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5-HT7 receptor

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 12

Nomenclature: 5-HT7 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 7 479 10q23.31 HTR7 5-hydroxytryptamine receptor 7 55
Mouse 7 448 19 30.3 cM Htr7 5-hydroxytryptamine (serotonin) receptor 7 46
Rat 7 448 1q53 Htr7 5-hydroxytryptamine receptor 7 38,50,52
Previous and Unofficial Names Click here for help
5-HTx | 5-HT1Y | 5-HT7 | GPRFO | serotonin receptor 7 | 5-hydroxytryptamine (serotonin) receptor 7, adenylate cyclase-coupled
Database Links Click here for help
Specialist databases
GPCRdb 5ht7r_human (Hs), 5ht7r_mouse (Mm), 5ht7r_rat (Rn)
Other databases
Alphafold P34969 (Hs), P32304 (Mm), P32305 (Rn)
ChEMBL Target CHEMBL3155 (Hs), CHEMBL4764 (Mm), CHEMBL3223 (Rn)
DrugBank Target P34969 (Hs)
Ensembl Gene ENSG00000148680 (Hs), ENSMUSG00000024798 (Mm), ENSRNOG00000018827 (Rn)
Entrez Gene 3363 (Hs), 15566 (Mm), 65032 (Rn)
Human Protein Atlas ENSG00000148680 (Hs)
KEGG Gene hsa:3363 (Hs), mmu:15566 (Mm), rno:65032 (Rn)
OMIM 182137 (Hs)
Pharos P34969 (Hs)
RefSeq Nucleotide NM_000872 (Hs), NM_008315 (Mm), NM_022938 (Rn)
RefSeq Protein NP_000863 (Hs), NP_032341 (Mm), NP_075227 (Rn)
UniProtKB P34969 (Hs), P32304 (Mm), P32305 (Rn)
Wikipedia HTR7 (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]5-CT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 9.4 pKd 60
⤷ pKd 9.4 (Kd 4x10-10 M) [60]
[125I]LSD Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Full agonist 8.9 pKd 38
⤷ pKd 8.9 [38]
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.5 – 8.6 pKd 55
⤷ pKd 8.5 – 8.6 (Kd 3.16x10-9 – 2.51x10-9 M) [55]
[3H]5-HT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.1 – 9.0 pKd 5,55
⤷ pKd 8.1 – 9.0 (Kd 7.94x10-9 – 1x10-9 M) [5,55]
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Full agonist 8.2 pKd 34
⤷ pKd 8.2 [34]
LP-12 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Agonist 9.9 pKi 35
⤷ pKi 9.9 (Ki 1.3x10-10 M) [35]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 9.5 – 9.9 pKi 50,52
⤷ pKi 9.5 – 9.9 [50,52]
LP-44 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Agonist 9.7 pKi 35
⤷ pKi 9.7 (Ki 2.2x10-10 M) [35]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.0 – 10.0 pKi 5,25,32,61
⤷ pKi 9.0 – 10.0 [5,25,32,61]
LP-211 Small molecule or natural product Rn Agonist 9.2 pKi 36
⤷ pKi 9.2 (Ki 5.8x10-10 M) [36]
AS-19 Small molecule or natural product Primary target of this compound Hs Agonist 9.2 pKi 30
⤷ pKi 9.2 (Ki 6x10-10 M) [30]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Full agonist 9.0 pKi 46
⤷ pKi 9.0 [46]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.8 – 9.2 pKi 50,52
⤷ pKi 8.8 – 9.2 [50,52]
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 8.7 – 9.2 pKi 50,52
⤷ pKi 8.7 – 9.2 [50,52]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.3 – 9.5 pKi 5,25,32
⤷ pKi 8.3 – 9.5 [5,25,32]
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 8.1 – 9.6 pKi 5,19,25,32,61
⤷ pKi 8.1 – 9.6 [5,19,25,32,61]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.2 – 9.3 pKi 50,52
⤷ pKi 8.2 – 9.3 [50,52]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Rn Full agonist 8.3 – 9.0 pKi 52
⤷ pKi 8.3 – 9.0 [52]
E55888 Small molecule or natural product Hs Full agonist 8.6 pKi 8
⤷ pKi 8.6 [8]
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 Mm Full agonist 8.3 pKi 46
⤷ pKi 8.3 [46]
dipropyl-5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 – 8.4 pKi 25
⤷ pKi 8.2 – 8.4 [25]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Full agonist 8.2 pKi 46
⤷ pKi 8.2 [46]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 pKi 50
⤷ pKi 8.0 [50]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.8 pKi 34
⤷ pKi 7.8 [34]
OPC 4392 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.7 pKi 34
