Nomenclature: 5-HT1A 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. 

Contents

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 (serotonin) receptor 1A, G protein-coupled 19,85
Mouse 7 421 13 D2.1 Htr1a 5-hydroxytryptamine (serotonin) receptor 1A 13
Rat 7 422 2q16 Htr1a 5-hydroxytryptamine (serotonin) receptor 1A, G protein-coupled 2,21
Previous and Unofficial Names
ADRB2RL1
ADRBRL1
5-HT1A
5-hydroxytryptamine (serotonin) receptor 1A
5HT1A
RAT5HT1A
5-HT-1A
5-hydroxytryptamine receptor 1A
serotonin receptor 1A
5-HT1A receptor
Gpcr18
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
5-HT
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]F13640 Hs Full agonist 8.9 pKd 28
pKd 8.9 (Kd 1.4x10-9 M) [28]
[3H]8-OH-DPAT Hs Full agonist 6.0 – 9.4 pKd 8,34,60,63
pKd 6.0 – 9.4 (Kd 3.98x10-10 – 1x10-6 M) [8,34,60,63]
[3H]S-15535 Hs Partial agonist 5.8 – 5.9 pKd 63
pKd 5.8 – 5.9 [63]
S-14671 Hs Full agonist 10.2 – 10.5 pKi 61,63
pKi 10.2 – 10.5 [61,63]
LY293284 Hs Full agonist 10.1 pKi 8
pKi 10.1 [8]
5-CT Hs Full agonist 9.4 – 10.3 pKi 59,61,63-64
pKi 9.4 – 10.3 [59,61,63-64]
lisuride Hs Full agonist 9.7 – 9.8 pKi 51,59,63
pKi 9.7 – 9.8 [51,59,63]
U92016A Hs Full agonist 9.7 pKi 48
pKi 9.7 [48]
vilazodone Hs Partial agonist 9.7 pKi 15
pKi 9.7 (Ki 2x10-10 M) [15]
Description: Binding of vilazodone to human 5-HT1A receptors against [3H]8-OH-DPAT (DPAT)
roxindole Hs Partial agonist 9.4 – 9.9 pKi 51,60
pKi 9.4 – 9.9 [51,60]
S-14506 Hs Full agonist 9.6 – 9.7 pKi 61,63
pKi 9.6 – 9.7 [61,63]
5-HT Hs Full agonist 9.1 – 9.7 pKi 34,59-61,63-64
pKi 9.1 – 9.7 [34,59-61,63-64]
L-694,247 Hs Full agonist 9.3 pKi 59
pKi 9.3 [59]
flesinoxan Hs Full agonist 9.3 pKi 61
pKi 9.3 [61]
S-15535 Hs Partial agonist 9.2 pKi 63
pKi 9.2 [63]
LSD Hs Full agonist 9.0 pKi 65
pKi 9.0 [65]
RU 24969 Hs Full agonist 9.0 pKi 61
pKi 9.0 [61]
8-OH-DPAT Hs Full agonist 8.4 – 9.4 pKi 16,24,34,42,52,61,63-64
pKi 8.4 – 9.4 [16,24,34,42,52,61,63-64]
LY 165,163 Hs Full agonist 8.9 pKi 61
pKi 8.9 [61]
spiroxatrine Hs Full agonist 8.8 pKi 61
pKi 8.8 [61]
ipsapirone Hs Partial agonist 8.6 – 8.8 pKi 61,63
pKi 8.6 – 8.8 [61,63]
pergolide Hs Partial agonist 8.7 pKi 51
pKi 8.7 [51]
FG-5893 Hs Full agonist 8.7 pKi 61
pKi 8.7 [61]
7-methoxy-1-naphthylpiperazine Hs Full agonist 8.6 pKi 33
pKi 8.6 [33]
F15599 Hs Full agonist 8.6 pKi 62
pKi 8.6 [62]
(R)-UH 301 Hs Partial agonist 8.6 pKi 61
pKi 8.6 (Ki 2.74x10-9 M) [61]
terguride Hs Partial agonist 8.5 pKi 51
pKi 8.5 [51]
ziprasidone Hs Partial agonist 7.9 – 8.9 pKi 61,81
