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 43
Mouse 7 448 19 C2 Htr7 5-hydroxytryptamine (serotonin) receptor 7 35
Rat 7 448 1q53 Htr7 5-hydroxytryptamine (serotonin) receptor 7, adenylate cyclase-coupled 27,39-40
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 Ligands
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 48
pKd 9.4 (Kd 4x10-10 M) [48]
[125I]LSD Rn Full agonist 8.9 pKd 27
pKd 8.9 [27]
[3H]LSD Hs Full agonist 8.5 – 8.6 pKd 43
pKd 8.5 – 8.6 (Kd 2.51x10-9 – 3.16x10-9 M) [43]
[3H]5-HT Hs Full agonist 8.1 – 9.0 pKd 4,43
pKd 8.1 – 9.0 (Kd 1x10-9 – 7.94x10-9 M) [4,43]
[3H]LSD Rn Full agonist 8.2 pKd 26
pKd 8.2 [26]
5-CT Rn Full agonist 9.5 – 9.9 pKi 39-40
pKi 9.5 – 9.9 [39-40]
5-CT Hs Full agonist 9.0 – 10.0 pKi 4,20,24,49
pKi 9.0 – 10.0 [4,20,24,49]
5-MeOT Rn Full agonist 8.8 – 9.2 pKi 39-40
pKi 8.8 – 9.2 [39-40]
5-CT Mm Full agonist 9.0 pKi 35
pKi 9.0 [35]
5-HT Rn Full agonist 8.7 – 9.2 pKi 39-40
pKi 8.7 – 9.2 [39-40]
5-MeOT Hs Full agonist 8.3 – 9.5 pKi 4,20,24
pKi 8.3 – 9.5 [4,20,24]
5-HT Hs Full agonist 8.1 – 9.6 pKi 4,14,20,24,49
pKi 8.1 – 9.6 [4,14,20,24,49]
lisuride Rn Full agonist 8.2 – 9.3 pKi 39-40
pKi 8.2 – 9.3 [39-40]
pergolide Rn Full agonist 8.3 – 9.0 pKi 40
pKi 8.3 – 9.0 [40]
E55888 Hs Full agonist 8.6 pKi 6
pKi 8.6 [6]
5-HT Mm Full agonist 8.3 pKi 35
pKi 8.3 [35]
dipropyl-5-CT Hs Full agonist 8.2 – 8.4 pKi 20
pKi 8.2 – 8.4 [20]
5-MeOT Mm Full agonist 8.2 pKi 35
pKi 8.2 [35]
(+)-LSD Hs Full agonist 8.0 pKi 39
pKi 8.0 [39]
aripiprazole Rn Full agonist 7.8 pKi 26
pKi 7.8 [26]
OPC 4392 Rn Full agonist 7.7 pKi 26
pKi 7.7 [26]
tryptamine Rn Full agonist 7.5 – 7.8 pKi 40
pKi 7.5 – 7.8 [40]
bromocriptine Rn Full agonist 7.3 – 8.0 pKi 40
pKi 7.3 – 8.0 [40]
1-naphthylpiperazine Rn Full agonist 7.5 – 7.7 pKi 40
pKi 7.5 – 7.7 [40]
5-MeO-DMT Rn Full agonist 7.4 – 7.7 pKi 40
pKi 7.4 – 7.7 [40]
8-OH-DPAT Rn Full agonist 7.3 – 7.5 pKi 39-40
pKi 7.3 – 7.5 [39-40]
1-naphthylpiperazine Hs Full agonist 7.1 pKi 4
pKi 7.1 [4]
bufotenine Mm Full agonist 7.0 pKi 35
pKi 7.0 [35]
8-OH-DPAT Hs Full agonist 6.3 – 7.6 pKi 4,20,24,49
pKi 6.3 – 7.6 [4,20,24,49]
xanomeline Hs Full agonist 6.9 pKi 51
pKi 6.9 [51]
RU 24969 Mm Full agonist 6.9 pKi 35
pKi 6.9 [35]
tryptamine Hs Full agonist 6.8 pKi 4
pKi 6.8 [4]
2-MPP Rn Full agonist 6.6 – 6.9 pKi 40
pKi 6.6 – 6.9 [40]
DM-1451 Rn Full agonist 6.7 pKi 26
pKi 6.7 [26]
8-OH-DPAT Mm Full agonist 6.6 pKi 35
pKi 6.6 [35]
m-CPP Rn Full agonist 6.4 – 6.6 pKi 40
pKi 6.4 – 6.6 [40]
EMDT Hs Full agonist 6.5 pKi 11
pKi 6.5 [11]
TFMPP Rn Full agonist 6.3 – 6.6 pKi 40
pKi 6.3 – 6.6 [40]
buspirone Rn Partial agonist 6.4 pKi 39
pKi 6.4 [39]
cisapride Mm Full agonist 5.8 pKi 35
pKi 5.8 [35]
SL65.0155 Hs Partial agonist 5.5 pKi 29
pKi 5.5 [29]
LY344864 Hs Full agonist 5.3 pKi 33
pKi 5.3 [33]
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 23,38
