 pKi 2
pKi 6.2 – 7.3 [2]
DM-1451 Rn Full agonist 6.5 pKi 21
pKi 6.5 [21]
TFMPP Hs Full agonist 6.4 pKi 18
pKi 6.4 [18]
TFMPP Rn Full agonist 6.3 pKi 23
pKi 6.3 [23]
tryptamine Rn Full agonist 5.8 – 6.8 pKi 2,23
pKi 5.8 – 6.8 [2,23]
OPC 4392 Rn Full agonist 6.2 pKi 21
pKi 6.2 [21]
RU 24969 Hs Full agonist 6.2 pKi 18
pKi 6.2 [18]
LY 165,163 Rn Full agonist 6.1 pKi 23
pKi 6.1 [23]
5-CT Hs Full agonist 6.1 pKi 18
pKi 6.1 [18]
5-CT Rn Full agonist 5.5 – 6.7 pKi 2,4,23
pKi 5.5 – 6.7 [2,4,23]
CGS-12066 Rn Full agonist 6.1 pKi 23
pKi 6.1 [23]
xanomeline Hs Full agonist 5.9 pKi 36
pKi 5.9 [36]
BRL-15572 Hs Partial agonist 5.9 pKi 28
pKi 5.9 [28]
GR-127935 Hs Partial agonist 5.8 pKi 28
pKi 5.8 [28]
donitriptan Hs Partial agonist 5.6 pKi 15
pKi 5.6 [15]
m-CPP Rn Full agonist 5.6 pKi 23
pKi 5.6 [23]
SL65.0155 Hs Partial agonist 5.6 pKi 24
pKi 5.6 [24]
α-methyl-5-HT Rn Full agonist 5.5 pKi 4
pKi 5.5 [4]
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
pKd 8.3 (Kd 5x10-9 M) [5]
SB399885 Hs Antagonist 9.0 pKi 13
pKi 9.0 [13]
zotepine Rn Inverse agonist 8.9 pKi 31
pKi 8.9 [31]
SB 271046 Hs Antagonist 8.9 pKi 8
pKi 8.9 [8]
cerlapirdine Hs Antagonist 8.89 pKi 11
pKi 8.89 (Ki 1.3x10-9 M) [11]
methiothepin Hs Antagonist 8.2 – 9.4 pKi 3,5,18
pKi 8.2 – 9.4 [3,5,18]
SB357134 Hs Antagonist 8.5 pKi 9
pKi 8.5 [9]
methiothepin Rn Antagonist 7.5 – 9.4 pKi 2,4-5,23
pKi 7.5 – 9.4 [2,4-5,23]
chlorpromazine Rn Inverse agonist 8.4 pKi 31
pKi 8.4 [31]
zotepine Hs Inverse agonist 8.3 pKi 29
pKi 8.3 [29]
thioridazine Rn Inverse agonist 8.2 pKi 31
pKi 8.2 [31]
Ro 63-0563 Hs Antagonist 7.9 – 8.4 pKi 5,34
pKi 7.9 – 8.4 [5,34]
olanzapine Rn Inverse agonist 7.6 – 8.6 pKi 19,31
pKi 7.6 – 8.6 [19,31]
dihydroergotamine Rn Antagonist 7.9 – 8.3 pKi 4,23
pKi 7.9 – 8.3 [4,23]
olanzapine Hs Inverse agonist 8.0 pKi 18,29
pKi 8.0 [18,29]
ICI 169369 Hs Antagonist 8.0 pKi 18
pKi 8.0 [18]
clozapine Hs Inverse agonist 7.8 – 8.1 pKi 3,5,18,29
pKi 7.8 – 8.1 [3,5,18,29]
clozapine Rn Inverse agonist 7.5 – 8.4 pKi 2,4-5,19,22-23,31
pKi 7.5 – 8.4 [2,4-5,19,22-23,31]
Ro 63-0563 Rn Antagonist 7.8 – 8.0 pKi 5,34
pKi 7.8 – 8.0 [5,34]
amoxapine Rn Antagonist 7.5 – 8.2 pKi 23,31
pKi 7.5 – 8.2 [23,31]
fluperlapine Rn Inverse agonist 7.8 pKi 31
pKi 7.8 [31]
perphenazine Rn Inverse agonist 7.8 pKi 31
pKi 7.8 [31]
fluphenazine Rn Inverse agonist 7.8 pKi 31
pKi 7.8 [31]
2-Br-LSD Rn Antagonist 7.8 pKi 23
pKi 7.8 [23]
chlorpromazine Hs Inverse agonist 7.7 – 7.8 pKi 18,29
pKi 7.7 – 7.8 [18,29]
MPDT Hs Antagonist 7.7 pKi 12
pKi 7.7 [12]
bufotenine Rn Antagonist 7.0 – 8.4 pKi 2
pKi 7.0 – 8.4 [2]
Ro 04-6790 Hs Antagonist 7.3 – 7.9 pKi 5,34
pKi 7.3 – 7.9 [5,34]
Ro 04-6790 Rn Antagonist 7.4 – 7.6 pKi 5,34
pKi 7.4 – 7.6 [5,34]
loxapine Hs Inverse agonist 7.4 – 7.6 pKi 18,29
pKi 7.4 – 7.6 [18,29]
loxapine Rn Inverse agonist 7.2 – 7.8 pKi 23,31
pKi 7.2 – 7.8 [23,31]
fluperlapine Hs Inverse agonist 7.3 – 7.5 pKi 18,29
pKi 7.3 – 7.5 [18,29]
iloperidone Rn Antagonist 7.4 pKi 19
pKi 7.4 [19]
fluphenazine Hs Inverse agonist 7.3 – 7.4 pKi 29