pKi 7.9 – 8.9 [61,81]
S 16924 Hs Partial agonist 8.4 pKi 49
pKi 8.4 [49]
aripiprazole Hs Full agonist 8.2 pKi 83
pKi 8.2 [83]
tandospirone Hs Full agonist 8.2 pKi 61
pKi 8.2 [61]
lurasidone Rn Partial agonist 8.17 pKi 29
pKi 8.17 (Ki 6.75x10-9 M) [29]
asenapine Hs Full agonist 8.0 – 8.3 pKi 61,81
pKi 8.0 – 8.3 [61,81]
zalospirone Hs Full agonist 8.1 pKi 61
pKi 8.1 [61]
1-naphthylpiperazine Hs Full agonist 8.0 pKi 33
pKi 8.0 [33]
ocaperidone Hs Full agonist 8.0 pKi 22
pKi 8.0 [22]
bromocriptine Hs Partial agonist 7.9 pKi 51
pKi 7.9 [51]
buspirone Hs Partial agonist 7.7 – 8.0 pKi 61,63-64
pKi 7.7 – 8.0 [61,63-64]
LY334370 Hs Full agonist 7.8 pKi 86
pKi 7.8 [86]
cabergoline Hs Full agonist 7.7 pKi 51
pKi 7.7 [51]
BRL-15572 Hs Partial agonist 7.7 pKi 75
pKi 7.7 [75]
donitriptan Hs Full agonist 7.6 pKi 32
pKi 7.6 [32]
eletriptan Hs Full agonist 7.4 pKi 58
pKi 7.4 [58]
naratriptan Hs Full agonist 7.1 – 7.6 pKi 58-59
pKi 7.1 – 7.6 [58-59]
nafadotride Hs Full agonist 7.3 pKi 61
pKi 7.3 [61]
frovatriptan Hs Agonist 7.22 pKi 90
pKi 7.22 (Ki 6x10-8 M) [90]
BMY-14802 Hs Full agonist 7.2 pKi 61
pKi 7.2 [61]
xanomeline Hs Full agonist 7.2 pKi 88
pKi 7.2 [88]
GR-127935 Hs Partial agonist 7.1 – 7.2 pKi 33,75
pKi 7.1 – 7.2 [33,75]
apomorphine Hs Partial agonist 6.9 pKi 51
pKi 6.9 [51]
clozapine Hs Full agonist 6.8 – 6.9 pKi 49,61,81
pKi 6.8 – 6.9 [49,61,81]
fluparoxan Hs Partial agonist 6.8 pKi 52
pKi 6.8 [52]
EMDT Hs Full agonist 6.8 pKi 23
pKi 6.8 [23]
zolmitriptan Hs Full agonist 6.6 pKi 58
pKi 6.6 [58]
quetiapine Hs Full agonist 6.5 – 6.6 pKi 61,81
pKi 6.5 – 6.6 [61,81]
rizatriptan Hs Full agonist 6.4 pKi 58
pKi 6.4 [58]
piribedil Hs Partial agonist 6.4 pKi 51
pKi 6.4 [51]
SB 216641 Hs Partial agonist 6.3 pKi 75
pKi 6.3 [75]
LY344864 Hs Full agonist 6.3 pKi 71
pKi 6.3 [71]
CP 93129 Hs Full agonist 6.1 pKi 59
pKi 6.1 [59]
sumatriptan Hs Full agonist 6.0 pKi 58
pKi 6.0 [58]
SL65.0155 Hs Partial agonist 6.0 pKi 55
pKi 6.0 [55]
quinpirole Hs Full agonist 5.8 pKi 60
pKi 5.8 [60]
olanzapine Hs Full agonist 5.6 – 5.8 pKi 61,81
pKi 5.6 – 5.8 [61,81]
vilazodone Hs Partial agonist 9.52 pIC50 26
pIC50 9.52 (IC50 3x10-10 M) [26]
BMY-7378 Hs Partial agonist 6.8 – 8.0 pIC50 37
pIC50 6.8 – 8.0 [37]
L-772,405 Hs Full agonist 7.2 pIC50 79
pIC50 7.2 [79]
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]NAD 299 Hs Antagonist 9.8 pKd 30
pKd 9.8 (Kd 1.58x10-10 M) [30]
[3H]WAY100635 Hs Antagonist 9.5 pKd 37
pKd 9.5 (Kd 3x10-10 M) [37]
[3H]p-MPPF Hs Antagonist 8.4 pKd 34
pKd 8.4 [34]
