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5-HT1A receptor

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Target id: 1

Nomenclature: 5-HT1A 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 7 422 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 P08908 (Hs), Q64264 (Mm), P19327 (Rn)
ChEMBL Target CHEMBL214 (Hs), CHEMBL3737 (Mm), CHEMBL273 (Rn)
DrugBank Target P08908 (Hs)
Ensembl Gene ENSG00000178394 (Hs), ENSMUSG00000021721 (Mm), ENSRNOG00000010254 (Rn)
Entrez Gene 3350 (Hs), 15550 (Mm), 24473 (Rn)
Human Protein Atlas ENSG00000178394 (Hs)
KEGG Gene hsa:3350 (Hs), mmu:15550 (Mm), rno:24473 (Rn)
OMIM 109760 (Hs)
Pharos P08908 (Hs)
RefSeq Nucleotide NM_000524 (Hs), NM_008308 (Mm), NM_012585 (Rn)
RefSeq Protein NP_000515 (Hs), NP_032334 (Mm), NP_036717 (Rn)
UniProtKB P08908 (Hs), Q64264 (Mm), P19327 (Rn)
Wikipedia HTR1A (Hs)
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:  56
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 Ligand has a PDB structure 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 20,30,40,62,71,73,73-74
⤷ pKi 8.4 – 9.4 (Ki 3.98x10-9 – 3.98x10-10 M) [20,30,40,62,71,73,73-74]
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 Ligand has a PDB structure 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 Ligand has a PDB structure 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 Ligand has a PDB structure 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 52
⤷ pKi 7.3 (Ki 5.27x10-8 M) [52]
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 52
⤷ pKi 7.2 (Ki 6.09x10-8 M) [52]
BMY-14802 Small molecule or natural product Hs Full agonist 7.2 pKi 71
⤷ pKi 7.2 [71]
xanomeline Small molecule or natural product Approved drug 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 Ligand has a PDB structure 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 53
⤷ pKi 6.7 (Ki 1.88x10-7 M) [53]
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 51
⤷ pKi 9.7 [51]
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 50,71
⤷ pKi 8.2 [50,71]
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 50,59,71,92
⤷ pKi 5.7 – 5.8 [50,59,71,92]
pipamperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 pKi 92
⤷ pKi 5.6 [92]
raclopride Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.2 pKi 71
⤷ pKi 5.2 [71]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.0 pKi 74
⤷ pKi 5.0 [74]
SDZ-216525 Small molecule or natural product Hs Antagonist 7.8 – 8.2 pIC50 43
⤷ pIC50 7.8 – 8.2 [43]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.2 – 5.5 pIC50 43
⤷ pIC50 5.2 – 5.5 [43]
p-[18F]MPPF Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist - - 18
⤷ [18]
[11C]WAY100635 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist - - 98
⤷ [98]
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
RS-30199 Small molecule or natural product Hs Positive 7.1 – 7.5 pKi 96
⤷ pKi 7.1 – 7.5 [96]
Immunopharmacology Comments
The chemoattractant properties of 5-HT on both human and mouse mast cells are mediated by 5-HT1A receptor [45]. Mouse 5-HT1A receptor activation stimulates production of pro-inflammatory cytokines (e.g. IL-1 and IL-6) from peritoneal macrophages in a NF-κB-dependent manner [28] and enhances their phagocytic capacity [25].
Cell Type Associations
Immuno Cell Type:  T cells
References:  93
Immuno Cell Type:  B cells
Cell Ontology Term:   B cell (CL:0000236)
References:  93
Immuno Cell Type:  Natural killer cells
References:  93
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  Involved in mast cell chemotaxix.
References:  1
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   macrophage (CL:0000235)
monocyte (CL:0000576)
Comment:  Involved in phagocytosis.
References:  1,93
Immuno Disease Associations
Disease Name:  Colitis
Disease Synonyms:  no synonynms
Comment:  Serotonin acting via 5-HT1A receptors plays a key role in the pathogenesis of experimental colitis
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
Comments:  The 5-HT1A has also been found to stimulate cAMP accumulation via Gi2 and ACII [2].
References:  2,24,55
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Phospholipase C stimulation
References:  24
Tissue Distribution Click here for help
Kidney: medullary and cortical thick ascending limbs (TAL), distal convoluted tubules (DCT), connecting tubule cells, principal cells of the initial collecting tubule.
Species:  Human
Technique:  Immunohistochemistry.
References:  87
Benign and malignant prostate tissue.
Species:  Human
Technique:  Western blotting.