pKi 7.3 – 7.4 [29]
α-ergocryptine Rn Antagonist 7.3 pKi 4
pKi 7.3 [4]
amoxapine Hs Antagonist 7.3 pKi 18
pKi 7.3 [18]
pimozide Rn Antagonist 7.2 pKi 31
pKi 7.2 [31]
dihydroergocristine Rn Antagonist 7.2 pKi 4
pKi 7.2 [4]
thioridazine Hs Inverse agonist 7.2 pKi 29
pKi 7.2 [29]
iloperidone Hs Antagonist 7.2 pKi 16
pKi 7.2 [16]
ritanserin Hs Antagonist 7.0 – 7.4 pKi 3,5,18
pKi 7.0 – 7.4 [3,5,18]
mianserin Rn Antagonist 6.9 – 7.4 pKi 2,5,23
pKi 6.9 – 7.4 [2,5,23]
ritanserin Rn Antagonist 6.5 – 7.8 pKi 2,4-5,23
pKi 6.5 – 7.8 [2,4-5,23]
mianserin Hs Antagonist 6.9 – 7.3 pKi 3,5,18
pKi 6.9 – 7.3 [3,5,18]
perphenazine Hs Inverse agonist 7.1 pKi 29
pKi 7.1 [29]
tiospirone Rn Antagonist 7.1 pKi 31
pKi 7.1 [31]
metergoline Rn Antagonist 6.6 – 7.5 pKi 2,4-5,23
pKi 6.6 – 7.5 [2,4-5,23]
amitriptyline Hs Antagonist 6.9 – 7.2 pKi 3,5,18
pKi 6.9 – 7.2 [3,5,18]
metergoline Hs Antagonist 6.4 – 7.4 pKi 3,5,18
pKi 6.4 – 7.4 [3,5,18]
cyproheptadine Rn Antagonist 6.9 pKi 23
pKi 6.9 [23]
amitriptyline Rn Antagonist 6.5 – 7.2 pKi 2,5,23
pKi 6.5 – 7.2 [2,5,23]
cyproheptadine Hs Antagonist 6.8 pKi 18
pKi 6.8 [18]
methysergide Hs Antagonist 6.5 – 6.8 pKi 3,5,18
pKi 6.5 – 6.8 [3,5,18]
methysergide Rn Antagonist 6.4 – 6.6 pKi 2,4-5,23
pKi 6.4 – 6.6 [2,4-5,23]
duloxetine Hs Antagonist 6.4 pKi 10
pKi 6.4 [10]
risperidone Rn Inverse agonist 6.0 – 6.4 pKi 19,31
pKi 6.0 – 6.4 [19,31]
tiospirone Hs Antagonist 6.0 pKi 18
pKi 6.0 [18]
spiperone Rn Antagonist 5.8 pKi 31
pKi 5.8 [31]
fluoxetine Rn Antagonist 5.8 pKi 23
pKi 5.8 [23]
sumatriptan Hs Antagonist 5.6 pKi 18
pKi 5.6 [18]
risperidone Hs Antagonist 5.6 pKi 18
pKi 5.6 [18]
mesulergine Hs Antagonist 5.4 – 5.7 pKi 3,5,18
pKi 5.4 – 5.7 [3,5,18]
mesulergine Rn Antagonist 5.1 – 5.8 pKi 2,5,23
pKi 5.1 – 5.8 [2,5,23]
sumatriptan Rn Antagonist 5.2 pKi 4
pKi 5.2 [4]
View species-specific antagonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  39
Secondary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  39
Tissue Distribution
Superior cervical ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  27
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  35
Brain: nucleus accumbens, olfactory tubercle, striatum, hippocampus, anterior corpus.
Species:  Rat
Technique:  in situ hybridisation.
References:  38
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 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:  39
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:  2,39
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:  17
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:  17
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:  32
Physiological Functions
Role in spatial learning and memory.
Species:  Rat
Tissue:  In vivo.
References:  26,30,37
Modulation of acetlycholinergic neurotransmission.
Species:  Rat
Tissue:  In vivo.
References:  1,6-7,20
Modulation of dopaminergic neurotransmission.
Species:  Rat
Tissue:  In vivo.
References:  20
Phenotypes, Alleles and Disease Models Mouse data from MGI