pKd 8.9 – 9.0 [23,38]
[3H]SB269970 Hs Antagonist 8.92 pKd 48
pKd 8.92 (Kd 1.2x10-9 M) [48]
lurasidone Hs Antagonist 9.31 pKi 19
pKi 9.31 (Ki 4.95x10-10 M) [19]
pimozide Rn Antagonist 9.3 pKi 38
pKi 9.3 [38]
methiothepin Rn Antagonist 9.0 – 9.4 pKi 40
pKi 9.0 – 9.4 [40]
tiospirone Rn Antagonist 9.2 pKi 38
pKi 9.2 [38]
methiothepin Hs Antagonist 8.4 – 9.4 pKi 4,20,24,49
pKi 8.4 – 9.4 [4,20,24,49]
zotepine Rn Inverse agonist 8.8 pKi 38
pKi 8.8 [38]
SB269970 Hs Antagonist 8.6 – 8.9 pKi 48
pKi 8.6 – 8.9 [48]
SB656104 Hs Antagonist 8.7 pKi 10
pKi 8.7 (Ki 1.9x10-9 M) [10]
metergoline Hs Antagonist 8.2 – 8.9 pKi 4,20,24
pKi 8.2 – 8.9 [4,20,24]
risperidone Hs Inverse agonist 8.3 – 8.7 pKi 36,49
pKi 8.3 – 8.7 [36,49]
ziprasidone Hs Inverse agonist 8.4 pKi 36
pKi 8.4 [36]
zotepine Hs Inverse agonist 8.4 pKi 36
pKi 8.4 [36]
pirenperone Hs Antagonist 8.2 – 8.5 pKi 20
pKi 8.2 – 8.5 [20]
fluperlapine Rn Inverse agonist 8.3 pKi 38
pKi 8.3 [38]
methiothepin Mm Antagonist 8.2 pKi 35
pKi 8.2 [35]
fluphenazine Rn Inverse agonist 8.1 pKi 38
pKi 8.1 [38]
2-Br-LSD Mm Antagonist 8.0 pKi 35
pKi 8.0 [35]
dihydroergotamine Hs Antagonist 8.0 pKi 4
pKi 8.0 [4]
metergoline Rn Antagonist 7.2 – 8.7 pKi 39-40
pKi 7.2 – 8.7 [39-40]
mesulergine Rn Antagonist 7.7 – 8.2 pKi 40
pKi 7.7 – 8.2 [40]
methysergide Rn Antagonist 7.9 pKi 40
pKi 7.9 [40]
methysergide Mm Antagonist 7.9 pKi 35
pKi 7.9 [35]
fluphenazine Hs Inverse agonist 7.9 pKi 36
pKi 7.9 [36]
mesulergine Hs Antagonist 7.5 – 8.2 pKi 4,20,24,49
pKi 7.5 – 8.2 [4,20,24,49]
spiperone Rn Antagonist 7.7 – 8.0 pKi 38-39
pKi 7.7 – 8.0 [38-39]
ritanserin Rn Antagonist 7.7 – 7.8 pKi 40
pKi 7.7 – 7.8 [40]
iloperidone Rn Antagonist 7.7 pKi 23
pKi 7.7 [23]
clozapine Rn Inverse agonist 7.2 – 8.2 pKi 23,38-40
pKi 7.2 – 8.2 [23,38-40]
mesulergine Mm Antagonist 7.6 pKi 35
pKi 7.6 [35]
perphenazine Rn Inverse agonist 7.6 pKi 38
pKi 7.6 [38]
chlorpromazine Rn Inverse agonist 7.6 pKi 38
pKi 7.6 [38]
chlorpromazine Hs Inverse agonist 7.6 pKi 36
pKi 7.6 [36]
metergoline Mm Antagonist 7.5 pKi 35
pKi 7.5 [35]
fluperlapine Hs Inverse agonist 7.5 pKi 36
pKi 7.5 [36]
spiperone Hs Antagonist 7.0 – 8.0 pKi 4,20,24
pKi 7.0 – 8.0 [4,20,24]
2-Br-LSD Hs Antagonist 7.5 pKi 4
pKi 7.5 [4]
clozapine Hs Inverse agonist 7.2 – 7.8 pKi 24,36,49
pKi 7.2 – 7.8 [24,36,49]
(+)-butaclamol Mm Antagonist 7.5 pKi 35
pKi 7.5 [35]
SB 258719 Hs Inverse agonist 7.5 pKi 49
pKi 7.5 [49]
methysergide Hs Antagonist 7.1 – 7.8 pKi 4,20,24
pKi 7.1 – 7.8 [4,20,24]
mianserin Hs Antagonist 7.3 – 7.6 pKi 20
pKi 7.3 – 7.6 [20]
amoxapine Rn Antagonist 7.4 pKi 38
pKi 7.4 [38]
clozapine Mm Inverse agonist 7.4 pKi 35
pKi 7.4 [35]
cyproheptadine Rn Antagonist 7.1 – 7.5 pKi 39-40
pKi 7.1 – 7.5 [39-40]
ergotamine Mm Antagonist 7.3 pKi 35
pKi 7.3 [35]
mianserin Rn Antagonist 7.0 – 7.4 pKi 39-40
