5-HT1A receptor

Target id: 1

Nomenclature: 5-HT1A receptor

Family: 5-Hydroxytryptamine receptors

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   GtoImmuPdb view: OFF :     5-HT1A 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 7 422 5q11.2-q13 HTR1A 5-hydroxytryptamine receptor 1A 23,94
Mouse 7 421 13 D2.1 Htr1a 5-hydroxytryptamine (serotonin) receptor 1A 15
Rat 7 422 2q16 Htr1a 5-hydroxytryptamine receptor 1A 3,25
Previous and Unofficial Names
ADRBRL1 | 5-HT1A | ADRB2RL1 | serotonin receptor 1A | Gpcr18 | 5-hydroxytryptamine (serotonin) receptor 1A, G protein-coupled
Database Links
Specialist databases
GPCRDB 5ht1a_human (Hs), 5ht1a_mouse (Mm), 5ht1a_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
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]NLX-112 Hs Full agonist 8.9 pKd 33
pKd 8.9 (Kd 1.4x10-9 M) [33]
[3H]8-OH-DPAT Hs Full agonist 6.0 – 9.4 pKd 9,39,68,71
pKd 6.0 – 9.4 (Kd 1x10-6 – 3.98x10-10 M) [9,39,68,71]
[3H]S-15535 Hs Partial agonist 5.8 – 5.9 pKd 71
pKd 5.8 – 5.9 [71]
S-14671 Hs Full agonist 10.2 – 10.5 pKi 69,71
pKi 10.2 – 10.5 [69,71]
LY293284 Hs Full agonist 10.1 pKi 9
pKi 10.1 [9]
5-CT Hs Full agonist 9.4 – 10.3 pKi 67,69,71-72
pKi 9.4 – 10.3 [67,69,71-72]
lisuride Hs Full agonist 9.7 – 9.8 pKi 59,67,71
pKi 9.7 – 9.8 [59,67,71]
U92016A Hs Full agonist 9.7 pKi 56
pKi 9.7 [56]
vilazodone 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 Hs Full agonist 9.6 – 9.7 pKi 69,71
pKi 9.6 – 9.7 [69,71]
roxindole Hs Partial agonist 9.4 – 9.9 pKi 59,68
pKi 9.4 – 9.9 [59,68]
5-hydroxytryptamine Hs Full agonist 9.1 – 9.7 pKi 39,67-69,71-72
pKi 9.1 – 9.7 [39,67-69,71-72]
flesinoxan Hs Full agonist 9.3 pKi 69
pKi 9.3 [69]
L-694,247 Hs Full agonist 9.3 pKi 67
pKi 9.3 [67]
S-15535 Hs Partial agonist 9.2 pKi 71
pKi 9.2 [71]
Lysergide Hs Full agonist 9.0 pKi 73
pKi 9.0 [73]
RU 24969 Hs Full agonist 9.0 pKi 69
pKi 9.0 [69]
flibanserin Hs Agonist 9.0 pKi 10
pKi 9.0 (Ki 1x10-9 M) [10]
8-OH-DPAT Hs Full agonist 8.4 – 9.4 pKi 20,29,39,48,60,69,71-72
pKi 8.4 – 9.4 (Ki 3.98x10-9 – 3.98x10-10 M) [20,29,39,48,60,69,71-72]
LY 165,163 Hs Full agonist 8.9 pKi 69
pKi 8.9 [69]
spiroxatrine Hs Full agonist 8.8 pKi 69
pKi 8.8 [69]
ipsapirone Hs Partial agonist 8.6 – 8.8 pKi 69,71
pKi 8.6 – 8.8 [69,71]
FG-5893 Hs Full agonist 8.7 pKi 69
pKi 8.7 [69]
pergolide Hs Partial agonist 8.7 pKi 59
pKi 8.7 [59]
7-methoxy-1-naphthylpiperazine Hs Full agonist 8.6 pKi 38
pKi 8.6 [38]
(R)-UH 301 Hs Partial agonist 8.6 pKi 69
pKi 8.6 (Ki 2.74x10-9 M) [69]
NLX-101 Hs Full agonist 8.6 pKi 70