Show »

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
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:  25
Available Assays
DiscoveRx PathHunter® DLD1 HTR6 β-Arrestin Cell Line (Cat no. 93-0294C13) more info

REFERENCES

1. Bentley JC, Bourson A, Boess FG, Fone KC, Marsden CA, Petit N, Sleight AJ. (1999) Investigation of stretching behaviour induced by the selective 5-HT6 receptor antagonist, Ro 04-6790, in rats. Br J Pharmacol126: 1537-1542. [PMID:10323584]

2. Boess FG, Monsma FJ, Carolo C, Meyer V, Rudler A, Zwingelstein C, Sleight AJ. (1997) Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells. Neuropharmacology36: 713-720. [PMID:9225298]

3. Boess FG, Monsma FJ, Meyer V, Zwingelstein C, Sleight AJ. (1997) Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor. Mol Pharmacol52: 515-523. [PMID:9284367]

4. Boess FG, Monsma FJ, Sleight AJ. (1998) Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor. J Neurochem71: 2169-2177. [PMID:9798944]

5. Boess FG, Riemer C, Bos M, Bentley J, Bourson A, Sleight AJ. (1998) The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum. Mol Pharmacol54: 577-583. [PMID:9730917]

6. Bourson A, Boess FG, Bos M, Sleight AJ. (1998) Involvement of 5-HT6 receptors in nigro-striatal function in rodents. Br J Pharmacol125: 1562-1566. [PMID:9884085]

7. Bourson A, Borroni E, Austin RH, Monsma FJ, Sleight AJ. (1994) Determination of the role of the 5-ht6 receptor in the rat brain: a study using antisense oligonucleotides. J Pharmacol Exp Ther275: 173-180. [PMID:7616396]

8. Bromidge SM, Brown AM, Clarke SE, Dodgson K, Gager T, Grassam HL, Jeffrey PM, Joiner GF, King FD, Middlemiss DN, Moss SF, Newman H, Riley G, Routledge C, Wyman P. (1999) 5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist. J Med Chem42: 202-205. [PMID:9925723]

9. Bromidge SM, Clarke SE, Gager T, Griffith K, Jeffrey P, Jennings AJ, Joiner GF, King FD, Lovell PJ, Moss SF et al.. (2001) Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134). Bioorg. Med. Chem. Lett.11 (1): 55-8. [PMID:11140733]

