5-HT<sub>7</sub> receptor | 5-Hydroxytryptamine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

5-HT7 receptor

Target id: 12

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.  » Email us

   GtoImmuPdb view: OFF :     5-HT7 receptor has curated GtoImmuPdb data

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 receptor 7 54
Mouse 7 448 19 C2 Htr7 5-hydroxytryptamine (serotonin) receptor 7 45
Rat 7 448 1q53 Htr7 5-hydroxytryptamine receptor 7 37,49,51
Previous and Unofficial Names
5-HTx | 5-HT1Y | 5-HT7 | GPRFO | serotonin receptor 7 | 5-hydroxytryptamine (serotonin) receptor 7, adenylate cyclase-coupled
Database Links
Specialist databases
GPCRDB 5ht7r_human (Hs), 5ht7r_mouse (Mm), 5ht7r_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
5-hydroxytryptamine

Download all structure-activity data for this target as a CSV file

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 59
pKd 9.4 (Kd 4x10-10 M) [59]
[125I]LSD Rn Full agonist 8.9 pKd 37
pKd 8.9 [37]
[3H]LSD Hs Full agonist 8.5 – 8.6 pKd 54
pKd 8.5 – 8.6 (Kd 3.16x10-9 – 2.51x10-9 M) [54]
[3H]5-HT Hs Full agonist 8.1 – 9.0 pKd 5,54
pKd 8.1 – 9.0 (Kd 7.94x10-9 – 1x10-9 M) [5,54]
[3H]LSD Rn Full agonist 8.2 pKd 33
pKd 8.2 [33]
LP-12 Hs Agonist 9.9 pKi 34
pKi 9.9 (Ki 1.3x10-10 M) [34]
5-CT Rn Full agonist 9.5 – 9.9 pKi 49,51
pKi 9.5 – 9.9 [49,51]
LP-44 Hs Agonist 9.7 pKi 34
pKi 9.7 (Ki 2.2x10-10 M) [34]
5-CT Hs Full agonist 9.0 – 10.0 pKi 5,24,31,60
pKi 9.0 – 10.0 [5,24,31,60]
LP-211 Rn Agonist 9.2 pKi 35
pKi 9.2 (Ki 5.8x10-10 M) [35]
AS-19 Hs Agonist 9.2 pKi 29
pKi 9.2 (Ki 6x10-10 M) [29]
5-CT Mm Full agonist 9.0 pKi 45
pKi 9.0 [45]
5-MeOT Rn Full agonist 8.8 – 9.2 pKi 49,51
pKi 8.8 – 9.2 [49,51]
5-hydroxytryptamine Rn Full agonist 8.7 – 9.2 pKi 49,51
pKi 8.7 – 9.2 [49,51]
5-MeOT Hs Full agonist 8.3 – 9.5 pKi 5,24,31
pKi 8.3 – 9.5 [5,24,31]
5-hydroxytryptamine Hs Full agonist 8.1 – 9.6 pKi 5,18,24,31,60
pKi 8.1 – 9.6 [5,18,24,31,60]
lisuride Rn Full agonist 8.2 – 9.3 pKi 49,51
pKi 8.2 – 9.3 [49,51]
pergolide Rn Full agonist 8.3 – 9.0 pKi 51
pKi 8.3 – 9.0 [51]
E55888 Hs Full agonist 8.6 pKi 8
pKi 8.6 [8]
5-hydroxytryptamine Mm Full agonist 8.3 pKi 45
pKi 8.3 [45]
dipropyl-5-CT Hs Full agonist 8.2 – 8.4 pKi 24
pKi 8.2 – 8.4 [24]
5-MeOT Mm Full agonist 8.2 pKi 45
pKi 8.2 [45]
(+)-LSD Hs Full agonist 8.0 pKi 49
pKi 8.0 [49]
aripiprazole Rn Partial agonist 7.8 pKi 33
pKi 7.8 [33]
OPC 4392 Rn Full agonist 7.7 pKi 33
pKi 7.7 [33]
bromocriptine Rn Full agonist 7.3 – 8.0 pKi 51
pKi 7.3 – 8.0 [51]
tryptamine Rn Full agonist 7.5 – 7.8 pKi 51
pKi 7.5 – 7.8 [51]
1-naphthylpiperazine Rn Full agonist 7.5 – 7.7 pKi 51
pKi 7.5 – 7.7 [51]
5-MeO-DMT Rn Full agonist 7.4 – 7.7 pKi 51
pKi 7.4 – 7.7 [51]
