Nomenclature: 5-HT7 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 7 479 10q21-q24 HTR7 5-hydroxytryptamine (serotonin) receptor 7, adenylate cyclase-coupled 41
Mouse 7 448 19 C2 Htr7 5-hydroxytryptamine (serotonin) receptor 7 33
Rat 7 448 1q53 Htr7 5-hydroxytryptamine (serotonin) receptor 7, adenylate cyclase-coupled 25,37-38
Previous and Unofficial Names
5-HTx
5-HT1-like
5-HT1Y
5-HT7
5-hydroxytryptamine (serotonin) receptor 7 (adenylate cyclase-coupled)
5Ht7
5-HT-7
5-HT-X
5-hydroxytryptamine receptor 7
GPRFO
high affinity serotonin receptor (5HT7)
high affinity serotonin receptor (5HT7) gene
serotonin receptor 7
5-hydroxytryptamine (serotonin) receptor 7
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]5-CT Hs Agonist 9.4 pKd 46
pKd 9.4 (Kd 4x10-10 M) [46]
[125I]LSD Rn Full agonist 8.9 pKd 25
pKd 8.9 [25]
[3H]LSD Hs Full agonist 8.5 – 8.6 pKd 41
pKd 8.5 – 8.6 (Kd 2.51x10-9 – 3.16x10-9 M) [41]
[3H]5-HT Hs Full agonist 8.1 – 9.0 pKd 3,41
pKd 8.1 – 9.0 (Kd 1x10-9 – 7.94x10-9 M) [3,41]
[3H]LSD Rn Full agonist 8.2 pKd 24
pKd 8.2 [24]
5-CT Rn Full agonist 9.5 – 9.9 pKi 37-38
pKi 9.5 – 9.9 [37-38]
5-CT Hs Full agonist 9.0 – 10.0 pKi 3,18,22,47
pKi 9.0 – 10.0 [3,18,22,47]
5-MeOT Rn Full agonist 8.8 – 9.2 pKi 37-38
pKi 8.8 – 9.2 [37-38]
5-CT Mm Full agonist 9.0 pKi 33
pKi 9.0 [33]
5-HT Rn Full agonist 8.7 – 9.2 pKi 37-38
pKi 8.7 – 9.2 [37-38]
5-MeOT Hs Full agonist 8.3 – 9.5 pKi 3,18,22
pKi 8.3 – 9.5 [3,18,22]
5-HT Hs Full agonist 8.1 – 9.6 pKi 3,13,18,22,47
pKi 8.1 – 9.6 [3,13,18,22,47]
lisuride Rn Full agonist 8.2 – 9.3 pKi 37-38
pKi 8.2 – 9.3 [37-38]
pergolide Rn Full agonist 8.3 – 9.0 pKi 38
pKi 8.3 – 9.0 [38]
E55888 Hs Full agonist 8.6 pKi 5
pKi 8.6 [5]
5-HT Mm Full agonist 8.3 pKi 33
pKi 8.3 [33]
dipropyl-5-CT Hs Full agonist 8.2 – 8.4 pKi 18
pKi 8.2 – 8.4 [18]
5-MeOT Mm Full agonist 8.2 pKi 33
pKi 8.2 [33]
(+)-LSD Hs Full agonist 8.0 pKi 37
pKi 8.0 [37]
aripiprazole Rn Full agonist 7.8 pKi 24
pKi 7.8 [24]
OPC 4392 Rn Full agonist 7.7 pKi 24
pKi 7.7 [24]
tryptamine Rn Full agonist 7.5 – 7.8 pKi 38
pKi 7.5 – 7.8 [38]
bromocriptine Rn Full agonist 7.3 – 8.0 pKi 38
pKi 7.3 – 8.0 [38]
1-naphthylpiperazine Rn Full agonist 7.5 – 7.7 pKi 38
pKi 7.5 – 7.7 [38]
5-MeO-DMT Rn Full agonist 7.4 – 7.7 pKi 38
pKi 7.4 – 7.7 [38]
8-OH-DPAT Rn Full agonist 7.3 – 7.5 pKi 37-38
pKi 7.3 – 7.5 [37-38]
1-naphthylpiperazine Hs Full agonist 7.1 pKi 3
pKi 7.1 [3]
bufotenine Mm Full agonist 7.0 pKi 33
pKi 7.0 [33]
8-OH-DPAT Hs Full agonist 6.3 – 7.6 pKi 3,18,22,47
pKi 6.3 – 7.6 [3,18,22,47]
xanomeline Hs Full agonist 6.9 pKi 49
pKi 6.9 [49]
RU 24969 Mm Full agonist 6.9 pKi 33
pKi 6.9 [33]
tryptamine Hs Full agonist 6.8 pKi 3
pKi 6.8 [3]
2-MPP Rn Full agonist 6.6 – 6.9 pKi 38
pKi 6.6 – 6.9 [38]