Rec 15/3079 Hs Antagonist 9.7 pKi 43
pKi 9.7 [43]
NAN 190 Hs Antagonist 9.4 pKi 61
pKi 9.4 [61]
repinotan Hs Antagonist 9.4 pKi 16
pKi 9.4 [16]
robalzotan Hs Antagonist 9.2 pKi 31
pKi 9.2 [31]
SB 649915 Hs Antagonist 8.6 pKi 87
pKi 8.6 [87]
WAY-100635 Hs Antagonist 7.9 – 9.2 pKi 61,63
pKi 7.9 – 9.2 [61,63]
p-MPPI Hs Antagonist 8.4 pKi 34
pKi 8.4 [34]
tiospirone Hs Antagonist 8.3 pKi 61
pKi 8.3 [61]
(-)-tertatolol Hs Antagonist 8.2 pKi 42,61
pKi 8.2 [42,61]
pindolol Hs Antagonist 8.1 pKi 63
pKi 8.1 [63]
SB 272183 Hs Antagonist 8.0 pKi 89
pKi 8.0 [89]
WAY-100135 Hs Antagonist 8.0 pKi 63
pKi 8.0 [63]
methiothepin Hs Antagonist 7.8 – 8.1 pKi 61,63
pKi 7.8 – 8.1 [61,63]
(S)-UH 301 Hs Antagonist 7.9 pKi 61
pKi 7.9 (Ki 1.35x10-8 M) [61]
vortioxetine Hs Antagonist 7.82 pKi 6
pKi 7.82 (Ki 1.5x10-8 M) [6]
spiperone Hs Antagonist 6.7 – 8.8 pKi 61,63-64
pKi 6.7 – 8.8 [61,63-64]
(S)-flurocarazolol Hs Antagonist 7.5 pKi 78
pKi 7.5 [78]
(-)-propranolol Hs Antagonist 7.5 pKi 59
pKi 7.5 [59]
pizotifen Hs Antagonist 7.4 pKi 59
pKi 7.4 [59]
yohimbine Hs Antagonist 7.3 pKi 52
pKi 7.3 [52]
GR 125,743 Hs Antagonist 7.3 pKi 59
pKi 7.3 [59]
fluspirilene Hs Antagonist 7.2 pKi 81
pKi 7.2 [81]
thioridazine Hs Antagonist 7.1 pKi 61
pKi 7.1 [61]
iloperidone Hs Antagonist 7.0 pKi 35
pKi 7.0 [35]
iloperidone Rn Antagonist 6.8 pKi 38
pKi 6.8 [38]
pimozide Hs Antagonist 6.8 pKi 61
pKi 6.8 [61]
GR 218,231 Hs Antagonist 6.8 pKi 50
pKi 6.8 [50]
zotepine Hs Antagonist 6.5 pKi 81
pKi 6.5 [81]
SB 714786 Hs Antagonist 6.5 pKi 87
pKi 6.5 [87]
(R)-flurocarazolol Hs Antagonist 6.5 pKi 78
pKi 6.5 [78]
sertindole Hs Antagonist 6.4 – 6.6 pKi 61,81
pKi 6.4 – 6.6 [61,81]
risperidone Hs Antagonist 6.4 – 6.5 pKi 61,81
pKi 6.4 – 6.5 [61,81]
(+)-butaclamol Hs Antagonist 6.4 pKi 61
pKi 6.4 [61]
cyamemazine Hs Antagonist 6.3 pKi 24
pKi 6.3 [24]
risperidone Rn Antagonist 6.2 pKi 38
pKi 6.2 [38]
9-OH-risperidone Hs Antagonist 6.2 pKi 81
pKi 6.2 [81]
chlorpromazine Hs Antagonist 6.2 pKi 61
pKi 6.2 [61]
MPDT Hs Antagonist 5.8 pKi 23
pKi 5.8 [23]
haloperidol Hs Antagonist 5.7 – 5.8 pKi 42,49,61,81
pKi 5.7 – 5.8 [42,49,61,81]
pipamperone Hs Antagonist 5.6 pKi 81
pKi 5.6 [81]
raclopride Hs Antagonist 5.2 pKi 61
pKi 5.2 [61]
ketanserin Hs Antagonist 5.0 pKi 64
pKi 5.0 [64]
SDZ-216525 Hs Antagonist 7.8 – 8.2 pIC50 37
pIC50 7.8 – 8.2 [37]
ritanserin Hs Antagonist 5.2 – 5.5 pIC50 37
pIC50 5.2 – 5.5 [37]
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 84
pKi 7.1 – 7.5 [84]
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 [1].