References:  23
Poorly expressed in coronary arteries, atrium, ventricle and epicardium.
Species:  Human
Technique:  RT-PCR.
References:  76
Spinal cord: dorsal horn > ventral horn.
Species:  Human
Technique:  Radioligand binding.
References:  49
CNS: dentate gyrus, hippocampus (all fields especially CA1), subiculum, parahippocampal gyrus and neocortical regions (superficial and middle laminae), raphe of the brainstem.
Species:  Human
Technique:  in situ hybridisation.
References:  14
Peritoneal macrophages.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  25
CNS: Dorsal raphe nucleus, septum, hippocampus, entorhinal cortex, interpeduncular nucleus > olfactory bulb, cerebral cortex, thalamic and hypothalamic nuclei, nuclei of the brainstem, dorsal horn of the spinal cord.
Species:  Rat
Technique:  in situ hybridisation.
References:  83
Superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  82
Brain: pyramidal and principal cells and calbindin- and parvalbumin-containing neurons.
Species:  Rat
Technique:  Immunohistochemistry.
References:  5
Limbic system: septum, hippocampus, thalamus, amygdala, olfactory bulb, medulla, mesencephalon, hypothalamus.
Species:  Rat
Technique:  Northern blotting.
References:  3
Posterior taste buds.
Species:  Rat
Technique:  RT-PCR.
References:  42
Kidney: medullary and cortical thick ascending limbs (TAL), distal convoluted tubules (DCT), connecting tubule cells, principal cells of the initial collecting tubule.
Species:  Rat
Technique:  Immunohistochemistry.
References:  87
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 IP3 levels in HeLa cells transfected with the 5-HT1A receptor.
Species:  Human
Tissue:  HeLa cells.
Response measured:  PLC mediated IP3 accumulation.
References:  24
Measurement of cAMP levels in rat CH4ZD10 cells endogenously expressing the 5-HT1A receptor.
Species:  Rat
Tissue:  CH4ZD10 cells.
Response measured:  PTX-sensitive inhibition of cAMP accumulation.
References:  3
Measurement of cAMP levels in SN-48 cells endogenously expressing the 5-HT1A receptor.
Species:  Mouse
Tissue:  Differentiated SN-48 cell line.
Response measured:  Inhibition of cAMP accumulation.
References:  15
Measurement of cAMP levels in HEK 293 cells transfected with the rat 5-HT1A receptor alone/with adenylyl cyclase II (ACII).
Species:  Rat
Tissue:  HEK 293 cells.
Response measured:  Inhibition of cAMP accumulation in the absence of ACII.
Increase in cAMP accumulation in the presence of ACII.
References:  2
Measurement of extracellular acidification rate (ECAR) in CHO-K1 cells transfected with the 5-HT1A receptor.
Species:  Human
Tissue:  CHO-K1 cells.
Response measured:  Activation of the Na+/H+ exchanger.
References:  27
Measurement of phosphorylated ERK1/2 levels in the rat hippocampus.
Species:  Rat
Tissue:  Hippocampus.
Response measured:  Inhibition of the Erk1/2 MAPK pathway.
References:  16
Measurement of cAMP levels in COS-7 cells transfected with the 5-HT1A receptor.
Species:  Human
Tissue:  COS-7
Response measured:  Inhibition of cAMP accumulation.
References:  24,74
Physiological Functions Click here for help
Stimulation of cell proliferation.
Species:  Human
Tissue:  DU145, PC-3, LNCaP and hPCP prostatic cell lines.
References:  23
Increase in phagocytic activity.
Species:  Mouse
Tissue:  Peritoneal macrophages.
References:  25
Hyperpolarisation of orexin neurons.
Species:  Mouse
Tissue:  Hypothalamus.
References:  66
Regulation of sleep-wakefulness cycles.
Species:  Rat
Tissue:  In vivo.
References:  63-64
Regulation of sleep-wakefulness cycles.
Species:  Mouse
Tissue:  In vivo.
References:  12
Regulation of epileptic activity.
Species:  Rat
Tissue:  In vivo.
References:  47
Regulation of oxytocin and adrenocorticotropin hormone release.
Species:  Rat
Tissue:  In vivo (paraventricular nucleus).
References:  77
Adult brain cell proliferation.
Species:  Rat
Tissue:  Subgranular layer (SGL) of the dentate gyrus (DG) and the subventricular zone (SVZ).
References:  6
Autoreceptor: autoinhibitory control.
Species:  Mouse
Tissue:  In vivo (dorsal raphe nucleus).