DM-1451 Rn Full agonist 6.7 pKi 24
pKi 6.7 [24]
8-OH-DPAT Mm Full agonist 6.6 pKi 33
pKi 6.6 [33]
m-CPP Rn Full agonist 6.4 – 6.6 pKi 38
pKi 6.4 – 6.6 [38]
EMDT Hs Full agonist 6.5 pKi 10
pKi 6.5 [10]
TFMPP Rn Full agonist 6.3 – 6.6 pKi 38
pKi 6.3 – 6.6 [38]
buspirone Rn Partial agonist 6.4 pKi 37
pKi 6.4 [37]
cisapride Mm Full agonist 5.8 pKi 33
pKi 5.8 [33]
SL65.0155 Hs Partial agonist 5.5 pKi 27
pKi 5.5 [27]
LY344864 Hs Full agonist 5.3 pKi 31
pKi 5.3 [31]
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
risperidone Rn Inverse agonist 8.9 – 9.0 pKd 21,36
pKd 8.9 – 9.0 [21,36]
[3H]SB269970 Hs Antagonist 8.92 pKd 46
pKd 8.92 (Kd 1.2x10-9 M) [46]
pimozide Rn Antagonist 9.3 pKi 36
pKi 9.3 [36]
methiothepin Rn Antagonist 9.0 – 9.4 pKi 38
pKi 9.0 – 9.4 [38]
tiospirone Rn Antagonist 9.2 pKi 36
pKi 9.2 [36]
methiothepin Hs Antagonist 8.4 – 9.4 pKi 3,18,22,47
pKi 8.4 – 9.4 [3,18,22,47]
zotepine Rn Inverse agonist 8.8 pKi 36
pKi 8.8 [36]
SB269970 Hs Antagonist 8.6 – 8.9 pKi 46
pKi 8.6 – 8.9 [46]
SB656104 Hs Antagonist 8.7 pKi 9
pKi 8.7 (Ki 1.9x10-9 M) [9]
metergoline Hs Antagonist 8.2 – 8.9 pKi 3,18,22
pKi 8.2 – 8.9 [3,18,22]
risperidone Hs Inverse agonist 8.3 – 8.7 pKi 34,47
pKi 8.3 – 8.7 [34,47]
ziprasidone Hs Inverse agonist 8.4 pKi 34
pKi 8.4 [34]
zotepine Hs Inverse agonist 8.4 pKi 34
pKi 8.4 [34]
pirenperone Hs Antagonist 8.2 – 8.5 pKi 18
pKi 8.2 – 8.5 [18]
fluperlapine Rn Inverse agonist 8.3 pKi 36
pKi 8.3 [36]
methiothepin Mm Antagonist 8.2 pKi 33
pKi 8.2 [33]
fluphenazine Rn Inverse agonist 8.1 pKi 36
pKi 8.1 [36]
2-Br-LSD Mm Antagonist 8.0 pKi 33
pKi 8.0 [33]
dihydroergotamine Hs Antagonist 8.0 pKi 3
pKi 8.0 [3]
metergoline Rn Antagonist 7.2 – 8.7 pKi 37-38
pKi 7.2 – 8.7 [37-38]
mesulergine Rn Antagonist 7.7 – 8.2 pKi 38
pKi 7.7 – 8.2 [38]
methysergide Rn Antagonist 7.9 pKi 38
pKi 7.9 [38]
methysergide Mm Antagonist 7.9 pKi 33
pKi 7.9 [33]
fluphenazine Hs Inverse agonist 7.9 pKi 34
pKi 7.9 [34]
mesulergine Hs Antagonist 7.5 – 8.2 pKi 3,18,22,47
pKi 7.5 – 8.2 [3,18,22,47]
spiperone Rn Antagonist 7.7 – 8.0 pKi 36-37
pKi 7.7 – 8.0 [36-37]
ritanserin Rn Antagonist 7.7 – 7.8 pKi 38
pKi 7.7 – 7.8 [38]
iloperidone Rn Antagonist 7.7 pKi 21
pKi 7.7 [21]
clozapine Rn Inverse agonist 7.2 – 8.2 pKi 21,36-38
pKi 7.2 – 8.2 [21,36-38]
mesulergine Mm Antagonist 7.6 pKi 33
pKi 7.6 [33]
perphenazine Rn Inverse agonist 7.6 pKi 36
pKi 7.6 [36]
chlorpromazine Rn Inverse agonist 7.6 pKi 36
pKi 7.6 [36]
chlorpromazine Hs Inverse agonist 7.6 pKi 34
pKi 7.6 [34]
metergoline Mm Antagonist 7.5 pKi 33
pKi 7.5 [33]
fluperlapine Hs Inverse agonist 7.5 pKi 34
pKi 7.5 [34]
spiperone Hs Antagonist 7.0 – 8.0 pKi 3,18,22
pKi 7.0 – 8.0 [3,18,22]
2-Br-LSD Hs Antagonist 7.5 pKi 3
pKi 7.5 [3]
clozapine Hs Inverse agonist 7.2 – 7.8 pKi 22,34,47