pKi 8.6 [70]
terguride Hs Partial agonist 8.5 pKi 59
pKi 8.5 [59]
ziprasidone Hs Partial agonist 7.9 – 8.9 pKi 69,89
pKi 7.9 – 8.9 [69,89]
S 16924 Hs Partial agonist 8.4 pKi 57
pKi 8.4 [57]
aripiprazole Hs Partial agonist 8.2 pKi 92
pKi 8.2 [92]
tandospirone Hs Full agonist 8.2 pKi 69
pKi 8.2 [69]
lurasidone Rn Partial agonist 8.2 pKi 34
pKi 8.2 (Ki 6.75x10-9 M) [34]
asenapine Hs Full agonist 8.0 – 8.3 pKi 69,89
pKi 8.0 – 8.3 [69,89]
zalospirone Hs Full agonist 8.1 pKi 69
pKi 8.1 [69]
1-naphthylpiperazine Hs Full agonist 8.0 pKi 38
pKi 8.0 [38]
ocaperidone Hs Full agonist 8.0 pKi 26
pKi 8.0 [26]
bromocriptine Hs Partial agonist 7.9 pKi 59
pKi 7.9 [59]
buspirone Hs Partial agonist 7.7 – 8.0 pKi 69,71-72
pKi 7.7 – 8.0 [69,71-72]
vortioxetine Hs Partial agonist 7.8 pKi 7
pKi 7.8 (Ki 1.5x10-8 M) [7]
LY334370 Hs Full agonist 7.8 pKi 96
pKi 7.8 [96]
BRL-15572 Hs Partial agonist 7.7 pKi 83
pKi 7.7 [83]
cabergoline Hs Full agonist 7.7 pKi 59
pKi 7.7 [59]
donitriptan Hs Full agonist 7.6 pKi 37
pKi 7.6 [37]
eletriptan Hs Full agonist 7.4 pKi 66
pKi 7.4 [66]
naratriptan Hs Full agonist 7.1 – 7.6 pKi 66-67
pKi 7.1 – 7.6 [66-67]
nafadotride Hs Full agonist 7.3 pKi 69
pKi 7.3 [69]
LP-44 Hs Agonist 7.3 pKi 50
pKi 7.3 (Ki 5.27x10-8 M) [50]
frovatriptan Hs Agonist 7.2 pKi 100
pKi 7.2 (Ki 6x10-8 M) [100]
LP-12 Hs Agonist 7.2 pKi 50
pKi 7.2 (Ki 6.09x10-8 M) [50]
BMY-14802 Hs Full agonist 7.2 pKi 69
pKi 7.2 [69]
xanomeline Hs Full agonist 7.2 pKi 98
pKi 7.2 [98]
GR 127935 Hs Partial agonist 7.1 – 7.2 pKi 38,83
pKi 7.1 – 7.2 [38,83]
apomorphine Hs Partial agonist 6.9 pKi 59
pKi 6.9 [59]
clozapine Hs Full agonist 6.8 – 6.9 pKi 57,69,89
pKi 6.8 – 6.9 [57,69,89]
EMDT Hs Full agonist 6.8 pKi 28
pKi 6.8 [28]
fluparoxan Hs Partial agonist 6.8 pKi 60
pKi 6.8 [60]
LP-211 Hs Agonist 6.7 pKi 51
pKi 6.7 (Ki 1.88x10-7 M) [51]
zolmitriptan Hs Full agonist 6.6 pKi 66
pKi 6.6 [66]
quetiapine Hs Full agonist 6.5 – 6.6 pKi 69,89
pKi 6.5 – 6.6 [69,89]
piribedil Hs Partial agonist 6.4 pKi 59
pKi 6.4 [59]
rizatriptan Hs Full agonist 6.4 pKi 66
pKi 6.4 [66]
LY344864 Hs Full agonist 6.3 pKi 79
pKi 6.3 [79]
SB 216641 Hs Partial agonist 6.3 pKi 83
pKi 6.3 [83]
CP 93129 Hs Full agonist 6.1 pKi 67
pKi 6.1 [67]
capeserod Hs Partial agonist 6.0 pKi 63
pKi 6.0 [63]
sumatriptan Hs Full agonist 6.0 pKi 66
pKi 6.0 [66]
quinpirole Hs Full agonist 5.8 pKi 68
pKi 5.8 [68]
olanzapine Hs Full agonist 5.6 – 5.8 pKi 69,89
pKi 5.6 – 5.8 [69,89]
vilazodone Hs Partial agonist 9.5 pIC50 31
pIC50 9.5 (IC50 3x10-10 M) [31]