8-OH-DPAT Rn Full agonist 7.3 – 7.5 pKi 49,51
pKi 7.3 – 7.5 [49,51]
1-naphthylpiperazine Hs Full agonist 7.1 pKi 5
pKi 7.1 [5]
bufotenine Mm Full agonist 7.0 pKi 45
pKi 7.0 [45]
8-OH-DPAT Hs Full agonist 6.3 – 7.6 pKi 5,24,31,60
pKi 6.3 – 7.6 [5,24,31,60]
RU 24969 Mm Full agonist 6.9 pKi 45
pKi 6.9 [45]
xanomeline Hs Full agonist 6.9 pKi 62
pKi 6.9 [62]
tryptamine Hs Full agonist 6.8 pKi 5
pKi 6.8 [5]
2-MPP Rn Full agonist 6.6 – 6.9 pKi 51
pKi 6.6 – 6.9 [51]
DM-1451 Rn Full agonist 6.7 pKi 33
pKi 6.7 [33]
8-OH-DPAT Mm Full agonist 6.6 pKi 45
pKi 6.6 [45]
EMDT Hs Full agonist 6.5 pKi 15
pKi 6.5 [15]
m-chlorophenylpiperazine Rn Full agonist 6.4 – 6.6 pKi 51
pKi 6.4 – 6.6 [51]
TFMPP Rn Full agonist 6.3 – 6.6 pKi 51
pKi 6.3 – 6.6 [51]
buspirone Rn Partial agonist 6.4 pKi 49
pKi 6.4 [49]
cisapride Mm Full agonist 5.8 pKi 45
pKi 5.8 [45]
capeserod Hs Partial agonist 5.5 pKi 39
pKi 5.5 [39]
LY344864 Hs Full agonist 5.3 pKi 43
pKi 5.3 [43]
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 30,48
pKd 8.9 – 9.0 [30,48]
[3H]SB269970 Hs Antagonist 8.9 pKd 59
pKd 8.9 (Kd 1.2x10-9 M) [59]
lurasidone Hs Antagonist 9.3 pKi 23
pKi 9.3 (Ki 4.95x10-10 M) [23]
pimozide Rn Antagonist 9.3 pKi 48
pKi 9.3 [48]
methiothepin Rn Antagonist 9.0 – 9.4 pKi 51
pKi 9.0 – 9.4 [51]
tiospirone Rn Antagonist 9.2 pKi 48
pKi 9.2 [48]
methiothepin Hs Antagonist 8.4 – 9.4 pKi 5,24,31,60
pKi 8.4 – 9.4 [5,24,31,60]
zotepine Rn Inverse agonist 8.8 pKi 48
pKi 8.8 [48]
SB269970 Hs Antagonist 8.6 – 8.9 pKi 59
pKi 8.6 – 8.9 [59]
SB656104 Hs Antagonist 8.7 pKi 13
pKi 8.7 (Ki 1.9x10-9 M) [13]
DR-4004 Hs Antagonist 8.7 pKi 14,27
pKi 8.7 (Ki 2x10-9 M) [14,27]
metergoline Hs Antagonist 8.2 – 8.9 pKi 5,24,31
pKi 8.2 – 8.9 [5,24,31]
risperidone Hs Inverse agonist 8.3 – 8.7 pKi 46,60
pKi 8.3 – 8.7 [46,60]
ziprasidone Hs Inverse agonist 8.4 pKi 46
pKi 8.4 [46]
zotepine Hs Inverse agonist 8.4 pKi 46
pKi 8.4 [46]
pirenperone Hs Antagonist 8.2 – 8.5 pKi 24
pKi 8.2 – 8.5 [24]
fluperlapine Rn Inverse agonist 8.3 pKi 48
pKi 8.3 [48]
methiothepin Mm Antagonist 8.2 pKi 45
pKi 8.2 [45]
JNJ-18038683 Hs Antagonist 8.2 pKi 7
pKi 8.2 [7]
fluphenazine Rn Inverse agonist 8.1 pKi 48
pKi 8.1 [48]
dihydroergotamine Hs Antagonist 8.0 pKi 5
pKi 8.0 [5]
2-bromo-LSD Mm Antagonist 8.0 pKi 45
pKi 8.0 [45]
metergoline Rn Antagonist 7.2 – 8.7 pKi 49,51
pKi 7.2 – 8.7 [49,51]
mesulergine Rn Antagonist 7.7 – 8.2 pKi 51
pKi 7.7 – 8.2 [51]
methysergide Mm Antagonist 7.9 pKi 45
pKi 7.9 [45]
methysergide Rn Antagonist 7.9 pKi 51
pKi 7.9 [51]
fluphenazine Hs Inverse agonist 7.9 pKi 46
pKi 7.9 [46]
spiperone Rn Antagonist 7.7 – 8.0 pKi 48-49
pKi 7.7 – 8.0 [48-49]
mesulergine Hs Antagonist 7.5 – 8.2 pKi 5,24,31,60
