Nomenclature: 5-HT1A receptor

Family: 5-Hydroxytryptamine receptors

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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 17,81
Mouse 7 421 13 D2.1 Htr1a 5-hydroxytryptamine (serotonin) receptor 1A 12
Rat 7 422 2q16 Htr1a 5-hydroxytryptamine (serotonin) receptor 1A, G protein-coupled 2,19
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 Ligand(s)
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 25
pKd 8.9 (Kd 1.4x10-9 M) [25]
[3H]8-OH-DPAT Hs Full agonist 6.0 – 9.4 pKd 7,30,56,59
pKd 6.0 – 9.4 (Kd 3.98x10-10 – 1x10-6 M) [7,30,56,59]
[3H]S-15535 Hs Partial agonist 5.8 – 5.9 pKd 59
pKd 5.8 – 5.9 [59]
S-14671 Hs Full agonist 10.2 – 10.5 pKi 57,59
pKi 10.2 – 10.5 [57,59]
LY293284 Hs Full agonist 10.1 pKi 7
pKi 10.1 [7]
5-CT Hs Full agonist 9.4 – 10.3 pKi 55,57,59-60
pKi 9.4 – 10.3 [55,57,59-60]
lisuride Hs Full agonist 9.7 – 9.8 pKi 47,55,59
pKi 9.7 – 9.8 [47,55,59]
U92016A Hs Full agonist 9.7 pKi 44
pKi 9.7 [44]
roxindole Hs Partial agonist 9.4 – 9.9 pKi 47,56
pKi 9.4 – 9.9 [47,56]
S-14506 Hs Full agonist 9.6 – 9.7 pKi 57,59
pKi 9.6 – 9.7 [57,59]
5-HT Hs Full agonist 9.1 – 9.7 pKi 30,55-57,59-60
pKi 9.1 – 9.7 [30,55-57,59-60]
L-694,247 Hs Full agonist 9.3 pKi 55
pKi 9.3 [55]
(+)-flesinoxan Hs Full agonist 9.3 pKi 57
pKi 9.3 [57]
S-15535 Hs Partial agonist 9.2 pKi 59
pKi 9.2 [59]
LSD Hs Full agonist 9.0 pKi 61
pKi 9.0 [61]
RU 24969 Hs Full agonist 9.0 pKi 57
pKi 9.0 [57]
8-OH-DPAT Hs Full agonist 8.4 – 9.4 pKi 14,22,30,38,48,57,59-60
pKi 8.4 – 9.4 [14,22,30,38,48,57,59-60]
LY 165,163 Hs Full agonist 8.9 pKi 57
pKi 8.9 [57]
spiroxatrine Hs Full agonist 8.8 pKi 57
pKi 8.8 [57]
ipsapirone Hs Partial agonist 8.6 – 8.8 pKi 57,59
pKi 8.6 – 8.8 [57,59]
pergolide Hs Partial agonist 8.7 pKi 47
pKi 8.7 [47]
FG-5893 Hs Full agonist 8.7 pKi 57
pKi 8.7 [57]
7-methoxy-1-naphthylpiperazine Hs Full agonist 8.6 pKi 29
pKi 8.6 [29]
F15599 Hs Full agonist 8.6 pKi 58
pKi 8.6 [58]
(R)-UH 301 Hs Partial agonist 8.6 pKi 57
pKi 8.6 (Ki 2.74x10-9 M) [57]
terguride Hs Partial agonist 8.5 pKi 47
pKi 8.5 [47]
ziprasidone Hs Partial agonist 7.9 – 8.9 pKi 57,77
pKi 7.9 – 8.9 [57,77]
S 16924 Hs Partial agonist 8.4 pKi 45
pKi 8.4 [45]
aripiprazole Hs Full agonist 8.2 pKi 79
pKi 8.2 [79]
tandospirone Hs Full agonist 8.2 pKi 57
pKi 8.2 [57]
asenapine Hs Full agonist 8.0 – 8.3 pKi 57,77
pKi 8.0 – 8.3 [57,77]
