image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates. 

5-HT1A receptor

Family: 5-Hydroxytryptamine receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Allosteric Regulators
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
Biologically Significant Variants
References
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 51 (Hs), 11863 (Mm), 10576 (Rn)
DrugBank Target 320 (Hs)
Ensembl ENSG00000178394 (Hs), ENSMUSG00000021721 (Mm), ENSRNOG00000010254 (Rn)
Entrez Gene 3350 (Hs), 15550 (Mm), 24473 (Rn)
GeneCards HTR1A (Hs)
GenitoUrinary Development Molecular Anatomy Project Htr1a (Mm)
HomoloGene 20148 (Hs)
Human Protein Reference Database 00190 (Hs)
InterPro P08908 (Hs), Q64264 (Mm), P19327 (Rn)
KEGG Gene hsa:3350 (Hs), mmu:15550 (Mm), rno:24473 (Rn)
OMIM 109760 (Hs)
PharmGKB Gene PA192 (Hs)
PhosphoSitePlus P08908 (Hs), Q64264 (Mm), P19327 (Rn)
Protein Ontology (PRO) PRO:000001161 (Hs)
RefSeq Nucleotide NM_000524 (Hs), NM_008308 (Mm), NM_012585 (Rn)
RefSeq Protein NP_000515 (Hs), NP_032334 (Mm), NP_036717 (Rn)
TreeFam ENSG00000178394 (Hs), ENSMUSG00000021721 (Mm), ENSRNOG00000010254 (Rn)
UniGene Hs. 247940 (Hs)
UniProt P08908 (Hs), Q64264 (Mm), P19327 (Rn)
Wikipedia 5-HT1A receptor
5-Hydroxytryptamine receptors
Search for 3D structures on the PDB
Search by keyword: 5-Hydroxytryptamine receptors 5-HT1A receptor Search by accession number: P19327, P08908, Q64264
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
[3H]8-OH-DPAT Hs Full agonist 6.0 – 9.4 pKd 7,30,56,58
[3H]S-15535 Hs Partial agonist 5.8 – 5.9 pKd 58
S-14671 Hs Full agonist 10.2 – 10.5 pKi 57-58
LY293284 Hs Full agonist 10.1 pKi 7
5-CT Hs Full agonist 9.4 – 10.3 pKi 55,57-59
lisuride Hs Full agonist 9.7 – 9.8 pKi 47,55,58
U92016A Hs Full agonist 9.7 pKi 44
roxindole Hs Partial agonist 9.4 – 9.9 pKi 47,56
S-14506 Hs Full agonist 9.6 – 9.7 pKi 57-58
5-HT Hs Full agonist 9.1 – 9.7 pKi 30,55-59
(+)-flesinoxan Hs Full agonist 9.3 pKi 57
L-694,247 Hs Full agonist 9.3 pKi 55
S-15535 Hs Partial agonist 9.2 pKi 58
LSD Hs Full agonist 9.0 pKi 61
RU 24969 Hs Full agonist 9.0 pKi 57
8-OH-DPAT Hs Full agonist 8.4 – 9.4 pKi 14,22,30,38,48,57-59
LY 165,163 Hs Full agonist 8.9 pKi 57
spiroxatrine Hs Full agonist 8.8 pKi 57
ipsapirone Hs Partial agonist 8.6 – 8.8 pKi 57-58
FG-5893 Hs Full agonist 8.7 pKi 57
pergolide Hs Partial agonist 8.7 pKi 47
7-methoxy-1-naphthylpiperazine Hs Full agonist 8.6 pKi 29
F15599 Hs Full agonist 8.6 pKi 60
(R)-UH 301 Hs Partial agonist 8.6 pKi 57
terguride Hs Partial agonist 8.5 pKi 47
S 16924 Hs Partial agonist 8.4 pKi 45
ziprasidone Hs Partial agonist 7.9 – 8.9 pKi 57,77
aripiprazole Hs Full agonist 8.2 pKi 79
tandospirone Hs Full agonist 8.2 pKi 57
asenapine Hs Full agonist 8.0 – 8.3 pKi 57,77
zalospirone Hs Full agonist 8.1 pKi 57
1-naphthylpiperazine Hs Full agonist 8.0 pKi 29
ocaperidone Hs Full agonist 8.0 pKi 20
bromocriptine Hs Partial agonist 7.9 pKi 47
buspirone Hs Partial agonist 7.7 – 8.0 pKi 57-59