References:  1,19,45
Secondary Transduction Mechanisms
Transducer Effector/Response
Phospholipase C stimulation
References:  19
Tissue Distribution
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:  77
Benign and malignant prostate tissue.
Species:  Human
Technique:  Western blotting.
References:  18
Poorly expressed in coronary arteries, atrium, ventricle and epicardium.
Species:  Human
Technique:  RT-PCR.
References:  66
Spinal cord: dorsal horn > ventral horn.
Species:  Human
Technique:  Radioligand binding.
References:  41
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:  12
Peritoneal macrophages.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  20
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:  73
Superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  72
Brain: pyramidal and principal cells and calbindin- and parvalbumin-containing neurons.
Species:  Rat
Technique:  Immunohistochemistry.
References:  4
Limbic system: septum, hippocampus, thalamus, amygdala, olfactory bulb, medulla, mesencephalon, hypothalamus.
Species:  Rat
Technique:  Northern blotting.
References:  2
Posterior taste buds.
Species:  Rat
Technique:  RT-PCR.
References:  36
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:  77
Expression Datasets

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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
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:  19
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:  2
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:  13
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:  22
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:  1
Measurement of phosphorylated ERK1/2 levels in the rat hippocampus.
Species:  Rat
Tissue:  Hippocampus.
Response measured:  Inhibition of the Erk1/2 MAPK pathway.
References:  14
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:  19,64
Physiological Functions
Stimulation of cell proliferation.
Species:  Human
Tissue:  DU145, PC-3, LNCaP and hPCP prostatic cell lines.
References:  18
Increase in phagocytic activity.
Species:  Mouse
Tissue:  Peritoneal macrophages.
References:  20
Hyperpolarisation of orexin neurons.
Species:  Mouse
Tissue:  Hypothalamus.
References:  56
Regulation of sleep-wakefulness cycles.
Species:  Rat
Tissue:  In vivo.
References:  53-54
Regulation of sleep-wakefulness cycles.
Species:  Mouse
Tissue:  In vivo.
References:  10
Regulation of epileptic activity.
Species:  Rat
Tissue:  In vivo.
References:  46
Regulation of oxytocin and adrenocorticotropin hormone release.
Species:  Rat
Tissue:  In vivo (paraventricular nucleus).
References:  67
Adult brain cell proliferation.
Species:  Rat
Tissue:  Subgranular layer (SGL) of the dentate gyrus (DG) and the subventricular zone (SVZ).
References:  5
Autoreceptor: autoinhibitory control.
Species:  Mouse
Tissue:  In vivo (dorsal raphe nucleus).
References:  9
Regulation of cholinergic, GABAergic and glutamatergic transmission and hence cognitive performance.
Species:  Mouse
Tissue:  In vivo.
References:  47
Regulation of anxiety-like behaviour.
Species:  Mouse
Tissue:  In vivo.
References:  39
Regulation of stress responses and locomotor activity.
Species:  Mouse
Tissue:  In vivo (hypothalamus).
References:  44
Regulation of aggressive bahaviour.
Species:  Rat
Tissue:  In vivo.
References:  74
Regulation of feeding behaviour by inducing preproNPY mRNA expression.
Species:  Rat
Tissue:  In vivo (arcuate nucleus).
References:  70
Facilitation of autoshaped learning.
Species:  Mouse
Tissue:  In vivo.
References:  69
Regulation of hippocampal functions.
Species:  Rat
Tissue:  In vivo.
References:  11
Antinociception.
Species:  Rat
Tissue:  In vivo.
References:  25,82
Physiological Consequences of Altering Gene Expression
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:  10
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.