pKi 7.5 – 8.2 [5,24,31,60]
ritanserin Rn Antagonist 7.7 – 7.8 pKi 51
pKi 7.7 – 7.8 [51]
clozapine Rn Inverse agonist 7.2 – 8.2 pKi 30,48-49,51
pKi 7.2 – 8.2 [30,48-49,51]
iloperidone Rn Antagonist 7.7 pKi 30
pKi 7.7 [30]
chlorpromazine Hs Inverse agonist 7.6 pKi 46
pKi 7.6 [46]
chlorpromazine Rn Inverse agonist 7.6 pKi 48
pKi 7.6 [48]
mesulergine Mm Antagonist 7.6 pKi 45
pKi 7.6 [45]
perphenazine Rn Inverse agonist 7.6 pKi 48
pKi 7.6 [48]
clozapine Hs Inverse agonist 7.2 – 7.8 pKi 31,46,60
pKi 7.2 – 7.8 [31,46,60]
(+)-butaclamol Mm Antagonist 7.5 pKi 45
pKi 7.5 [45]
spiperone Hs Antagonist 7.0 – 8.0 pKi 5,24,31
pKi 7.0 – 8.0 [5,24,31]
metergoline Mm Antagonist 7.5 pKi 45
pKi 7.5 [45]
2-bromo-LSD Hs Antagonist 7.5 pKi 5
pKi 7.5 [5]
fluperlapine Hs Inverse agonist 7.5 pKi 46
pKi 7.5 [46]
SB 258719 Hs Inverse agonist 7.5 pKi 60
pKi 7.5 (Ki 3.16x10-8 M) [60]
methysergide Hs Antagonist 7.1 – 7.8 pKi 5,24,31
pKi 7.1 – 7.8 [5,24,31]
mianserin Hs Antagonist 7.3 – 7.6 pKi 24
pKi 7.3 – 7.6 [24]
clozapine Mm Inverse agonist 7.4 pKi 45
pKi 7.4 [45]
amoxapine Rn Antagonist 7.4 pKi 48
pKi 7.4 [48]
ergotamine Mm Antagonist 7.3 pKi 45
pKi 7.3 [45]
cyproheptadine Rn Antagonist 7.1 – 7.5 pKi 49,51
pKi 7.1 – 7.5 [49,51]
cyamemazine Hs Antagonist 7.2 pKi 18
pKi 7.2 [18]
spiperone Mm Antagonist 7.2 pKi 45
pKi 7.2 [45]
thioridazine Rn Inverse agonist 7.2 pKi 48
pKi 7.2 [48]
mianserin Rn Antagonist 7.0 – 7.4 pKi 49,51
pKi 7.0 – 7.4 [49,51]
perphenazine Hs Inverse agonist 7.2 pKi 46
pKi 7.2 [46]
ritanserin Hs Antagonist 6.8 – 7.4 pKi 5,31
pKi 6.8 – 7.4 [5,31]
loxapine Rn Antagonist 6.8 – 7.4 pKi 48,51
pKi 6.8 – 7.4 [48,51]
thioridazine Hs Inverse agonist 7.1 pKi 46
pKi 7.1 [46]
(+)-butaclamol Rn Antagonist 7.0 pKi 49
pKi 7.0 [49]
iloperidone Hs Antagonist 7.0 pKi 25
pKi 7.0 [25]
mianserin Mm Antagonist 7.0 pKi 45
pKi 7.0 [45]
dihydroergocryptine Mm Antagonist 7.0 pKi 45
pKi 7.0 [45]
amitriptyline Rn Antagonist 6.9 – 7.0 pKi 51
pKi 6.9 – 7.0 [51]
olanzapine Rn Antagonist 6.8 – 7.0 pKi 30,48
pKi 6.8 – 7.0 [30,48]
cyproheptadine Hs Antagonist 6.9 pKi 5
pKi 6.9 [5]
MPDT Hs Antagonist 6.8 pKi 15
pKi 6.8 [15]
dihydroergotamine Rn Antagonist 6.8 pKi 49
pKi 6.8 [49]
ketanserin Rn Antagonist 6.6 – 6.7 pKi 51
pKi 6.6 – 6.7 [51]
olanzapine Hs Antagonist 6.5 pKi 60
pKi 6.5 [60]
dihydroergocryptine Rn Antagonist 6.5 pKi 49
pKi 6.5 [49]
haloperidol Hs Antagonist 6.3 – 6.6 pKi 24
pKi 6.3 – 6.6 [24]
haloperidol Rn Antagonist 6.3 – 6.6 pKi 30,48-49
pKi 6.3 – 6.6 [30,48-49]
buspirone Mm Antagonist 6.4 pKi 45
pKi 6.4 [45]
ketanserin Mm Antagonist 6.4 pKi 45
pKi 6.4 [45]
amitriptyline Mm Antagonist 6.4 pKi 45
pKi 6.4 [45]
sumatriptan Rn Antagonist 6.2 – 6.6 pKi 49,51
pKi 6.2 – 6.6 [49,51]
vortioxetine