⤷ pKi 7.7 [34]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.3 – 8.0 pKi 52
⤷ pKi 7.3 – 8.0 [52]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.5 – 7.8 pKi 52
⤷ pKi 7.5 – 7.8 [52]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.5 – 7.7 pKi 52
⤷ pKi 7.5 – 7.7 [52]
5-MeO-DMT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.4 – 7.7 pKi 52
⤷ pKi 7.4 – 7.7 [52]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.3 – 7.5 pKi 50,52
⤷ pKi 7.3 – 7.5 [50,52]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.1 pKi 5
⤷ pKi 7.1 [5]
bufotenine Small molecule or natural product Click here for species-specific activity table Mm Full agonist 7.0 pKi 46
⤷ pKi 7.0 [46]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.3 – 7.6 pKi 5,25,32,61
⤷ pKi 6.3 – 7.6 [5,25,32,61]
RU 24969 Small molecule or natural product Click here for species-specific activity table Mm Full agonist 6.9 pKi 46
⤷ pKi 6.9 [46]
xanomeline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.9 pKi 63
⤷ pKi 6.9 [63]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.8 pKi 5
⤷ pKi 6.8 [5]
2-MPP Small molecule or natural product Rn Full agonist 6.6 – 6.9 pKi 52
⤷ pKi 6.6 – 6.9 [52]
DM-1451 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.7 pKi 34
⤷ pKi 6.7 [34]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Mm Full agonist 6.6 pKi 46
⤷ pKi 6.6 [46]
EMDT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.5 pKi 16
⤷ pKi 6.5 [16]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.4 – 6.6 pKi 52
⤷ pKi 6.4 – 6.6 [52]
TFMPP Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.3 – 6.6 pKi 52
⤷ pKi 6.3 – 6.6 [52]
buspirone Small molecule or natural product Approved drug Ligand has a PDB structure Rn Partial agonist 6.4 pKi 50
⤷ pKi 6.4 [50]
cisapride Small molecule or natural product Approved drug Click here for species-specific activity table Mm Full agonist 5.8 pKi 46
⤷ pKi 5.8 [46]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.5 pKi 40
⤷ pKi 5.5 [40]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.3 pKi 44
⤷ pKi 5.3 [44]
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
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.9 – 9.0 pKd 31,49
⤷ pKd 8.9 – 9.0 [31,49]
[3H]SB269970 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.9 pKd 60
⤷ pKd 8.9 (Kd 1.2x10-9 M) [60]
lurasidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.3 pKi 24
⤷ pKi 9.3 (Ki 4.95x10-10 M) [24]
pimozide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.3 pKi 49
⤷ pKi 9.3 [49]
methiothepin Small molecule or natural product Click here for species-specific activity table Rn Antagonist 9.0 – 9.4 pKi 52
⤷ pKi 9.0 – 9.4 [52]
tiospirone Small molecule or natural product Click here for species-specific activity table Rn Antagonist 9.2 pKi 49
⤷ pKi 9.2 [49]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 – 9.4 pKi 5,25,32,61
⤷ pKi 8.4 – 9.4 [5,25,32,61]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.8 pKi 49
⤷ pKi 8.8 [49]
SB269970 Small molecule or natural product Hs Antagonist 8.6 – 8.9 pKi 60
⤷ pKi 8.6 – 8.9 [60]
SB656104 Small molecule or natural product Hs Antagonist 8.7 pKi 13
⤷ pKi 8.7 (Ki 1.9x10-9 M) [13]
DR-4004 Small molecule or natural product Primary target of this compound Hs Antagonist 8.7 pKi 15,28
⤷ pKi 8.7 (Ki 2x10-9 M) [15,28]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 8.9 pKi 5,25,32
⤷ pKi 8.2 – 8.9 [5,25,32]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.3 – 8.7 pKi 47,61
⤷ pKi 8.3 – 8.7 [47,61]
ziprasidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.4 pKi 47
⤷ pKi 8.4 [47]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.4 pKi 47
⤷ pKi 8.4 [47]
pirenperone Small molecule or natural product Hs Antagonist 8.2 – 8.5 pKi 25
⤷ pKi 8.2 – 8.5 [25]
fluperlapine Small molecule or natural product Click here for species-specific activity table Rn Inverse agonist 8.3 pKi 49