zalospirone Hs Full agonist 8.1 pKi 57
pKi 8.1 [57]
1-naphthylpiperazine Hs Full agonist 8.0 pKi 29
pKi 8.0 [29]
ocaperidone Hs Full agonist 8.0 pKi 20
pKi 8.0 [20]
bromocriptine Hs Partial agonist 7.9 pKi 47
pKi 7.9 [47]
buspirone Hs Partial agonist 7.7 – 8.0 pKi 57,59-60
pKi 7.7 – 8.0 [57,59-60]
LY334370 Hs Full agonist 7.8 pKi 82
pKi 7.8 [82]
cabergoline Hs Full agonist 7.7 pKi 47
pKi 7.7 [47]
BRL-15572 Hs Partial agonist 7.7 pKi 71
pKi 7.7 [71]
donitriptan Hs Full agonist 7.6 pKi 28
pKi 7.6 [28]
eletriptan Hs Full agonist 7.4 pKi 54
pKi 7.4 [54]
naratriptan Hs Full agonist 7.1 – 7.6 pKi 54-55
pKi 7.1 – 7.6 [54-55]
nafadotride Hs Full agonist 7.3 pKi 57
pKi 7.3 [57]
BMY-14802 Hs Full agonist 7.2 pKi 57
pKi 7.2 [57]
xanomeline Hs Full agonist 7.2 pKi 84
pKi 7.2 [84]
GR-127935 Hs Partial agonist 7.1 – 7.2 pKi 29,71
pKi 7.1 – 7.2 [29,71]
apomorphine Hs Partial agonist 6.9 pKi 47
pKi 6.9 [47]
clozapine Hs Full agonist 6.8 – 6.9 pKi 45,57,77
pKi 6.8 – 6.9 [45,57,77]
fluparoxan Hs Partial agonist 6.8 pKi 48
pKi 6.8 [48]
EMDT Hs Full agonist 6.8 pKi 21
pKi 6.8 [21]
zolmitriptan Hs Full agonist 6.6 pKi 54
pKi 6.6 [54]
quetiapine Hs Full agonist 6.5 – 6.6 pKi 57,77
pKi 6.5 – 6.6 [57,77]
rizatriptan Hs Full agonist 6.4 pKi 54
pKi 6.4 [54]
piribedil Hs Partial agonist 6.4 pKi 47
pKi 6.4 [47]
SB 216641 Hs Partial agonist 6.3 pKi 71
pKi 6.3 [71]
LY344864 Hs Full agonist 6.3 pKi 67
pKi 6.3 [67]
CP 93129 Hs Full agonist 6.1 pKi 55
pKi 6.1 [55]
sumatriptan Hs Full agonist 6.0 pKi 54
pKi 6.0 [54]
SL65.0155 Hs Partial agonist 6.0 pKi 51
pKi 6.0 [51]
(-)-quinpirole Hs Full agonist 5.8 pKi 56
pKi 5.8 [56]
olanzapine Hs Full agonist 5.6 – 5.8 pKi 57,77
pKi 5.6 – 5.8 [57,77]
BMY-7378 Hs Partial agonist 6.8 – 8.0 pIC50 33
pIC50 6.8 – 8.0 [33]
L-772,405 Hs Full agonist 7.2 pIC50 75
pIC50 7.2 [75]
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 26
pKd 9.8 (Kd 1.58x10-10 M) [26]
[3H]WAY100635 Hs Antagonist 9.5 pKd 33
pKd 9.5 (Kd 3x10-10 M) [33]
[3H]p-MPPF Hs Antagonist 8.4 pKd 30
pKd 8.4 [30]
Rec 15/3079 Hs Antagonist 9.7 pKi 39
pKi 9.7 [39]
NAN 190 Hs Antagonist 9.4 pKi 57
pKi 9.4 [57]
repinotan Hs Antagonist 9.4 pKi 14
pKi 9.4 [14]
NAD 299 Hs Antagonist 9.2 pKi 27
pKi 9.2 [27]
SB 649915 Hs Antagonist 8.6 pKi 83
pKi 8.6 [83]
WAY-100635 Hs Antagonist 7.9 – 9.2 pKi 57,59
pKi 7.9 – 9.2 [57,59]
p-MPPI Hs Antagonist 8.4 pKi 30
pKi 8.4 [30]