pKi 7.0 – 7.4 [39-40]
thioridazine Rn Inverse agonist 7.2 pKi 38
pKi 7.2 [38]
perphenazine Hs Inverse agonist 7.2 pKi 36
pKi 7.2 [36]
spiperone Mm Antagonist 7.2 pKi 35
pKi 7.2 [35]
cyamemazine Hs Antagonist 7.2 pKi 14
pKi 7.2 [14]
ritanserin Hs Antagonist 6.8 – 7.4 pKi 4,24
pKi 6.8 – 7.4 [4,24]
loxapine Rn Antagonist 6.8 – 7.4 pKi 38,40
pKi 6.8 – 7.4 [38,40]
thioridazine Hs Inverse agonist 7.1 pKi 36
pKi 7.1 [36]
mianserin Mm Antagonist 7.0 pKi 35
pKi 7.0 [35]
iloperidone Hs Antagonist 7.0 pKi 21
pKi 7.0 [21]
(+)-butaclamol Rn Antagonist 7.0 pKi 39
pKi 7.0 [39]
dihydroergocryptine Mm Antagonist 7.0 pKi 35
pKi 7.0 [35]
amitriptyline Rn Antagonist 6.9 – 7.0 pKi 40
pKi 6.9 – 7.0 [40]
olanzapine Rn Antagonist 6.8 – 7.0 pKi 23,38
pKi 6.8 – 7.0 [23,38]
cyproheptadine Hs Antagonist 6.9 pKi 4
pKi 6.9 [4]
dihydroergotamine Rn Antagonist 6.8 pKi 39
pKi 6.8 [39]
MPDT Hs Antagonist 6.8 pKi 11
pKi 6.8 [11]
ketanserin Rn Antagonist 6.6 – 6.7 pKi 40
pKi 6.6 – 6.7 [40]
olanzapine Hs Antagonist 6.5 pKi 49
pKi 6.5 [49]
dihydroergocryptine Rn Antagonist 6.5 pKi 39
pKi 6.5 [39]
haloperidol Rn Antagonist 6.3 – 6.6 pKi 23,38-39
pKi 6.3 – 6.6 [23,38-39]
haloperidol Hs Antagonist 6.3 – 6.6 pKi 20
pKi 6.3 – 6.6 [20]
buspirone Mm Antagonist 6.4 pKi 35
pKi 6.4 [35]
ketanserin Mm Antagonist 6.4 pKi 35
pKi 6.4 [35]
amitriptyline Mm Antagonist 6.4 pKi 35
pKi 6.4 [35]
sumatriptan Rn Antagonist 6.2 – 6.6 pKi 39-40
pKi 6.2 – 6.6 [39-40]
vortioxetine Hs Antagonist 6.35 pKi 3
pKi 6.35 (Ki 4.5x10-7 M) [3]
TFMPP Mm Antagonist 6.3 pKi 35
pKi 6.3 [35]
haloperidol Mm Antagonist 6.3 pKi 35
pKi 6.3 [35]
ketanserin Hs Antagonist 5.9 – 6.5 pKi 4,20,24,49
pKi 5.9 – 6.5 [4,20,24,49]
sumatriptan Hs Antagonist 5.7 – 6.0 pKi 4,20
pKi 5.7 – 6.0 [4,20]
yohimbine Hs Antagonist 5.6 pKi 4
pKi 5.6 [4]
SB 207710 Hs Antagonist 5.3 – 5.5 pKi 24
pKi 5.3 – 5.5 [24]
chlorpromazine Mm Inverse agonist 5.3 pKi 35
pKi 5.3 [35]
View species-specific antagonist tables
Allosteric Modulators
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 16
pKd 8.6 [16]
Primary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  2
Tissue Distribution
Heart: ventricle wall > epicardium > atrium, coronary artery.
Species:  Human
Technique:  RT-PCR.
References:  30
CNS: trigeminal ganglia.
Species:  Human
Technique:  RT-PCR.
References:  47
CNS: suprachiasmatic nucleus.
Species:  Human
Technique:  Electron microscopic immunocytochemistry.
References:  5
Amygdala, aorta, cerebral cortex, hippocampus, thalamus, small intestine >> spleen, pancreas, stomach, kidney.
Species:  Human
Technique:  RT-PCR.
References:  20
Coronary artery > brain > descending colon, ileum.
Species:  Human
Technique:  RT-PCR.
References:  4
CNS: lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  34
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.