⤷ pKi 8.3 [49]
methiothepin Small molecule or natural product Click here for species-specific activity table Mm Antagonist 8.2 pKi 46
⤷ pKi 8.2 [46]
JNJ-18038683 Small molecule or natural product Primary target of this compound Hs Antagonist 8.2 pKi 7
⤷ pKi 8.2 [7]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 8.1 pKi 49
⤷ pKi 8.1 [49]
EGIS-11150 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.1 pKi 14
⤷ pKi 8.1 (Ki 9x10-9 M) [14]
dihydroergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.0 pKi 5
⤷ pKi 8.0 [5]
2-bromo-LSD Small molecule or natural product Mm Antagonist 8.0 pKi 46
⤷ pKi 8.0 [46]
metergoline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.2 – 8.7 pKi 50,52
⤷ pKi 7.2 – 8.7 [50,52]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.7 – 8.2 pKi 52
⤷ pKi 7.7 – 8.2 [52]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 7.9 pKi 46
⤷ pKi 7.9 [46]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.9 pKi 52
⤷ pKi 7.9 [52]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.9 pKi 47
⤷ pKi 7.9 [47]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.7 – 8.0 pKi 49-50
⤷ pKi 7.7 – 8.0 [49-50]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 – 8.2 pKi 5,25,32,61
⤷ pKi 7.5 – 8.2 [5,25,32,61]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.7 – 7.8 pKi 52
⤷ pKi 7.7 – 7.8 [52]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 7.2 – 8.2 pKi 31,49-50,52
⤷ pKi 7.2 – 8.2 [31,49-50,52]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.7 pKi 31
⤷ pKi 7.7 [31]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 7.6 pKi 47
⤷ pKi 7.6 [47]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 7.6 pKi 49
⤷ pKi 7.6 [49]
mesulergine Small molecule or natural product Mm Antagonist 7.6 pKi 46
⤷ pKi 7.6 [46]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.6 pKi 49
⤷ pKi 7.6 [49]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 7.2 – 7.8 pKi 32,47,61
⤷ pKi 7.2 – 7.8 [32,47,61]
(+)-butaclamol Small molecule or natural product Mm Antagonist 7.5 pKi 46
⤷ pKi 7.5 [46]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 – 8.0 pKi 5,25,32
⤷ pKi 7.0 – 8.0 [5,25,32]
metergoline Small molecule or natural product Mm Antagonist 7.5 pKi 46
⤷ pKi 7.5 [46]
2-bromo-LSD Small molecule or natural product Hs Antagonist 7.5 pKi 5
⤷ pKi 7.5 [5]
fluperlapine Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 7.5 pKi 47
⤷ pKi 7.5 [47]
SB 258719 Small molecule or natural product Hs Inverse agonist 7.5 pKi 61
⤷ pKi 7.5 (Ki 3.16x10-8 M) [61]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.1 – 7.8 pKi 5,25,32
⤷ pKi 7.1 – 7.8 [5,25,32]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 – 7.6 pKi 25
⤷ pKi 7.3 – 7.6 [25]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Inverse agonist 7.4 pKi 46
⤷ pKi 7.4 [46]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.4 pKi 49
⤷ pKi 7.4 [49]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 7.3 pKi 46
⤷ pKi 7.3 [46]
cyproheptadine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.1 – 7.5 pKi 50,52
⤷ pKi 7.1 – 7.5 [50,52]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.2 pKi 19
⤷ pKi 7.2 [19]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 7.2 pKi 46
⤷ pKi 7.2 [46]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.2 pKi 49
⤷ pKi 7.2 [49]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.0 – 7.4 pKi 50,52
⤷ pKi 7.0 – 7.4 [50,52]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.2 pKi 47
⤷ pKi 7.2 [47]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.8 – 7.4 pKi 5,32
⤷ pKi 6.8 – 7.4 [5,32]
loxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.8 – 7.4 pKi 49,52
⤷ pKi 6.8 – 7.4 [49,52]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.1 pKi 47
⤷ pKi 7.1 [47]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.0 pKi 50
⤷ pKi 7.0 [50]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 pKi 26
⤷ pKi 7.0 [26]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Mm Antagonist 7.0 pKi 46
⤷ pKi 7.0 [46]
dihydroergocryptine Small molecule or natural product Mm Antagonist 7.0 pKi 46
⤷ pKi 7.0 [46]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.9 – 7.0 pKi 52
⤷ pKi 6.9 – 7.0 [52]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.8 – 7.0 pKi 31,49
⤷ pKi 6.8 – 7.0 [31,49]
cyproheptadine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.9 pKi 5
⤷ pKi 6.9 [5]
MPDT Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 16
⤷ pKi 6.8 [16]
dihydroergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.8 pKi 50
⤷ pKi 6.8 [50]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.6 – 6.7 pKi 52
⤷ pKi 6.6 – 6.7 [52]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.5 pKi 61
⤷ pKi 6.5 [61]
dihydroergocryptine Small molecule or natural product Rn Antagonist 6.5 pKi 50
⤷ pKi 6.5 [50]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.3 – 6.6 pKi 25
⤷ pKi 6.3 – 6.6 [25]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.3 – 6.6 pKi 31,49-50
⤷ pKi 6.3 – 6.6 [31,49-50]
buspirone Small molecule or natural product Approved drug Ligand has a PDB structure Mm Antagonist 6.4 pKi 46
⤷ pKi 6.4 [46]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 6.4 pKi 46
⤷ pKi 6.4 [46]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 6.4 pKi 46
⤷ pKi 6.4 [46]
sumatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.2 – 6.6 pKi 50,52
⤷ pKi 6.2 – 6.6 [50,52]
vortioxetine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist 6.3 pKi 4
⤷ pKi 6.3 (Ki 4.5x10-7 M) [4]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 6.3 pKi 46
⤷ pKi 6.3 [46]
TFMPP Small molecule or natural product Click here for species-specific activity table Mm Antagonist 6.3 pKi 46
⤷ pKi 6.3 [46]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.9 – 6.5 pKi 5,25,32,61
⤷ pKi 5.9 – 6.5 [5,25,32,61]
sumatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.7 – 6.0 pKi 5,25
⤷ pKi 5.7 – 6.0 [5,25]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.6 pKi 5
⤷ pKi 5.6 [5]
SB 207710 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.3 – 5.5 pKi 32
⤷ pKi 5.3 – 5.5 [32]
chlorpromazine Small molecule or natural product Approved drug Ligand has a PDB structure Mm Inverse agonist 5.3 pKi 46
⤷ pKi 5.3 [46]
View species-specific antagonist tables
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
oleamide Small molecule or natural product Hs Negative 8.6 pKd 21
⤷ pKd 8.6 [21]
Immunopharmacology Comments
5-HT has been shown to alter cytokine production by dendritic cells via 5-HT4 and 5-HT7 receptors [2]. 5-HT7 receptor plays a vital role in 5-HT-stimulated generation of a more inflammatory adaptive immune response, particulary in relation to gut inflammation [29,37].
Cell Type Associations
Immuno Cell Type:  T cells
Comment:  Involved in T cell proliferation.
References:  2
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   neutrophil (CL:0000775)
References:  51
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   macrophage (CL:0000235)
monocyte (CL:0000576)
Comment:  5-HT7 receptor activation has been shown to promote anti-inflammatory macrophage polarization.
References:  2,12,51
Immuno Cell Type:  Dendritic cells
Cell Ontology Term:   dendritic cell (CL:0000451)
Comment:  Involved in cytokine production/release from DCs.
References:  2,51
Immuno Cell Type:  B cells
Cell Ontology Term:   B cell (CL:0000236)
References:  51
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family Adenylyl cyclase stimulation
References:  3
Tissue Distribution Click here for help
Amygdala, aorta, cerebral cortex, hippocampus, thalamus, small intestine >> spleen, pancreas, stomach, kidney.