BMY-7378 Hs Partial agonist 6.8 – 8.0 pIC50 42
pIC50 6.8 – 8.0 [42]
L-772,405 Hs Full agonist 7.2 pIC50 87
pIC50 7.2 [87]
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
[3H]robalzotan Hs Antagonist 9.8 pKd 35
pKd 9.8 (Kd 1.58x10-10 M) [35]
[3H]WAY100635 Hs Antagonist 9.5 pKd 42
pKd 9.5 (Kd 3x10-10 M) [42]
[3H]p-MPPF Hs Antagonist 8.4 pKd 39
pKd 8.4 [39]
Rec 15/3079 Hs Antagonist 9.7 pKi 49
pKi 9.7 [49]
NAN 190 Hs Antagonist 9.4 pKi 69
pKi 9.4 [69]
repinotan Hs Antagonist 9.4 pKi 20
pKi 9.4 [20]
robalzotan Hs Antagonist 9.2 pKi 36
pKi 9.2 (Ki 6.31x10-10 M) [36]
SB 649915 Hs Antagonist 8.6 pKi 97
pKi 8.6 [97]
WAY-100635 Hs Antagonist 7.9 – 9.2 pKi 69,71
pKi 7.9 – 9.2 (Ki 1.26x10-8 – 6.31x10-10 M) [69,71]
p-MPPI Hs Antagonist 8.4 pKi 39
pKi 8.4 [39]
tiospirone Hs Antagonist 8.3 pKi 69
pKi 8.3 [69]
(-)-tertatolol Hs Antagonist 8.2 pKi 48,69
pKi 8.2 [48,69]
pindolol Hs Antagonist 8.1 pKi 71
pKi 8.1 [71]
SB 272183 Hs Antagonist 8.0 pKi 99
pKi 8.0 [99]
WAY-100135 Hs Antagonist 8.0 pKi 71
pKi 8.0 [71]
methiothepin Hs Antagonist 7.8 – 8.1 pKi 69,71
pKi 7.8 – 8.1 [69,71]
(S)-UH 301 Hs Antagonist 7.9 pKi 69
pKi 7.9 (Ki 1.35x10-8 M) [69]
spiperone Hs Antagonist 6.7 – 8.8 pKi 69,71-72
pKi 6.7 – 8.8 [69,71-72]
(-)-propranolol Hs Antagonist 7.5 pKi 67
pKi 7.5 [67]
(S)-flurocarazolol Hs Antagonist 7.5 pKi 86
pKi 7.5 [86]
pizotifen Hs Antagonist 7.4 pKi 67
pKi 7.4 [67]
GR 125,743 Hs Antagonist 7.3 pKi 67
pKi 7.3 [67]
yohimbine Hs Antagonist 7.3 pKi 60
pKi 7.3 [60]
fluspirilene Hs Antagonist 7.2 pKi 89
pKi 7.2 [89]
thioridazine Hs Antagonist 7.1 pKi 69
pKi 7.1 [69]
iloperidone Hs Antagonist 7.0 pKi 40
pKi 7.0 [40]
mesoridazine Hs Antagonist 7.0 pKi 17
pKi 7.0 (Ki 1.05x10-7 M) [17]
GR 218,231 Hs Antagonist 6.8 pKi 58
pKi 6.8 [58]
iloperidone Rn Antagonist 6.8 pKi 43
pKi 6.8 [43]
pimozide Hs Antagonist 6.8 pKi 69
pKi 6.8 [69]
(R)-flurocarazolol Hs Antagonist 6.5 pKi 86
pKi 6.5 [86]
SB 714786 Hs Antagonist 6.5 pKi 97
pKi 6.5 [97]
sertindole Hs Antagonist 6.4 – 6.6 pKi 69,89
pKi 6.4 – 6.6 [69,89]
zotepine Hs Antagonist 6.5 pKi 89
pKi 6.5 [89]
risperidone Hs Antagonist 6.4 – 6.5 pKi 69,89
pKi 6.4 – 6.5 [69,89]
(+)-butaclamol Hs Antagonist 6.4 pKi 69
pKi 6.4 [69]
cyamemazine Hs Antagonist 6.3 pKi 29
pKi 6.3 [29]
9-OH-risperidone Hs Antagonist 6.2 pKi 89
pKi 6.2 [89]
chlorpromazine Hs Antagonist 6.2 pKi 69
pKi 6.2 [69]
risperidone Rn Antagonist 6.2 pKi 43
pKi 6.2 [43]
MPDT Hs Antagonist 5.8 pKi 28
pKi 5.8 [28]
haloperidol Hs Antagonist 5.7 – 5.8 pKi 48,57,69,89
pKi 5.7 – 5.8 [48,57,69,89]
pipamperone Hs Antagonist 5.6 pKi 89