tiospirone Hs Antagonist 8.3 pKi 57
pKi 8.3 [57]
(-)-tertatolol Hs Antagonist 8.2 pKi 38,57
pKi 8.2 [38,57]
pindolol Hs Antagonist 8.1 pKi 59
pKi 8.1 [59]
SB 272183 Hs Antagonist 8.0 pKi 85
pKi 8.0 [85]
WAY-100135 Hs Antagonist 8.0 pKi 59
pKi 8.0 [59]
methiothepin Hs Antagonist 7.8 – 8.1 pKi 57,59
pKi 7.8 – 8.1 [57,59]
(S)-UH 301 Hs Antagonist 7.9 pKi 57
pKi 7.9 (Ki 1.35x10-8 M) [57]
spiperone Hs Antagonist 6.7 – 8.8 pKi 57,59-60
pKi 6.7 – 8.8 [57,59-60]
(S)-flurocarazolol Hs Antagonist 7.5 pKi 74
pKi 7.5 [74]
(-)-propranolol Hs Antagonist 7.5 pKi 55
pKi 7.5 [55]
pizotifen Hs Antagonist 7.4 pKi 55
pKi 7.4 [55]
yohimbine Hs Antagonist 7.3 pKi 48
pKi 7.3 [48]
GR 125,743 Hs Antagonist 7.3 pKi 55
pKi 7.3 [55]
fluspirilene Hs Antagonist 7.2 pKi 77
pKi 7.2 [77]
thioridazine Hs Antagonist 7.1 pKi 57
pKi 7.1 [57]
iloperidone Hs Antagonist 7.0 pKi 31
pKi 7.0 [31]
iloperidone Rn Antagonist 6.8 pKi 34
pKi 6.8 [34]
pimozide Hs Antagonist 6.8 pKi 57
pKi 6.8 [57]
GR 218,231 Hs Antagonist 6.8 pKi 46
pKi 6.8 [46]
zotepine Hs Antagonist 6.5 pKi 77
pKi 6.5 [77]
SB 714786 Hs Antagonist 6.5 pKi 83
pKi 6.5 [83]
(R)-flurocarazolol Hs Antagonist 6.5 pKi 74
pKi 6.5 [74]
sertindole Hs Antagonist 6.4 – 6.6 pKi 57,77
pKi 6.4 – 6.6 [57,77]
risperidone Hs Antagonist 6.4 – 6.5 pKi 57,77
pKi 6.4 – 6.5 [57,77]
(+)-butaclamol Hs Antagonist 6.4 pKi 57
pKi 6.4 [57]
cyamemazine Hs Antagonist 6.3 pKi 22
pKi 6.3 [22]
risperidone Rn Antagonist 6.2 pKi 34
pKi 6.2 [34]
9-OH-risperidone Hs Antagonist 6.2 pKi 77
pKi 6.2 [77]
chlorpromazine Hs Antagonist 6.2 pKi 57
pKi 6.2 [57]
MPDT Hs Antagonist 5.8 pKi 21
pKi 5.8 [21]
haloperidol Hs Antagonist 5.7 – 5.8 pKi 38,45,57,77
pKi 5.7 – 5.8 [38,45,57,77]
pipamperone Hs Antagonist 5.6 pKi 77
pKi 5.6 [77]
raclopride Hs Antagonist 5.2 pKi 57
pKi 5.2 [57]
ketanserin Hs Antagonist 5.0 pKi 60
pKi 5.0 [60]
SDZ-216525 Hs Antagonist 7.8 – 8.2 pIC50 33
pIC50 7.8 – 8.2 [33]
ritanserin Hs Antagonist 5.2 – 5.5 pIC50 33
pIC50 5.2 – 5.5 [33]
View species-specific antagonist tables
Allosteric Regulators
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 – 7.6 pKi 80
pKi 7.1 – 7.6 [80]
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:  1,17,41
Secondary Transduction Mechanisms
Transducer Effector/Response
Phospholipase C stimulation
References:  17
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:  73
Benign and malignant prostate tissue.