Species:  Human
Technique:  RT-PCR.
References:  25
CNS: trigeminal ganglia.
Species:  Human
Technique:  RT-PCR.
References:  58
CNS: suprachiasmatic nucleus.
Species:  Human
Technique:  Electron microscopic immunocytochemistry.
References:  6
Coronary artery > brain > descending colon, ileum.
Species:  Human
Technique:  RT-PCR.
References:  5
Heart: ventricle wall > epicardium > atrium, coronary artery.
Species:  Human
Technique:  RT-PCR.
References:  41
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  56
CNS: lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  45
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 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:  42
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:  39
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:  5
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:  38
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:  42
Physiological Functions Click here for help
Nociception.
Species:  Rat
Tissue:  In vivo.
References:  48
Antinociception.
Species:  Rat
Tissue:  In vivo (parafascicular nucleus).
References:  20
Hypotension.
Species:  Rat
Tissue:  In vivo.
References:  10,59
Depolarisation via an increase in hyperpolarisation-activated conductance.
Species:  Rat
Tissue:  Anterodorsal nucleus of the thalamus.
References:  11
Hypothermia.
Species:  Mouse
Tissue:  In vivo.
References:  18,22
Modulation of REM sleep.
Species:  Rat
Tissue:  In vivo.
References:  62
Regulation of suprachiasmatic nuclei neuronal firing (potential role in the control of circadian rhythms).
Species:  Rat
Tissue:  Hypothalamic slices.
References:  54
Regulation of LH release.
Species:  Rat
Tissue:  In vivo (zona incerta of dorsal hypothalamus).
References:  53
Regulation of vagal outflow to the heart.
Species:  Rat
Tissue:  In vivo.
References:  27
Role in learning and memory.
Species:  Rat
Tissue:  In vivo.
References:  43
Regulation of locomotor activity.
Species:  Mouse
Tissue:  In vivo.
References:  57
Physiological Consequences of Altering Gene Expression Click here for help
5-HT7 receptor knockout mice have an abolished hypothermic response upon agonist administration.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  18,22
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:  17
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
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:0001777 abnormal body temperature regulation PMID: 12763096 
Htr7tm1Wtkn Htr7tm1Wtkn/Htr7tm1Wtkn
involves: 129S1/Sv * 129X1/SvJ * CD-1		 MGI:99841  MP:0001650 abnormal seizure response to electrical stimulation PMID: 17485199 
Htr7tm1Dgen Htr7tm1Dgen/Htr7tm1Dgen
involves: 129P2/OlaHsd * C57BL/6		 MGI:99841  MP:0003858 enhanced coordination
Htr7tm1Wtkn Htr7tm1Wtkn/Htr7tm1Wtkn
involves: 129S1/Sv * 129X1/SvJ * CD-1		 MGI:99841  MP:0009766 increased sensitivity to xenobiotic induced morbidity/mortality PMID: 17485199 
Htr7tm1Wtkn Htr7tm1Wtkn/Htr7tm1Wtkn
involves: 129S1/Sv * 129X1/SvJ * CD-1		 MGI:99841  MP:0002906 increased susceptibility to pharmacologically induced seizures PMID: 17485199 
Htr7tm1Dgen Htr7tm1Dgen/Htr7tm1Dgen
involves: 129P2/OlaHsd * C57BL/6		 MGI:99841  MP:0001973 increased thermal nociceptive threshold
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Description:  The human 5-HT7(a) receptor polymorphism Thr92 -> Lys exhibits reduced agonist binding affinities.
References:  9
Type:  Splice variants
Species:  Human
Description:  Splice variants of the 5-HT7 receptor have been found in the human brain, 5-HT7(a), 5-HT7(b) and 5-HT7(d). Differing only in the lengths of their carboxy terminal, these variants are all functional receptors.
References:  25,32-33,55
Type:  Splice variants
Species:  Rat
Description:  Splice variants of the 5-HT7 receptor have been found in rat tissues, 5-HT7(a), 5-HT7(b) and 5-HT7(c). Differing only in the lengths of their carboxy terminal, these variants are all functional receptors.
References:  23

References

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