10. Bymaster FP, Dreshfield-Ahmad LJ, Threlkeld PG, Shaw JL, Thompson L, Nelson DL, Hemrick-Luecke SK, Wong DT. (2001) Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology25: 871-880. [PMID:11750180]

11. Commery TA. (2010) SAM-531, N,N-dimethyl-3-{[3-(1-naphthylsulfonyl)-1H-indazol-5-yl]oxy} propan-1-amine, a novel serotonin-6 receptor antagonist with preclinical pro-cognitive efficacy. Alzheimer's & Dementia6 (4): S548-S549.

12. Glennon RA, Lee M, Rangisetty JB, Dukat M, Roth BL, Savage JE, McBride A, Rauser L, Hufeisen S, Lee DK. (2000) 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem43: 1011-1018. [PMID:10715164]

13. Hirst WD, Stean TO, Rogers DC, Sunter D, Pugh P, Moss SF, Bromidge SM, Riley G, Smith DR, Bartlett S et al.. (2006) SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models. Eur. J. Pharmacol.553 (1-3): 109-19. [PMID:17069795]

14. Holenz J, Mercè R, Díaz JL, Guitart X, Codony X, Dordal A, Romero G, Torrens A, Mas J, Andaluz B et al.. (2005) Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. J. Med. Chem.48 (6): 1781-95. [PMID:15771424]

15. John GW, Pauwels PJ, Perez M, Halazy S, Le Grand B, Verscheure Y, Valentin JP, Palmier C, Wurch T, Chopin P, Marien M, Kleven MS, Koek W, Assie MB, Carilla-Durand E, Tarayre JP, Colpaert FC. (1999) F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine. J Pharmacol Exp Ther290: 83-95. [PMID:10381763]

16. Kalkman HO, Subramanian N, Hoyer D. (2001) Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders. Neuropsychopharmacology25: 904-914. [PMID:11750183]

17. Kohen R, Fashingbauer LA, Heidmann DE, Guthrie CR, Hamblin MW. (2001) Cloning of the mouse 5-HT6 serotonin receptor and mutagenesis studies of the third cytoplasmic loop. Brain Res Mol Brain Res90: 110-117. [PMID:11406289]

18. Kohen R, Metcalf MA, Khan N, Druck T, Huebner K, Lachowicz JE, Meltzer HY, Sibley DR, Roth BL, Hamblin MW. (1996) Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. J Neurochem66: 47-56. [PMID:8522988]

19. Kongsamut S, Roehr JE, Cai J, Hartman HB, Weissensee P, Kerman LL, Tang L, Sandrasagra A. (1996) Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol317: 417-423. [PMID:8997630]

20. Lacroix LP, Dawson LA, Hagan JJ, Heidbreder CA. (2004) 5-HT6 receptor antagonist SB-271046 enhances extracellular levels of monoamines in the rat medial prefrontal cortex. Synapse51: 258-264. [PMID:14618683]

21. Lawler CP, Prioleau C, Lewis MM, Mak C, Jiang D, Schetz JA, Gonzalez AM, Sibley DR, Mailman RB. (1999) Interactions of the novel antipsychotic aripiprazole (OPC-14597) with dopamine and serotonin receptor subtypes. Neuropsychopharmacology20: 612-627. [PMID:10327430]

22. Millan MJ, Gobert A, Newman-Tancredi A, Audinot V, Lejeune F, Rivet JM, Cussac D, Nicolas JP, Muller O, Lavielle G. (1998) S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol. J Pharmacol Exp Ther286: 1341-1355. [PMID:9732398]

23. Monsma FJ, Shen Y, Ward RP, Hamblin MW, Sibley DR. (1993) Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. Mol Pharmacol43: 320-327. [PMID:7680751]

24. Moser PC, Bergis OE, Jegham S, Lochead A, Duconseille E, Terranova JP, Caille D, Berque-Bestel I, Lezoualc'h F, Fischmeister R, Dumuis A, Bockaert J, George P, Soubrie P, Scatton B. (2002) SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties. J Pharmacol Exp Ther302: 731-741. [PMID:12130738]

