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5-HT1A receptor

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Target id: 1

Nomenclature: 5-HT1A receptor

Family: 5-Hydroxytryptamine receptors

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 7 422 5q12.3 HTR1A 5-hydroxytryptamine receptor 1A 24,97
Mouse 7 421 13 56.92 cM Htr1a 5-hydroxytryptamine (serotonin) receptor 1A 15
Rat 7 422 2q13 Htr1a 5-hydroxytryptamine receptor 1A 3,26
Previous and Unofficial Names Click here for help
ADRBRL1 | 5-HT1A | ADRB2RL1 | serotonin receptor 1A | Gpcr18 | 5-hydroxytryptamine (serotonin) receptor 1A, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRdb 5ht1a_human (Hs), 5ht1a_mouse (Mm), 5ht1a_rat (Rn)
Other databases
Alphafold
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Cryo-EM structure of SEP-363856 bound serotonin 1A (5-HT1A) receptor-Gi protein complex
PDB Id:  8W8B
Ligand:  ulotaront
Resolution:  3.0Å
Species:  Human
References:  55
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]NLX-112 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 8.9 pKd 34
pKd 8.9 (Kd 1.4x10-9 M) [34]
[3H]8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 6.0 – 9.4 pKd 9,40,70,73
pKd 6.0 – 9.4 (Kd 1x10-6 – 3.98x10-10 M) [9,40,70,73]
[3H]S-15535 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Partial agonist 5.8 – 5.9 pKd 73
pKd 5.8 – 5.9 [73]
S-14671 Small molecule or natural product Hs Full agonist 10.2 – 10.5 pKi 71,73
pKi 10.2 – 10.5 [71,73]
LY293284 Small molecule or natural product Hs Full agonist 10.1 pKi 9
pKi 10.1 [9]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.4 – 10.3 pKi 69,71,73-74
pKi 9.4 – 10.3 [69,71,73-74]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.7 – 9.8 pKi 61,61,73
pKi 9.7 – 9.8 [61,61,73]
U92016A Small molecule or natural product Hs Full agonist 9.7 pKi 58
pKi 9.7 [58]
vilazodone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 9.7 pKi 19
pKi 9.7 (Ki 2x10-10 M) [19]
Description: Binding of vilazodone to human 5-HT1A receptors against [3H]8-OH-DPAT (DPAT)
S-14506 Small molecule or natural product Hs Full agonist 9.6 – 9.7 pKi 71,73
pKi 9.6 – 9.7 [71,73]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 9.4 – 9.9 pKi 61,70
pKi 9.4 – 9.9 [61,70]
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 9.1 – 9.7 pKi 40,69-71,73-74
pKi 9.1 – 9.7 [40,69-71,73-74]
flesinoxan Small molecule or natural product Hs Full agonist 9.3 pKi 71
pKi 9.3 [71]
L-694,247 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.3 pKi 69
pKi 9.3 [69]
S-15535 Small molecule or natural product Hs Partial agonist 9.2 pKi 73
pKi 9.2 [73]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.0 pKi 75
pKi 9.0 [75]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 71
pKi 9.0 [71]
flibanserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Agonist 9.0 pKi 10
pKi 9.0 (Ki 1x10-9 M) [10]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.4 – 9.4 pKi 20,30,40,49,62,71,73-74
pKi 8.4 – 9.4 (Ki 3.98x10-9 – 3.98x10-10 M) [20,30,40,49,62,71,73-74]
LY 165,163 Small molecule or natural product Hs Full agonist 8.9 pKi 71
pKi 8.9 [71]
spiroxatrine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.8 pKi 71
pKi 8.8 [71]
ipsapirone Small molecule or natural product Hs Partial agonist 8.6 – 8.8 pKi 71,73
pKi 8.6 – 8.8 [71,73]
FG-5893 Small molecule or natural product Hs Full agonist 8.7 pKi 71
pKi 8.7 [71]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.7 pKi 61
pKi 8.7 [61]
7-methoxy-1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.6 pKi 39
pKi 8.6 [39]
(R)-UH 301 Small molecule or natural product Hs Partial agonist 8.6 pKi 71
pKi 8.6 (Ki 2.74x10-9 M) [71]
NLX-101 Small molecule or natural product Hs Full agonist 8.6 pKi 72
pKi 8.6 [72]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.5 pKi 61
pKi 8.5 [61]
ziprasidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 7.9 – 8.9 pKi 71,92
pKi 7.9 – 8.9 [71,92]
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 8.4 pKi 59
pKi 8.4 [59]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.2 pKi 95
pKi 8.2 [95]
tandospirone Small molecule or natural product Hs Full agonist 8.2 pKi 71
pKi 8.2 [71]
lurasidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Partial agonist 8.2 pKi 35
pKi 8.2 (Ki 6.75x10-9 M) [35]
asenapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.0 – 8.3 pKi 71,92
pKi 8.0 – 8.3 [71,92]
zalospirone Small molecule or natural product Hs Full agonist 8.1 pKi 71
pKi 8.1 [71]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 pKi 39
pKi 8.0 [39]
ocaperidone Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 pKi 27
pKi 8.0 [27]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.9 pKi 61
pKi 7.9 [61]
buspirone Small molecule or natural product Approved drug Primary target of this compound Hs Partial agonist 7.7 – 8.0 pKi 71,73-74
pKi 7.7 – 8.0 [71,73-74]
vortioxetine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 7.8 pKi 7
pKi 7.8 (Ki 1.5x10-8 M) [7]
LY334370 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 99
pKi 7.8 [99]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 7.7 pKi 85
pKi 7.7 [85]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.7 pKi 61
pKi 7.7 [61]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.6 pKi 38
pKi 7.6 [38]
eletriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.4 pKi 68
pKi 7.4 [68]
naratriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.1 – 7.6 pKi 68-69
pKi 7.1 – 7.6 [68-69]
nafadotride Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 pKi 71
pKi 7.3 [71]
LP-44 Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.3 pKi 51
pKi 7.3 (Ki 5.27x10-8 M) [51]
frovatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist 7.2 pKi 103
pKi 7.2 (Ki 6x10-8 M) [103]
LP-12 Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.2 pKi 51
pKi 7.2 (Ki 6.09x10-8 M) [51]
BMY-14802 Small molecule or natural product Hs Full agonist 7.2 pKi 71
pKi 7.2 [71]
xanomeline Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.2 pKi 101
pKi 7.2 [101]
avitriptan Small molecule or natural product Click here for species-specific activity table Rn Agonist 7.2 pKi 91
pKi 7.2 (Ki 7.08x10-8 M) [91]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.1 – 7.2 pKi 39,85
pKi 7.1 – 7.2 [39,85]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 6.9 pKi 61
pKi 6.9 [61]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.8 – 6.9 pKi 59,71,92
pKi 6.8 – 6.9 [59,71,92]
EMDT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.8 pKi 29
pKi 6.8 [29]
fluparoxan Small molecule or natural product Hs Partial agonist 6.8 pKi 62
pKi 6.8 [62]
LP-211 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.7 pKi 52
pKi 6.7 (Ki 1.88x10-7 M) [52]
zolmitriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.6 pKi 68
pKi 6.6 [68]
quetiapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.5 – 6.6 pKi 71,92
pKi 6.5 – 6.6 [71,92]
piribedil Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.4 pKi 61
pKi 6.4 [61]
rizatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.4 pKi 68
pKi 6.4 [68]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.3 pKi 81
pKi 6.3 [81]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.3 pKi 85
pKi 6.3 [85]
CP 93129 Small molecule or natural product Hs Full agonist 6.1 pKi 69
pKi 6.1 [69]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.0 pKi 65
pKi 6.0 [65]
sumatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.0 pKi 68
pKi 6.0 [68]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.8 pKi 70
pKi 5.8 [70]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.6 – 5.8 pKi 71,92
pKi 5.6 – 5.8 [71,92]
vilazodone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 9.5 pIC50 32
pIC50 9.5 (IC50 3x10-10 M) [32]
BMY-7378 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 – 8.0 pIC50 43