pKi 7.2 – 7.8 [22,34,47]
(+)-butaclamol Mm Antagonist 7.5 pKi 33
pKi 7.5 [33]
SB 258719 Hs Inverse agonist 7.5 pKi 47
pKi 7.5 [47]
methysergide Hs Antagonist 7.1 – 7.8 pKi 3,18,22
pKi 7.1 – 7.8 [3,18,22]
mianserin Hs Antagonist 7.3 – 7.6 pKi 18
pKi 7.3 – 7.6 [18]
amoxapine Rn Antagonist 7.4 pKi 36
pKi 7.4 [36]
clozapine Mm Inverse agonist 7.4 pKi 33
pKi 7.4 [33]
cyproheptadine Rn Antagonist 7.1 – 7.5 pKi 37-38
pKi 7.1 – 7.5 [37-38]
ergotamine Mm Antagonist 7.3 pKi 33
pKi 7.3 [33]
mianserin Rn Antagonist 7.0 – 7.4 pKi 37-38
pKi 7.0 – 7.4 [37-38]
thioridazine Rn Inverse agonist 7.2 pKi 36
pKi 7.2 [36]
perphenazine Hs Inverse agonist 7.2 pKi 34
pKi 7.2 [34]
spiperone Mm Antagonist 7.2 pKi 33
pKi 7.2 [33]
cyamemazine Hs Antagonist 7.2 pKi 13
pKi 7.2 [13]
ritanserin Hs Antagonist 6.8 – 7.4 pKi 3,22
pKi 6.8 – 7.4 [3,22]
loxapine Rn Antagonist 6.8 – 7.4 pKi 36,38
pKi 6.8 – 7.4 [36,38]
thioridazine Hs Inverse agonist 7.1 pKi 34
pKi 7.1 [34]
mianserin Mm Antagonist 7.0 pKi 33
pKi 7.0 [33]
iloperidone Hs Antagonist 7.0 pKi 19
pKi 7.0 [19]
(+)-butaclamol Rn Antagonist 7.0 pKi 37
pKi 7.0 [37]
dihydroergocryptine Mm Antagonist 7.0 pKi 33
pKi 7.0 [33]
amitriptyline Rn Antagonist 6.9 – 7.0 pKi 38
pKi 6.9 – 7.0 [38]
olanzapine Rn Antagonist 6.8 – 7.0 pKi 21,36
pKi 6.8 – 7.0 [21,36]
cyproheptadine Hs Antagonist 6.9 pKi 3
pKi 6.9 [3]
dihydroergotamine Rn Antagonist 6.8 pKi 37
pKi 6.8 [37]
MPDT Hs Antagonist 6.8 pKi 10
pKi 6.8 [10]
ketanserin Rn Antagonist 6.6 – 6.7 pKi 38
pKi 6.6 – 6.7 [38]
olanzapine Hs Antagonist 6.5 pKi 47
pKi 6.5 [47]
dihydroergocryptine Rn Antagonist 6.5 pKi 37
pKi 6.5 [37]
haloperidol Rn Antagonist 6.3 – 6.6 pKi 21,36-37
pKi 6.3 – 6.6 [21,36-37]
haloperidol Hs Antagonist 6.3 – 6.6 pKi 18
pKi 6.3 – 6.6 [18]
buspirone Mm Antagonist 6.4 pKi 33
pKi 6.4 [33]
ketanserin Mm Antagonist 6.4 pKi 33
pKi 6.4 [33]
amitriptyline Mm Antagonist 6.4 pKi 33
pKi 6.4 [33]
sumatriptan Rn Antagonist 6.2 – 6.6 pKi 37-38
pKi 6.2 – 6.6 [37-38]
TFMPP Mm Antagonist 6.3 pKi 33
pKi 6.3 [33]
haloperidol Mm Antagonist 6.3 pKi 33
pKi 6.3 [33]
ketanserin Hs Antagonist 5.9 – 6.5 pKi 3,18,22,47
pKi 5.9 – 6.5 [3,18,22,47]
sumatriptan Hs Antagonist 5.7 – 6.0 pKi 3,18
pKi 5.7 – 6.0 [3,18]
yohimbine Hs Antagonist 5.6 pKi 3
pKi 5.6 [3]
SB 207710 Hs Antagonist 5.3 – 5.5 pKi 22
pKi 5.3 – 5.5 [22]
chlorpromazine Mm Inverse agonist 5.3 pKi 33
pKi 5.3 [33]
View species-specific antagonist tables
Allosteric Regulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
oleamide Hs Negative 8.6 pKd 15
pKd 8.6 [15]
Primary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  2
Tissue Distribution
Amygdala, aorta, cerebral cortex, hippocampus, thalamus, small intestine >> spleen, pancreas, stomach, kidney.