References:  11
Regulation of cholinergic, GABAergic and glutamatergic transmission and hence cognitive performance.
Species:  Mouse
Tissue:  In vivo.
References:  57
Regulation of anxiety-like behaviour.
Species:  Mouse
Tissue:  In vivo.
References:  46
Regulation of stress responses and locomotor activity.
Species:  Mouse
Tissue:  In vivo (hypothalamus).
References:  54
Regulation of aggressive bahaviour.
Species:  Rat
Tissue:  In vivo.
References:  84
Regulation of feeding behaviour by inducing preproNPY mRNA expression.
Species:  Rat
Tissue:  In vivo (arcuate nucleus).
References:  80
Facilitation of autoshaped learning.
Species:  Mouse
Tissue:  In vivo.
References:  79
Regulation of hippocampal functions.
Species:  Rat
Tissue:  In vivo.
References:  13
Antinociception.
Species:  Rat
Tissue:  In vivo.
References:  31,94
Physiological Consequences of Altering Gene Expression Click here for help
5-HT1A receptor knockout mice exhibit higher amounts of paradoxical sleep than wild-type mice during both the light and the dark phases.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  12
5-HT1A receptor knockout mice have an increased responsiveness to 5-HT in the dorsal raphe nucleus due to lack of autoinhibitory control by 5-HT1A autoreceptors.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  11
Increased 5-HT1A receptor expression during postnatal development caused elevated 5-HT levels in the hippocampus and striatum, decreased anxiety-like behaviour (in male and female) and decreased body temperature (male only).
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  46
5-HT1A receptor knockout mice exhibit a deficit in hippocampal-dependent learning and memory as well as higher limbic excitability.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  90
5-HT1A receptor knockout mice exhibit altered decision making abilities and response inhibition.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  79
Temporary 5-HT1A receptor overexpression during embryonic and perinatal development causes long-term memory impairment.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  8
5-HT1A receptor knockout mice show increases in typical anxiety and stress responses.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  33,78,86
5-HT1A receptor knockout mice exhibit down-regulation of the 5-HT transporter.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  4
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
Htr1atm2Rhn|Slc6a4+|Slc6a4tm1(tTA)Cogr Htr1atm2Rhn/Htr1atm2Rhn,Slc6a4tm1(tTA)Cogr/Slc6a4+
involves: 129S1/Sv * BALB/cJ * C57BL/6 * CBA		 MGI:96273  MGI:96285  MP:0006276 abnormal autonomic nervous system physiology PMID: 18599790 
Htr1atm1Rhn Htr1atm1Rhn/Htr1atm1Rhn
129S6/SvEvTac-Htr1a		 MGI:96273  MP:0005663 abnormal circulating noradrenaline level PMID: 11080193 
Htr1atm2Rhn|Slc6a4+|Slc6a4tm1(tTA)Cogr Htr1atm2Rhn/Htr1atm2Rhn,Slc6a4tm1(tTA)Cogr/Slc6a4+
involves: 129S1/Sv * BALB/cJ * C57BL/6 * CBA		 MGI:96273  MGI:96285  MP:0004811 abnormal neuron physiology PMID: 18599790 
Htr1atm1Rhn Htr1atm1Rhn/Htr1atm1Rhn
129S6/SvEvTac-Htr1a		 MGI:96273  MP:0005322 abnormal serotonin concentration PMID: 11080193  11483665 
Htr1atm1Toth Htr1atm1Toth/Htr1atm1Toth
involves: 129P2/OlaHsd * Black Swiss		 MGI:96273  MP:0001463 abnormal spatial learning PMID: 11121072 
Htr1atm1Tct Htr1atm1Tct/Htr1atm1Tct
involves: 129X1/SvJ * C57BL/6J		 MGI:96273  MP:0002573 behavioral despair PMID: 9844013 
Htr1a+|Htr1atm1Tct Htr1atm1Tct/Htr1a+