25. Olsen MA, Nawoschik SP, Schurman BR, Schmitt HL, Burno M, Smith DL, Schechter LE. (1999) Identification of a human 5-HT6 receptor variant produced by alternative splicing. Brain Res Mol Brain Res64: 255-263. [PMID:9931499]

26. Perez-Garcia G, Meneses A. (2005) Oral administration of the 5-HT6 receptor antagonists SB-357134 and SB-399885 improves memory formation in an autoshaping learning task. Pharmacol Biochem Behav81: 673-682. [PMID:15964617]

27. Pierce PA, Xie GX, Levine JD, Peroutka SJ. (1996) 5-Hydroxytryptamine receptor subtype messenger RNAs in rat peripheral sensory and sympathetic ganglia: a polymerase chain reaction study. Neuroscience70: 553-559. [PMID:8848158]

28. Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Gothert M, Jones BJ, Roberts C, Watson JM, Middlemiss DN. (1997) SB-216641 and BRL-15572 compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch. Pharmacol.356: 312-320. [PMID:9303567]

29. Purohit A, Smith C, Herrick-Davis K, Teitler M. (2005) Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs. Psychopharmacology (Berl)179: 461-469. [PMID:15821958]

30. Rogers DC, Hagan JJ. (2001) 5-HT6 receptor antagonists enhance retention of a water maze task in the rat. Psychopharmacology (Berl)158: 114-119. [PMID:11702084]

31. Roth BL, Craigo SC, Choudhary MS, Uluer A, Monsma FJ, Shen Y, Meltzer HY, Sibley DR. (1994) Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. J Pharmacol Exp Ther268: 1403-1410. [PMID:7908055]

32. Ruat M, Traiffort E, Arrang JM, Tardivel-Lacombe J, Diaz J, Leurs R, Schwartz JC. (1993) A novel rat serotonin (5-HT6) receptor: molecular cloning, localization and stimulation of cAMP accumulation. Biochem Biophys Res Commun193: 268-276. [PMID:8389146]

33. Schechter LE, Lin Q, Smith DL, Zhang G, Shan Q, Platt B, Brandt MR, Dawson LA, Cole D, Bernotas R et al.. (2008) Neuropharmacological profile of novel and selective 5-HT6 receptor agonists: WAY-181187 and WAY-208466. Neuropsychopharmacology33 (6): 1323-35. [PMID:17625499]

34. Sleight AJ, Boess FG, Bos M, Levet-Trafit B, Riemer C, Bourson A. (1998) Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-ht6receptors. Br. J. Pharmacol.124: 556-562. [PMID:9647481]

35. Stefulj J, Jernej B, Cicin-Sain L, Rinner I, Schauenstein K. (2000) mRNA expression of serotonin receptors in cells of the immune tissues of the rat. Brain Behav Immun14: 219-224. [PMID:10970681]

36. Watson J, Brough S, Coldwell MC, Gager T, Ho M, Hunter AJ, Jerman J, Middlemiss DN, Riley GJ, Brown AM. (1998) Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors. Br J Pharmacol125: 1413-1420. [PMID:9884068]

37. Woolley ML, Bentley JC, Sleight AJ, Marsden CA, Fone KC. (2001) A role for 5-ht6 receptors in retention of spatial learning in the Morris water maze. Neuropharmacology41: 210-219. [PMID:11489457]

38. Yoshioka M, Matsumoto M, Togashi H, Mori K, Saito H. (1998) Central distribution and function of 5-HT6 receptor subtype in the rat brain. Life Sci62: 1473-1477. [PMID:9585121]

39. Zhang JY, Nawoschik S, Kowal D, Smith D, Spangler T, Ochalski R, Schechter L, Dunlop J. (2003) Characterization of the 5-HT6 receptor coupled to Ca2+ signaling using an enabling chimeric G-protein. Eur J Pharmacol472: 33-38. [PMID:12860470]

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 21/03/2014. Accessed on 18/04/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=11.

Contact us | Print | Back to top | Help
Copyright © 2014 IUPHAR