Species:  Human
Technique:  Western blotting.
References:  16
Poorly expressed in coronary arteries, atrium, ventricle and epicardium.
Species:  Human
Technique:  RT-PCR.
References:  62
Spinal cord: dorsal horn > ventral horn.
Species:  Human
Technique:  Radioligand binding.
References:  37
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:  11
Peritoneal macrophages.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  18
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:  69
Superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  68
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:  32
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:  73
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:  17
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:  12
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 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:  20
Measurement of phosphorylated ERK1/2 levels in the rat hippocampus.
Species:  Rat
Tissue:  Hippocampus.
Response measured:  Inhibition of the Erk1/2 MAPK pathway.
References:  13
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:  17,60
Physiological Functions
Stimulation of cell proliferation.
Species:  Human
Tissue:  DU145, PC-3, LNCaP and hPCP prostatic cell lines.
References:  16
Increase in phagocytic activity.
Species:  Mouse
Tissue:  Peritoneal macrophages.
References:  18
Hyperpolarisation of orexin neurons.
Species:  Mouse
Tissue:  Hypothalamus.
References:  52
Regulation of sleep-wakefulness cycles.
Species:  Rat
Tissue:  In vivo.
References:  49-50
Regulation of sleep-wakefulness cycles.
Species:  Mouse
Tissue:  In vivo.
References:  9
Regulation of epileptic activity.
Species:  Rat
Tissue:  In vivo.
References:  42
Regulation of oxytocin and adrenocorticotropin hormone release.
Species:  Rat
Tissue:  In vivo (paraventricular nucleus).
References:  63
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:  8
Regulation of cholinergic, GABAergic and glutamatergic transmission and hence cognitive performance.
Species:  Mouse
Tissue:  In vivo.
References:  43
Regulation of anxiety-like behaviour.
Species:  Mouse
Tissue:  In vivo.
References:  35
Regulation of stress responses and locomotor activity.
Species:  Mouse
Tissue:  In vivo (hypothalamus).
References:  40
Regulation of aggressive bahaviour.
Species:  Rat
Tissue:  In vivo.
References:  70
Regulation of feeding behaviour by inducing preproNPY mRNA expression.
Species:  Rat
Tissue:  In vivo (arcuate nucleus).
References:  66
Facilitation of autoshaped learning.
Species:  Mouse
Tissue:  In vivo.
References:  65
Regulation of hippocampal functions.
Species:  Rat
Tissue:  In vivo.
References:  10
Antinociception.
Species:  Rat
Tissue:  In vivo.
References:  23,78
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:  9
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:  8
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:  35
Temporary 5-HT1A receptor overexpression during embryonic and perinatal development causes long-term memory impairment.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  6
5-HT1A receptor knockout mice show increases in typical anxiety and stress responses.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  24,64,72
5-HT1A receptor knockout mice exhibit down-regulation of the 5-HT transporter.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  3
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:  76
5-HT1A receptor knockout mice exhibit altered decision making abilities and response inhibition.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  65
Phenotypes, Alleles and Disease Models 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
Disease:  Periodic fever, menstrual cycle dependent
OMIM:  614674
References: 
Mutations not determined
Biologically Significant Variants
Type:  Single nucletide 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:  53
Type:  Single nucleotide polymorphism.
Species:  Human
Description:  The polymorphism Arg219 -> Leu has been associated with Tourette's syndrome.
References:  36
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:  15
Available Assays
DiscoveRx PathHunter® CHO-K1 HTR1A β-Arrestin Cell Line (Cat no. 93-0696C2)
PathHunter® eXpress HTR1A CHO-K1 β-Arrestin GPCR Assay (Cat no. 93-0696E2CP0M)
more info

REFERENCES

1. Albert PR, Sajedi N, Lemonde S, Gha