LY334370 Hs Full agonist 7.8 pKi 82
BRL-15572 Hs Partial agonist 7.7 pKi 71
cabergoline Hs Full agonist 7.7 pKi 47
donitriptan Hs Full agonist 7.6 pKi 28
eletriptan Hs Full agonist 7.4 pKi 54
naratriptan Hs Full agonist 7.1 – 7.6 pKi 54-55
nafadotride Hs Full agonist 7.3 pKi 57
BMY-14802 Hs Full agonist 7.2 pKi 57
xanomeline Hs Full agonist 7.2 pKi 84
GR-127935 Hs Partial agonist 7.1 – 7.2 pKi 29,71
apomorphine Hs Partial agonist 6.9 pKi 47
clozapine Hs Full agonist 6.8 – 6.9 pKi 45,57,77
EMDT Hs Full agonist 6.8 pKi 21
fluparoxan Hs Partial agonist 6.8 pKi 48
zolmitriptan Hs Full agonist 6.6 pKi 54
quetiapine Hs Full agonist 6.5 – 6.6 pKi 57,77
piribedil Hs Partial agonist 6.4 pKi 47
rizatriptan Hs Full agonist 6.4 pKi 54
LY344864 Hs Full agonist 6.3 pKi 67
SB 216641 Hs Partial agonist 6.3 pKi 71
CP 93129 Hs Full agonist 6.1 pKi 55
SL65.0155 Hs Partial agonist 6.0 pKi 51
sumatriptan Hs Full agonist 6.0 pKi 54
(-)-quinpirole Hs Full agonist 5.8 pKi 56
olanzapine Hs Full agonist 5.6 – 5.8 pKi 57,77
BMY-7378 Hs Partial agonist 6.8 – 8.0 pIC50 33
L-772,405 Hs Full agonist 7.2 pIC50 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
[3H]WAY100635 Hs Antagonist 9.5 pKd 33
[3H]p-MPPF Hs Antagonist 8.4 pKd 30
Rec 15/3079 Hs Antagonist 9.7 pKi 39
NAN 190 Hs Antagonist 9.4 pKi 57
repinotan Hs Antagonist 9.4 pKi 14
NAD 299 Hs Antagonist 9.2 pKi 27
SB 649915 Hs Antagonist 8.6 pKi 83
WAY-100635 Hs Antagonist 7.9 – 9.2 pKi 57-58
p-MPPI Hs Antagonist 8.4 pKi 30
tiospirone Hs Antagonist 8.3 pKi 57
(-)-tertatolol Hs Antagonist 8.2 pKi 38,57
pindolol Hs Antagonist 8.1 pKi 58
SB 272183 Hs Antagonist 8.0 pKi 85
WAY-100135 Hs Antagonist 8.0 pKi 58
methiothepin Hs Antagonist 7.8 – 8.1 pKi 57-58
(S)-UH 301 Hs Antagonist 7.9 pKi 57
spiperone Hs Antagonist 6.7 – 8.8 pKi 57-59
(-)-propranolol Hs Antagonist 7.5 pKi 55
(S)-flurocarazolol Hs Antagonist 7.5 pKi 74
pizotifen Hs Antagonist 7.4 pKi 55
GR 125,743 Hs Antagonist 7.3 pKi 55
yohimbine Hs Antagonist 7.3 pKi 48
fluspirilene Hs Antagonist 7.2 pKi 77
thioridazine Hs Antagonist 7.1 pKi 57
iloperidone Hs Antagonist 7.0 pKi 31
GR 218,231 Hs Antagonist 6.8 pKi 46
iloperidone Rn Antagonist 6.8 pKi 34
pimozide Hs Antagonist 6.8 pKi 57
(R)-flurocarazolol Hs Antagonist 6.5 pKi 74
SB 714786 Hs Antagonist 6.5 pKi 83
sertindole Hs Antagonist 6.4 – 6.6 pKi 57,77
zotepine Hs Antagonist 6.5 pKi 77
risperidone Hs Antagonist 6.4 – 6.5 pKi 57,77
(+)-butaclamol Hs Antagonist 6.4 pKi 57
cyamemazine Hs Antagonist 6.3 pKi 22
9-OH-risperidone Hs Antagonist 6.2 pKi 77
chlorpromazine Hs Antagonist 6.2 pKi 57
risperidone Rn Antagonist 6.2 pKi 34
MPDT Hs Antagonist 5.8 pKi 21
haloperidol Hs Antagonist 5.7 – 5.8 pKi 38,45,57,77
pipamperone Hs Antagonist 5.6 pKi 77
raclopride Hs Antagonist 5.2 pKi 57
ketanserin Hs Antagonist 5.0 pKi 59
SDZ-216525 Hs Antagonist 7.8 – 8.2 pIC50 33
ritanserin Hs Antagonist 5.2 – 5.5 pIC50 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