Species:  Human
Technique:  RT-PCR.
References:  18
CNS: trigeminal ganglia.
Species:  Human
Technique:  RT-PCR.
References:  45
CNS: suprachiasmatic nucleus.
Species:  Human
Technique:  Electron microscopic immunocytochemistry.
References:  4
Coronary artery > brain > descending colon, ileum.
Species:  Human
Technique:  RT-PCR.
References:  3
Heart: ventricle wall > epicardium > atrium, coronary artery.
Species:  Human
Technique:  RT-PCR.
References:  28
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  42
CNS: lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  32
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 cAMP levels in HeLa cells transfected with the rat 5-HT7 receptor.
Species:  Rat
Tissue:  HeLa cells.
Response measured:  Stimulation of cAMP accumulation.
References:  25
Measurement of cAMP levels in rat hippocampal homogenates endogenously expressing the rat 5-HT7 receptor.
Species:  Rat
Tissue:  Hippocampal cells.
Response measured:  Stimulation of cAMP accumulation.
References:  26
Measurement of cAMP levels in LM(tk-) cells transfected with the human 5-HT7(a) receptor.
Species:  Human
Tissue:  LM(tk-) cells.
Response measured:  Stimulation of cAMP accumulation.
References:  1
Measurement of cAMP levels in COS-7 cells transfected with the human 5-HT7 receptor.
Species:  Human
Tissue:  COS-7 cells.
Response measured:  Stimulation of cAMP accumulation.
References:  3
Measurement of ERK1/2 activity in HEK 293 cells transfected with the human 5-HT7 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  ERK1/2 activation via a pathway involving PKA and Ras.
References:  29
Measurement of ERK1/2 activity in HEK 293 cells transfected with the human 5-HT7 receptor.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  ERK1/2 activation via a pathway involving PKA and Ras.
References:  29
Physiological Functions
Nociception.
Species:  Rat
Tissue:  In vivo.
References:  35
Antinociception.
Species:  Rat
Tissue:  In vivo (parafascicular nucleus).
References:  14
Hypotension.
Species:  Rat
Tissue:  In vivo.
References:  7,44
Depolarisation via an increase in hyperpolarisation-activated conductance.
Species:  Rat
Tissue:  Anterodorsal nucleus of the thalamus.
References:  8
Hypothermia.
Species:  Mouse
Tissue:  In vivo.
References:  12,16
Modulation of REM sleep.
Species:  Rat
Tissue:  In vivo.
References:  48
Regulation of suprachiasmatic nuclei neuronal firing (potential role in the control of circadian rhythms).
Species:  Rat
Tissue:  Hypothalamic slices.
References:  40
Regulation of LH release.
Species:  Rat
Tissue:  In vivo (zona incerta of dorsal hypothalamus).
References:  39
Regulation of vagal outflow to the heart.
Species:  Rat
Tissue:  In vivo.
References:  20
Role in learning and memory.
Species:  Rat
Tissue:  In vivo.
References:  30
Regulation of locomotor activity.
Species:  Mouse
Tissue:  In vivo.
References:  43
Physiological Consequences of Altering Gene Expression
5-HT7 receptor knockout mice have an abolished hypothermic response upon agonist administration.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  12,16
Hypothalamic slices from 5-HT7 receptor knockout mice suggest a reduced circadian rhythm phase shift in response to agonist stimulation.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  11
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Htr7tm1Sut Htr7tm1Sut/Htr7tm1Sut
B6.129X1-Htr7
MGI:99841  MP:0001777 abnormal body temperature regulation PMID: 12529502 
Htr7tm1Mrg Htr7tm1Mrg/Htr7tm1Mrg
involves: 129S/SvEv * C57BL/6
MGI:99841  MP:00