pIC50 6.8 – 8.0 [43]
L-772,405 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pIC50 89
pIC50 7.2 [89]
ulotaront Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Agonist 5.6 pIC50 21
pIC50 5.6 (IC50 2.3x10-6 M) [21]
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
[3H]robalzotan Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.8 pKd 36
pKd 9.8 (Kd 1.58x10-10 M) [36]
[3H]WAY100635 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.5 pKd 43
pKd 9.5 (Kd 3x10-10 M) [43]
[3H]p-MPPF Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.4 pKd 40
pKd 8.4 [40]
Rec 15/3079 Small molecule or natural product Hs Antagonist 9.7 pKi 50
pKi 9.7 [50]
NAN 190 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.4 pKi 71
pKi 9.4 [71]
repinotan Small molecule or natural product Hs Antagonist 9.4 pKi 20
pKi 9.4 [20]
robalzotan Small molecule or natural product Hs Antagonist 9.2 pKi 37
pKi 9.2 (Ki 6.31x10-10 M) [37]
SB 649915 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 100
pKi 8.6 [100]
WAY-100635 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.9 – 9.2 pKi 71,73
pKi 7.9 – 9.2 (Ki 1.26x10-8 – 6.31x10-10 M) [71,73]
p-MPPI Small molecule or natural product Hs Antagonist 8.4 pKi 40
pKi 8.4 [40]
tiospirone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 71
pKi 8.3 [71]
(-)-tertatolol Small molecule or natural product Hs Antagonist 8.2 pKi 49,71
pKi 8.2 [49,71]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.1 pKi 73
pKi 8.1 [73]
SB 272183 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 pKi 102
pKi 8.0 [102]
WAY-100135 Small molecule or natural product Hs Antagonist 8.0 pKi 73
pKi 8.0 [73]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 – 8.1 pKi 71,73
pKi 7.8 – 8.1 [71,73]
(S)-UH 301 Small molecule or natural product Hs Antagonist 7.9 pKi 71
pKi 7.9 (Ki 1.35x10-8 M) [71]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.7 – 8.8 pKi 71,73-74
pKi 6.7 – 8.8 [71,73-74]
(-)-propranolol Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.5 pKi 69
pKi 7.5 [69]
(S)-flurocarazolol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 88
pKi 7.5 [88]
pizotifen Small molecule or natural product Approved drug Hs Antagonist 7.4 pKi 69
pKi 7.4 [69]
GR 125,743 Small molecule or natural product Hs Antagonist 7.3 pKi 69
pKi 7.3 [69]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 pKi 62
pKi 7.3 [62]
fluspirilene Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.2 pKi 92
pKi 7.2 [92]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.1 pKi 71
pKi 7.1 [71]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 pKi 41
pKi 7.0 [41]
mesoridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 pKi 17
pKi 7.0 (Ki 1.05x10-7 M) [17]
GR 218,231 Small molecule or natural product Hs Antagonist 6.8 pKi 60
pKi 6.8 [60]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.8 pKi 44
pKi 6.8 [44]
pimozide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.8 pKi 71
pKi 6.8 [71]
(R)-flurocarazolol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 88
pKi 6.5 [88]
SB 714786 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 100
pKi 6.5 [100]
sertindole Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.4 – 6.6 pKi 71,92
pKi 6.4 – 6.6 [71,92]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.5 pKi 92
pKi 6.5 [92]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.4 – 6.5 pKi 71,92
pKi 6.4 – 6.5 [71,92]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 pKi 71
pKi 6.4 [71]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 30
pKi 6.3 [30]
9-OH-risperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 92
pKi 6.2 [92]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.2 pKi 71
pKi 6.2 [71]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.2 pKi 44
pKi 6.2 [44]
MPDT Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.8 pKi 29
pKi 5.8 [29]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.7 – 5.8 pKi