involves: 129X1/SvJ * C57BL/6J		 MGI:96273  MP:0002573 behavioral despair PMID: 9844013 
Htr1atm1Rhn Htr1atm1Rhn/Htr1atm1Rhn
involves: 129S1/Sv		 MGI:96273  MP:0002573 behavioral despair PMID: 9826725 
Htr1atm2Rhn|Slc6a4+|Slc6a4tm1(tTA)Cogr Htr1atm2Rhn/Htr1atm2Rhn,Slc6a4tm1(tTA)Cogr/Slc6a4+
involves: 129S1/Sv * BALB/cJ * C57BL/6 * CBA		 MGI:96273  MGI:96285  MP:0005534 decreased body temperature PMID: 18599790 
Htr1atm2Rhn|Slc6a4+|Slc6a4tm1(tTA)Cogr Htr1atm2Rhn/Htr1atm2Rhn,Slc6a4tm1(tTA)Cogr/Slc6a4+
involves: 129S1/Sv * BALB/cJ * C57BL/6 * CBA		 MGI:96273  MGI:96285  MP:0005333 decreased heart rate PMID: 18599790 
Htr1atm1Toth Htr1atm1Toth/Htr1atm1Toth
involves: 129P2/OlaHsd * Black Swiss		 MGI:96273  MP:0002920 decreased paired-pulse facilitation PMID: 10751426  11121072 
Htr1atm2Rhn|Slc6a4+|Slc6a4tm1(tTA)Cogr Htr1atm2Rhn/Htr1atm2Rhn,Slc6a4tm1(tTA)Cogr/Slc6a4+
involves: 129S1/Sv * BALB/cJ * C57BL/6 * CBA		 MGI:96273  MGI:96285  MP:0008770 decreased survivor rate PMID: 18599790 
Htr1a+|Htr1atm2Rhn Htr1atm2Rhn/Htr1a+
involves: BALB/c * C57BL/6		 MGI:96273  MP:0002757 decreased vertical activity PMID: 16507009 
Htr1atm1Toth Htr1atm1Toth/Htr1atm1Toth
involves: 129P2/OlaHsd * Black Swiss		 MGI:96273  MP:0001399 hyperactivity PMID: 9724773 
Htr1atm1Tct Htr1atm1Tct/Htr1atm1Tct
involves: 129X1/SvJ * C57BL/6J		 MGI:96273  MP:0001363 increased anxiety-related response PMID: 9844013 
Htr1a+|Htr1atm1Tct Htr1atm1Tct/Htr1a+
involves: 129X1/SvJ * C57BL/6J		 MGI:96273  MP:0001363 increased anxiety-related response PMID: 9844013 
Htr1atm1Toth Htr1atm1Toth/Htr1atm1Toth
involves: 129P2/OlaHsd * Black Swiss		 MGI:96273  MP:0001363 increased anxiety-related response PMID: 10751426  9724773 
Htr1atm1Rhn Htr1atm1Rhn/Htr1atm1Rhn
involves: 129S1/Sv		 MGI:96273  MP:0001363 increased anxiety-related response PMID: 9826725 
Htr1a+|Htr1atm1Rhn Htr1atm1Rhn/Htr1a+
involves: 129S1/Sv		 MGI:96273  MP:0001363 increased anxiety-related response PMID: 9826725 
Htr1a+|Htr1atm1Toth Htr1atm1Toth/Htr1a+
involves: 129P2/OlaHsd * Black Swiss		 MGI:96273  MP:0001363 increased anxiety-related response PMID: 9724773 
Htr1atm1Rhn Htr1atm1Rhn/Htr1atm1Rhn
129S6/SvEvTac-Htr1a		 MGI:96273  MP:0001906 increased dopamine level PMID: 11080193 
Htr1atm1Toth Htr1atm1Toth/Htr1atm1Toth
involves: 129P2/OlaHsd * Black Swiss		 MGI:96273  MP:0002906 increased susceptibility to pharmacologically induced seizures PMID: 11121072 
Htr1atm1Tct Htr1atm1Tct/Htr1atm1Tct
involves: 129X1/SvJ * C57BL/6J		 MGI:96273  MP:0002797 increased thigmotaxis PMID: 9844013 
Htr1atm2Rhn|Slc6a4+|Slc6a4tm1(tTA)Cogr Htr1atm2Rhn/Htr1atm2Rhn,Slc6a4tm1(tTA)Cogr/Slc6a4+
involves: 129S1/Sv * BALB/cJ * C57BL/6 * CBA		 MGI:96273  MGI:96285  MP:0002083 premature death PMID: 18599790 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Periodic fever, menstrual cycle dependent
OMIM: 614674
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphisms
Species:  Human
Description:  Two polymorphisms, Gly22 -> Ser and Ile28 -> Val, have been found to alter the extracellular amino terminal region of the receptor.
References:  67
Type:  Single nucleotide polymorphism
Species:  Human
Description:  The polymorphism Arg219 -> Leu has been associated with Tourette's syndrome.
References:  48
Type:  Single nucleotide polymorphism
Species:  Human
Description:  The polymorphism Ala50 -> Val, occurring in transmembrane 1, results in a loss of response to 5-HT.
References:  22

References

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