Explore drug-target interactions for this set of compounds using iPHACE

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

Click here to show/hide data

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]

There should be a chart of expression data here, you may need to enable JavaScript!
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:  17,59
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

Click here to show/hide data

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 
Biologically Significant Variants
Two polymorphisms, Gly22 -> Ser and Ile28 -> Val, have been found to alter the extracellular amino terminal region of the receptor.
Type:  Single nucletide polymorphisms.
Species:  Human
References:  53
The polymorphism Arg219 -> Leu has been associated with Tourette's syndrome.
Type:  Single nucleotide polymorphism.
Species:  Human
References:  36
The polymorphism Ala50 -> Val, occurring in transmembrane 1, results in a loss of response to 5-HT.
Type:  Single nucleotide polymorphism.
Species:  Human
References:  15

REFERENCES

Show »

1. Albert, P. R., Sajedi, N., Lemonde, S. and Ghahremani, M. H. (1999) Constitutive G(i2)-dependent activation of adenylyl cyclase type II by the 5-HT1A receptor. Inhibition by anxiolytic partial agonists. J Biol Chem, 274: 35469-35474. [PMID:10585418]

2. Albert, P. R., Zhou, Q. Y., Van Tol, H. H., Bunzow, J. R. and Civelli, O. (1990) Cloning, functional expression, and mRNA tissue distribution of the rat 5-hydroxytryptamine1A receptor gene. J Biol Chem, 265: 5825-5832. [PMID:2156831]

3. Ase, A. R., Reader, T. A., Hen, R., Riad, M. and Descarries, L. (2001) Regional changes in density of serotonin transporter in the brain of 5-HT1A and 5-HT1B knockout mice, and of serotonin innervation in the 5-HT1B knockout. J Neurochem, 78: 619-630. [PMID:11483665]

4. Aznar, S., Qian, Z., Shah, R., Rahbek, B. and Knudsen, G. M. (2003) The 5-HT1A serotonin receptor is located on calbindin- and parvalbumin-containing neurons in the rat brain. Brain Res, 959: 58-67. [PMID:12480158]

5. Banasr, M., Hery, M., Printemps, R. and Daszuta, A. (2004) Serotonin-induced increases in adult cell proliferation and neurogenesis are mediated through different and common 5-HT receptor subtypes in the dentate gyrus and the subventricular zone. Neuropsychopharmacology, 29: 450-460. [PMID:14872203]

6. Bert, B., Dere, E., Wilhelmi, N., Kusserow, H., Theuring, F., Huston, J. P. and Fink, H. (2005) Transient overexpression of the 5-HT1A receptor impairs water-maze but not hole-board performance. Neurobiol Learn Mem, 84: 57-68. [PMID:15936683]

7. Blair, J. B., Kurrasch-Orbaugh, D., Marona-Lewicka, D., Cumbay, M. G., Watts, V. J., Barker, E. L. and Nichols, D. E. (2000) Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. J Med Chem, 43: 4701-4710. [PMID:11101361]

8. Bortolozzi, A., Amargos-Bosch, M., Toth, M., Artigas, F. and Adell, A. (2004) In vivo efflux of serotonin in the dorsal raphe nucleus of 5-HT1A receptor knockout mice. J Neurochem, 88: 1373-1379. [PMID:15009637]

9. Boutrel, B., Monaca, C., Hen, R., Hamon, M. and Adrien, J. (2002) Involvement of 5-HT1A receptors in homeostatic and stress-induced adaptive regulations of paradoxical sleep: studies in 5-HT1A knock-out mice. J Neurosci, 22: 4686-4692. [PMID:12040075]

10. Buhot, M. C. and Naili, S. (1995) Changes in exploratory activity following stimulation of hippocampal 5-HT1A and 5-HT1B receptors in the rat. Hippocampus, 5: 198-208. [PMID:7550615]

11. Burnet, P. W., Eastwood, S. L., Lacey, K. and Harrison, P. J. (1995) The distribution of 5-HT1A and 5-HT2A receptor mRNA in human brain. Brain Res, 676: 157-168. [PMID:7796165]

12. Charest, A., Wainer, B. H. and Albert, P. R. (1993) Cloning and differentiation-induced expression of a murine serotonin1A receptor in a septal cell line. J Neurosci, 13: 5164-5171. [PMID:8254366]

13. Chen, J., Shen, C. and Meller, E. (2002) 5-HT1A receptor-mediated regulation of mitogen-activated protein kinase phosphorylation in rat brain. Eur J Pharmacol, 452: 155-162. [PMID:12354565]

14. De Vry, J., Schohe-Loop, R., Heine, H. G., Greuel, J. M., Mauler, F., Schmidt, B., Sommermeyer, H. and Glaser, T. (1998) Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist. J Pharmacol Exp Ther, 284: 1082-1094. [PMID:9495870]

15. Del Tredici, A. L., Schiffer, H. H., Burstein, E. S., Lameh, J., Mohell, N., Hacksell, U., Brann, M. R. and Weiner, D. M. (2004) Pharmacology of polymorphic variants of the human 5-HT1A receptor. Biochem Pharmacol, 67: 479-490. [PMID:15037200]

16. Dizeyi, N., Bjartell, A., Nilsson, E., Hansson, J., Gadaleanu, V., Cross, N. and Abrahamsson, P. A. (2004) Expression of serotonin receptors and role of serotonin in human prostate cancer tissue and cell lines. Prostate, 59: 328-336. [PMID:15042609]

17. Fargin, A., Raymond, J. R., Regan, J. W., Cotecchia, S., Lefkowitz, R. J. and Caron, M. G. (1989) Effector coupling mechanisms of the cloned 5-HT1A receptor. J Biol Chem, 264: 14848-14852. [PMID:2549039]

18. Freire-Garabal, M., Nunez, M. J., Balboa, J., Lopez-Delgado, P., Gallego, R., Garcia-Caballero, T., Fernandez-Roel, M. D., Brenlla, J. and Rey-Mendez, M. (2003) Serotonin upregulates the activity of phagocytosis through 5-HT1A receptors. Br J Pharmacol, 139: 457-463. [PMID:12770951]

19. Fujiwara, Y., Nelson, D. L., Kashihara, K., Varga, E., Roeske, W. R. and Yamamura, H. I. (1990) The cloning and sequence analysis of the rat serotonin-1A receptor gene. Life Sci, 47: 127-132. [PMID:2273937]

20. Garnovskaya, M. N., Gettys, T. W., van Biesen, T., Prpic, V., Chuprun, J. K. and Raymond, J. R. (1997) 5-HT1A receptor activates Na+/H+ exchange in CHO-K1 cells through Gialpha2 and Gialpha3. J Biol Chem, 272: 7770-7776. [PMID:9065439]

21. Glennon, R. A., Lee, M., Rangisetty, J. B., Dukat, M., Roth, B. L., Savage, J. E., McBride, A., Rauser, L., Hufeisen, S. and Lee, D. K. (2000) 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem, 43: 1011-1018. [PMID:10715164]

22. Hameg, A., Bayle, F., Nuss, P., Dupuis, P., Garay, R. P. and Dib, M. (2003) Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol, 65: 435-440. [PMID:12527336]

23. Harte, S. E., Kender, R. G. and Borszcz, G. S. (2005) Activation of 5-HT1A and 5-HT7 receptors in the parafascicular nucleus suppresses the affective reaction of rats to noxious stimulation. Pain, 113: 405-415. [PMID:15661450]

24. Heisler, L. K., Chu, H. M., Brennan, T. J., Danao, J. A., Bajwa, P., Parsons, L. H. and Tecott, L. H. (1998) Elevated anxiety and antidepressant-like responses in serotonin 5-HT1A receptor mutant mice. Proc Natl Acad Sci U S A, 95: 15049-15054. [PMID:9844013]

25. Heusler, P; Palmier, C; Tardif, S; Bernois, S; Colpaert, FC; Cussac, D. (2010) [(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand. Naunyn Schmiedebergs Arch. Pharmacol., 382 (4): 321-30. [PMID:20799027]

26. Jerning, E., Svantesson, G. T. and Mohell, N. (1998) Receptor binding characteristics of [3H]NAD-299, a new selective 5-HT1A receptor antagonist. Eur J Pharmacol, 360: 219-225. [PMID:9851589]

27. Johansson, L., Sohn, D., Thorberg, S. O., Jackson, D. M., Kelder, D., Larsson, L. G., Renyi, L., Ross, S. B., Wallsten, C., Eriksson, H., Hu, P. S., Jerning, E., Mohell, N. and Westlind-Danielsson, A. (1997) The pharmacological characterization of a novel selective 5-hydroxytryptamine1A receptor antagonist, NAD-299. J Pharmacol Exp Ther, 283: 216-225. [PMID:9336327]

28. John, G. W., Pauwels, P. J., Perez, M., Halazy, S., Le Grand, B., Verscheure, Y., Valentin, J. P., Palmier, C., Wurch, T., Chopin, P., Marien, M., Kleven, M. S., Koek, W., Assie, M. B., Carilla-Durand, E., Tarayre, J. P. and Colpaert, F. C. (1999) F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine. J Pharmacol Exp Ther, 290: 83-95. [PMID:10381763]

29. Jorand-Lebrun, C., Pauwels, P. J., Palmier, C., Moret, C., Chopin, P., Perez, M., Marien, M. and Halazy, S. (1997) 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J Med Chem, 40: 3974-3978. [PMID:9397179]

30. Kalipatnapu, S., Pucadyil, T. J., Harikumar, K. G. and Chattopadhyay, A. (2004) Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. Biosci Rep, 24: 101-115. [PMID:15628665]

31. Kalkman, H. O., Subramanian, N. and Hoyer, D. (2001) Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders. Neuropsychopharmacology, 25: 904-914. [PMID:11750183]

32. Kaya, N., Shen, T., Lu, S. G., Zhao, F. L. and Herness, S. (2004) A paracrine signaling role for serotonin in rat taste buds: expression and localization of serotonin receptor subtypes. Am J Physiol Regul Integr Comp Physiol, 286: R649-R658. [PMID:14715493]

33. Khawaja, X., Ennis, C. and Minchin, M. C. (1997) Pharmacological characterization of recombinant human 5-hydroxytryptamine1A receptors using a novel antagonist radioligand, [3H]WAY-100635. Life Sci, 60: 653-665. [PMID:9048968]

34. Kongsamut, S., Roehr, J. E., Cai, J., Hartman, H. B., Weissensee, P., Kerman, L. L., Tang, L. and Sandrasagra, A. (1996) Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol, 317: 417-423. [PMID:8997630]

35. Kusserow, H., Davies, B., Hortnagl, H., Voigt, I., Stroh, T., Bert, B., Deng, D. R., Fink, H., Veh, R. W. and Theuring, F. (2004) Reduced anxiety-related behaviour in transgenic mice overexpressing serotonin 1A receptors. Brain Res Mol Brain Res, 129: 104-116. [PMID:15469887]

36. Lam, S., Shen, Y., Nguyen, T., Messier, T. L., Brann, M., Comings, D., George, S. R. and O'Dowd, B. F. (1996) A serotonin receptor gene (5HT1A) variant found in a Tourette's syndrome patient. Biochem Biophys Res Commun, 219: 853-858. [PMID:8645269]

37. Laporte, A. M., Doyen, C., Nevo, I. T., Chauveau, J., Hauw, J. J. and Hamon, M. (1996) Autoradiographic mapping of serotonin 5-HT1A, 5-HT1D, 5-HT2A and 5-HT3 receptors in the aged human spinal cord. J Chem Neuroanat, 11: 67-75. [PMID:8841890]

38. Lejeune, F., Newman-Tancredi, A., Audinot, V. and Millan, M. J. (1997) Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats. J Pharmacol Exp Ther, 280: 1241-1249. [PMID:9067310]

39. Leonardi, A., Guarneri, L., Poggesi, E., Angelico, P., Velasco, C., Cilia, A. and Testa, R. (2001) N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract. J Pharmacol Exp Ther, 299: 1027-1037. [PMID:11714892]

40. Li, Q., Holmes, A., Ma, L., Van de Kar, L. D., Garcia, F. and Murphy, D. L. (2004) Medial hypothalamic 5-hydroxytryptamine (5-HT)1A receptors regulate neuroendocrine responses to stress and exploratory locomotor activity: application of recombinant adenovirus containing 5-HT1A sequences. J Neurosci, 24: 10868-10877. [PMID:15574737]

41. Lin, S. L., Setya, S., Johnson-Farley, N. N. and Cowen, D. S. (2002) Differential coupling of 5-HT(1) receptors to G proteins of the G(i) family. Br J Pharmacol, 136: 1072-1078. [PMID:12145108]

42. Lopez-Meraz, M. L., Gonzalez-Trujano, M. E., Neri-Bazan, L., Hong, E. and Rocha, L. L. (2005) 5-HT1A receptor agonists modify epileptic seizures in three experimental models in rats. Neuropharmacology, 49: 367-375. [PMID:15993434]

43. Madjid, N., Elvander Tottie, E., Luttgen, M., Meister, B., Sandin, J., Kuzmin, A., Stiedl, O. and Ogren, S. O. (2005) 5-HT1A Receptor Blockade Facilitates Aversive Learning in Mice: Interactions with Cholinergic and Glutamatergic Mechanisms. J Pharmacol Exp Ther, : -. [PMID:16223872]

44. McCall, R. B., Romero, A. G., Bienkowski, M. J., Harris, D. W., McGuire, J. C., Piercey, M. F., Shuck, M. E., Smith, M. W., Svensson, K. A., Schreur, P. J. et al.. (1994) Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist. J Pharmacol Exp Ther, 271: 875-883. [PMID:7965808]

45. Millan, M. J., Gobert, A., Newman-Tancredi, A., Audinot, V., Lejeune, F., Rivet, J. M., Cussac, D., Nicolas, J. P., Muller, O. and Lavielle, G. (1998) S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol. J Pharmacol Exp Ther, 286: 1341-1355. [PMID:9732398]

46. Millan, M. J., Gobert, A., Newman-Tancredi, A., Lejeune, F., Cussac, D., Rivet, J. M., Audinot, V., Dubuffet, T. and Lavielle, G. (2000) S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626. J Pharmacol Exp Ther, 293: 1048-1062. [PMID:10869410]

47. Millan, M. J., Maiofiss, L., Cussac, D., Audinot, V., Boutin, J. A. and Newman-Tancredi, A. (2002) Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther, 303: 791-804. [PMID:12388666]

48. Millan, M. J., Newman-Tancredi, A., Audinot, V., Cussac, D., Lejeune, F., Nicolas, J. P., Cogé, F., Galizzi, J. P., Boutin, J. A., Rivet, J. M., Dekeyne, A. and Gobert, A. (2000) Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse, 35: 79-95. [PMID:10611634]

49. Monti, J. M. and Jantos, H. (2003) Differential effects of the 5-HT1A receptor agonist flesinoxan given locally or systemically on REM sleep in the rat. Eur J Pharmacol, 478: 121-130. [PMID:14575796]

50. Monti, J. M. and Jantos, H. (2004) Effects of the 5-HT1A receptor ligands flesinoxan and WAY 100635 given systemically or microinjected into the laterodorsal tegmental nucleus on REM sleep in the rat. Behav Brain Res, 151: 159-166. [PMID:15084431]

51. Moser, P. C., Bergis, O. E., Jegham, S., Lochead, A., Duconseille, E., Terranova, J. P., Caille, D., Berque-Bestel, I., Lezoualc'h, F., Fischmeister, R., Dumuis, A., Bockaert, J., George, P., Soubrie, P. and Scatton, B. (2002) SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties. J Pharmacol Exp Ther, 302: 731-741. [PMID:12130738]

52. Muraki, Y., Yamanaka, A., Tsujino, N., Kilduff, T. S., Goto, K. and Sakurai, T. (2004) Serotonergic regulation of the orexin/hypocretin neurons through the 5-HT1A receptor. J Neurosci, 24: 7159-7166. [PMID:15306649]

53. Nakhai, B., Nielsen, D. A., Linnoila, M. and Goldman, D. (1995) Two naturally occurring amino acid substitutions in the human 5-HT1A receptor: glycine 22 to serine 22 and isoleucine 28 to valine 28. Biochem Biophys Res Commun, 210: 530-536. [PMID:7755630]

54. Napier, C., Stewart, M., Melrose, H., Hopkins, B., McHarg, A. and Wallis, R. (1999) Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol, 368: 259-268. [PMID:10193663]

55. Newman-Tancredi, A., Conte, C., Chaput, C., Verriele, L., Audinot-Bouchez, V., Lochon, S., Lavielle, G. and Millan, M. J. (1997) Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy. Naunyn Schmiedebergs Arch Pharmacol, 355: 682-688. [PMID:9205951]

56. Newman-Tancredi, A., Cussac, D., Audinot, V. and Millan, M. J. (1999) Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol, 359: 447-453. [PMID:10431754]

57. Newman-Tancredi, A., Gavaudan, S., Conte, C., Chaput, C., Touzard, M., Verriele, L., Audinot, V. and Millan, M. J. (1998) Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. Eur J Pharmacol, 355: 245-256. [PMID:9760039]

58. Newman-Tancredi, A., Verriele, L., Chaput, C. and Millan, M. J. (1998) Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. Naunyn Schmiedebergs Arch Pharmacol, 357: 205-217. [PMID:9550290]

59. Newman-Tancredi, A., Wootton, R. and Strange, P. G. (1992) High-level stable expression of recombinant 5-HT1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells. Biochem J, 285: 933-938. [PMID:1386736]

60. Newman-Tancredi, A; Martel, JC; Assié, MB; Buritova, J; Lauressergues, E; Cosi, C; Heusler, P; Bruins Slot, L; Colpaert, FC; Vacher, B; et al.. (2009) Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist. Br. J. Pharmacol., 156 (2): 338-53. [PMID:19154445]

61. Nichols, D. E., Frescas, S., Marona-Lewicka, D. and Kurrasch-Orbaugh, D. M. (2002) Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD). J Med Chem, 45: 4344-4349. [PMID:12213075]

62. Nilsson, T., Longmore, J., Shaw, D., Pantev, E., Bard, J. A., Branchek, T. and Edvinsson, L. (1999) Characterisation of 5-HT receptors in human coronary arteries by molecular and pharmacological techniques. Eur J Pharmacol, 372: 49-56. [PMID:10374714]

63. Osei-Owusu, P., James, A., Crane, J. and Scrogin, K. E. (2005) 5-Hydroxytryptamine 1A receptors in the paraventricular nucleus of the hypothalamus mediate oxytocin and adrenocorticotropin hormone release and some behavioral components of the serotonin syndrome. J Pharmacol Exp Ther, 313: 1324-1330. [PMID:15743927]

64. Parks, C. L., Robinson, P. S., Sibille, E., Shenk, T. and Toth, M. (1998) Increased anxiety of mice lacking the serotonin1A receptor. Proc Natl Acad Sci U S A, 95: 10734-10739. [PMID:9724773]

65. Pattij, T., Broersen, L. M., van der Linde, J., Groenink, L., van der Gugten, J., Maes, R. A. and Olivier, B. (2003) Operant learning and differential-reinforcement-of-low-rate 36-s responding in 5-HT1A and 5-HT1B receptor knockout mice. Behav Brain Res, 141: 137-145. [PMID:12742250]

66. Pesonen, U., Rouru, J., Huupponen, R. and Koulu, M. (1991) Effects of repeated administration of mifepristone and 8-OH-DPAT on expression of preproneuropeptide Y mRNA in the arcuate nucleus of obese Zucker rats. Brain Res Mol Brain Res, 10: 267-272. [PMID:1653393]

67. Phebus, L. A., Johnson, K. W., Zgombick, J. M., Gilbert, P. J., Van Belle, K., Mancuso, V., Nelson, D. L., Calligaro, D. O., Kiefer, A. D., Branchek, T. A. and Flaugh, M. E. (1997) Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci, 61: 2117-212. [PMID:9395253]

68. Pierce, P. A., Xie, G. X., Levine, J. D. and Peroutka, S. J. (1996) 5-Hydroxytryptamine receptor subtype messenger RNAs in rat peripheral sensory and sympathetic ganglia: a polymerase chain reaction study. Neuroscience, 70: 553-559. [PMID:8848158]

69. Pompeiano, M., Palacios, J. M. and Mengod, G. (1992) Distribution and cellular localization of mRNA coding for 5-HT1A receptor in the rat brain: correlation with receptor binding. J Neurosci, 12: 440-453. [PMID:1531498]

70. Popova, N. K., Naumenko, V. S., Plyusnina, I. Z. and Kulikov, A. V. (2005) Reduction in 5-HT1A receptor density, 5-HT1A mRNA expression, and functional correlates for 5-HT1A receptors in genetically defined aggressive rats. J Neurosci Res, 80: 286-292. [PMID:15765530]

71. Price, G. W., Burton, M. J., Collin, L. J., Duckworth, M., Gaster, L., Gothert, M., Jones, B. J., Roberts, C., Watson, J. M. and Middlemiss, D. N. (1997) SB-216641 and BRL-15572 compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch. Pharmacol., 356: 312-320. [PMID:9303567]

72. Ramboz, S., Oosting, R., Amara, D. A., Kung, H. F., Blier, P., Mendelsohn, M., Mann, J. J., Brunner, D. and Hen, R. (1998) Serotonin receptor 1A knockout: an animal model of anxiety-related disorder. Proc Natl Acad Sci U S A, 95: 14476-14481. [PMID:9826725]

73. Raymond, J. R., Kim, J., Beach, R. E. and Tisher, C. C. (1993) Immunohistochemical mapping of cellular and subcellular distribution of 5-HT1A receptors in rat and human kidneys. Am J Physiol, 264: 9-19. [PMID:8430834]

74. Roth, B. L., Ernsberger, P., Steinberg, S. A., Rao, S., Rauser, L., Savage, J., Hufeisen, S., Berridge, M. S. and Muzic, R. F. (2001) The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor. Psychopharmacology (Berl), 157: 111-114. [PMID:11512051]

75. Russell, M. G., Matassa, V. G., Pengilley, R. R., van Niel, M. B., Sohal, B., Watt, A. P., Hitzel, L., Beer, M. S., Stanton, J. A., Broughton, H. B. and Castro, J. L. (1999) 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. J Med Chem, 42: 4981-5001. [PMID:10585208]

76. Sarnyai, Z., Sibille, E. L., Pavlides, C., Fenster, R. J., McEwen, B. S. and Toth, M. (2000) Impaired hippocampal-dependent learning and functional abnormalities in the hippocampus in mice lacking serotonin(1A) receptors. Proc Natl Acad Sci U S A, 97: 14731-14736. [PMID:11121072]

77. Schotte, A., Janssen, P. F., Gommeren, W., Luyten, W. H., Van Gompel, P., Lesage, A. S., De Loore, K. and Leysen, J. E. (1996) Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl), 124: 57-73. [PMID:8935801]

78. Shannon, H. E. and Lutz, E. A. (2000) Yohimbine produces antinociception in the formalin test in rats: involvement of serotonin(1A) receptors. Psychopharmacology (Berl), 149: 93-97. [PMID:10789888]

79. Shapiro, D. A., Renock, S., Arrington, E., Chiodo, L. A., Liu, L. X., Sibley, D. R., Roth, B. L. and Mailman, R. (2003) Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology. Neuropsychopharmacology, 28: 1400-1411. [PMID:12784105]

80. Spedding, M., Newman-Tancredi, A., Millan, M. J., Dacquet, C., Michel, A. N., Jacoby, E., Vickery, B. and Tallentire, D. (1998) Interaction of the anxiogenic agent, RS-30199, with 5-HT1A receptors: modulation of sexual activity in the male rat. Neuropharmacology, 37: 769-780. [PMID:9707291]

81. Stam, N. J., Van Huizen, F., Van Alebeek, C., Brands, J., Dijkema, R., Tonnaer, J. A. and Olijve, W. (1992) Genomic organization, coding sequence and functional expression of human 5-HT2 and 5-HT1A receptor genes. Eur J Pharmacol, 227: 153-162. [PMID:1330647]

82. Wainscott, D. B., Krushinski, J. H., Audia, J. E., Schaus, J. M., Zgombick, J. M., Lucaites, V. L. and Nelson, D. L. (2005) [3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties. Naunyn Schmiedebergs Arch Pharmacol, 371: 169-177. [PMID:15900510]

83. Ward, S. E., Harrington, F. P., Gordon, L. J., Hopley, S. C., Scott, C. M. and Watson, J. M. (2005) Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem, 48: 3478-3480. [PMID:15887956]

84. Watson, J., Brough, S., Coldwell, M. C., Gager, T., Ho, M., Hunter, A. J., Jerman, J., Middlemiss, D. N., Riley, G. J. and Brown, A. M. (1998) Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors. Br J Pharmacol, 125: 1413-1420. [PMID:9884068]

85. Watson, J., Roberts, C., Scott, C., Kendall, I., Collin, L., Day, N. C., Harries, M. H., Soffin, E., Davies, C. H., Randall, A. D., Heightman, T., Gaster, L., Wyman, P., Parker, C., Price, G. W. and Middlemiss, D. N. (2001) SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue. Br J Pharmacol, 133: 797-806. [PMID:11454652]

To cite this database page, please use the following:

Rodrigo Andrade, Nicholas M. Barnes, Gordon Baxter, Joel Bockaert, Theresa Branchek, Marlene L. Cohen, Aline Dumuis, Richard M. Eglen, Manfred Göthert, Mark Hamblin, Michel Hamon, Paul R. Hartig, René Hen, Katharine Herrick-Davis, Rebecca Hills, Daniel Hoyer, Patrick P. A. Humphrey, Klaus Peter Latté, Luc Maroteaux, Graeme R. Martin, Derek N. Middlemiss, Ewan Mylecharane, Stephen J. Peroutka, Pramod R. Saxena, Andrew Sleight, Carlos M. Villalon, Frank Yocca.
5-Hydroxytryptamine receptors: 5-HT1A receptor. Last modified on 12/02/2013. Accessed on 23/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=1.


Contact us | Print | Back to top | Help