pKi 5.6 [89]
raclopride Hs Antagonist 5.2 pKi 69
pKi 5.2 [69]
ketanserin Hs Antagonist 5.0 pKi 72
pKi 5.0 [72]
SDZ-216525 Hs Antagonist 7.8 – 8.2 pIC50 42
pIC50 7.8 – 8.2 [42]
ritanserin Hs Antagonist 5.2 – 5.5 pIC50 42
pIC50 5.2 – 5.5 [42]
p-[18F]MPPF Hs Antagonist - - 18
[18]
[11C]WAY100635 Hs Antagonist - - 95
[95]
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
RS-30199 Hs Positive 7.1 – 7.5 pKi 93
pKi 7.1 – 7.5 [93]
Immunopharmacology Comments
The chemoattractant properties of 5-HT on both human and mouse mast cells are mediated by 5-HT1A receptor [44]. 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 [24] and enhances their phagocytic capacity [24].
Immuno Cell Type Associations
Immuno Cell Type:  T cells
Cell Ontology Term:  
Comment: 
References:  90
Immuno Cell Type:  B cells
Cell Ontology Term:   B cell (CL:0000236)
Comment: 
References:  90
Immuno Cell Type:  Natural killer cells
Cell Ontology Term:  
Comment: 
References:  90
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:  1,90
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
Disease X-refs: 
References:  27
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
Comments:  The 5-HT1A has also been found to stimulate cAMP accumulation via Gi2 and ACII [2].
References:  2,23,53
Secondary Transduction Mechanisms
Transducer Effector/Response
Phospholipase C stimulation
References:  23
Tissue Distribution
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
Poorly expressed in coronary arteries, atrium, ventricle and epicardium.
Species:  Human
Technique:  RT-PCR.
References:  74
Spinal cord: dorsal horn > ventral horn.
Species:  Human
Technique:  Radioligand binding.
References:  47
Benign and malignant prostate tissue.
Species:  Human
Technique:  Western blotting.
References:  22
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:  85
Peritoneal macrophages.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  24
Brain: pyramidal and principal cells and calbindin- and parvalbumin-containing neurons.
Species:  Rat
Technique:  Immunohistochemistry.
References:  5
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:  85
Posterior taste buds.
Species:  Rat
Technique:  RT-PCR.
References:  41
Limbic system: septum, hippocampus, thalamus, amygdala, olfactory bulb, medulla, mesencephalon, hypothalamus.
Species:  Rat
Technique:  Northern blotting.
References:  3
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:  81
Superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique: