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

5-HT2A receptor

Family: 5-Hydroxytryptamine receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 471 13q14-q21 HTR2A 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled 63
Mouse 7 471 14 D2 Htr2a 5-hydroxytryptamine (serotonin) receptor 2A 13,70
Rat 7 471 15q11 Htr2a 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled 16
Previous and Unofficial Names
'D' receptor
HTR2
5-HT2A
5-hydroxytryptamine (serotonin) receptor 2A
5Ht-2
5-HT-2
5-HT-2A
5-hydroxytryptamine receptor 2A
serotonin 5HT-2 receptor
serotonin 5HT-2 receptor gene
serotonin receptor 2A
5-HT2A receptor
Htr-2
Database Links
ChEMBL Target 107 (Hs), 10620 (Mm), 12687 (Rn)
DrugBank Target 502 (Hs)
Ensembl ENSG00000102468 (Hs), ENSMUSG00000034997 (Mm), ENSRNOG00000010063 (Rn)
Entrez Gene 3356 (Hs), 15558 (Mm), 29595 (Rn)
GeneCards HTR2A (Hs)
GenitoUrinary Development Molecular Anatomy Project Htr2a (Mm)
HomoloGene 68073 (Hs)
Human Protein Reference Database 01638 (Hs)
InterPro P28223 (Hs), P35363 (Mm), P14842 (Rn)
KEGG Gene hsa:3356 (Hs), mmu:15558 (Mm), rno:29595 (Rn)
OMIM 182135 (Hs)
PharmGKB Gene PA193 (Hs)
PhosphoSitePlus P28223 (Hs), P35363 (Mm), P14842 (Rn)
Protein Ontology (PRO) PRO:000001166 (Hs)
RefSeq Nucleotide NM_000621 (Hs), NM_172812 (Mm), NM_017254 (Rn)
RefSeq Protein NP_000612 (Hs), NP_766400 (Mm), NP_058950 (Rn)
TreeFam ENSG00000102468 (Hs), ENSMUSG00000034997 (Mm), ENSRNOG00000010063 (Rn)
UniGene Hs. 424980 (Hs)
UniProt P28223 (Hs), P35363 (Mm), P14842 (Rn)
Wikipedia 5-HT2A receptor
5-Hydroxytryptamine receptors
Search for 3D structures on the PDB
Search by keyword: 5-Hydroxytryptamine receptors 5-HT2A receptor Search by accession number: P14842, P28223, P35363
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
[125I]DOI Rn Full agonist 9.1 pKd 3
[3H](+)DOB Hs Full agonist 9.1 pKd 33,62
5-HT Hs Full agonist 8.9 pKd 62
asenapine Hs Full agonist 9.6 pKi 59
LSD Hs Full agonist 9.4 pKi 1
methylergonovine Hs Full agonist 9.4 pKi 27
(R)-DOI Hs Full agonist 9.2 – 9.3 pKi 27,48
(R)-DOI Hs Full agonist 9.2 pKi 36
(+)-LSD Hs Full agonist 9.1 pKi 27
DOB Hs Full agonist 8.9 – 9.2 pKi 27,44
(+)-DOI Hs Full agonist 9.0 pKi 27
ergotamine Hs Partial agonist 9.0 pKi 27
S 16924 Hs Full agonist 9.0 pKi 39
5-MeOT Hs Full agonist 8.9 pKi 23
AL-37350A Hs Full agonist 8.7 pKi 36
lisuride Hs Partial agonist 8.6 pKi 41
ergonovine Rn Full agonist 8.5 pKi 23
LSD Rn Full agonist 8.5 pKi 45
DOI Hs Full agonist 7.4 – 9.2 pKi 5,44,62
terguride Hs Partial agonist 8.3 pKi 41
cabergoline Hs Full agonist 8.2 pKi 41
5-MeOT Rn Full agonist 8.1 pKi 23
pergolide Hs Full agonist 8.1 pKi 41
ergotamine Rn Partial agonist 8.0 pKi 58
methylergonovine Rn Full agonist 7.9 pKi 58
α-methyl-5-HT Hs Full agonist 7.8 pKi 27
aripiprazole Hs Full agonist 7.5 – 8.1 pKi 30,61
DOB Rn Full agonist 7.8 pKi 11
GR-127935 Hs Full agonist 7.8 pKi 18,54
methysergide Rn Partial agonist 7.8 pKi 58
aripiprazole Rn Full agonist 7.7 pKi 61
org 12962 Hs Full agonist 7.5 pKi 27
org 37684 Hs Full agonist 7.5 pKi 27
TFMPP Hs Full agonist 7.5 pKi 27
N-1-isopropyl-5-MeOT Rn Full agonist 7.4 pKi 23
Ro 60-0175 Hs Full agonist 7.4 pKi 27
SB 216641 Hs Full agonist 7.3 pKi 54
5-HT Hs Full agonist 6.0 – 8.4 pKi 1,5,23,27,36,62
BW723C86 Hs Full agonist 7.2 pKi 27
m-CPP Hs Partial agonist 6.8 – 7.5 pKi 27,44,62
DOI Rn Full agonist 7.1 pKi 60
N-1-isopropyltryptamine Rn Full agonist 7.1 pKi 23
tryptamine Rn Full agonist 7.1 pKi 23
bromocriptine Hs Partial agonist 7.0 pKi 41
quetiapine Hs Full agonist 7.0 pKi 59
quipazine Hs Full agonist 6.9 pKi 27
RU 24969 Hs Full agonist 6.9 pKi 27
DOM Rn Full agonist 6.8 pKi 11
lorcaserin Hs Full agonist 6.8 pKi 65
donitriptan Hs Full agonist 6.7 pKi 22
BRL-15572 Hs Full agonist 6.6 pKi 54
N-1-isopropyltryptamine Hs Full agonist 6.6 pKi 23
tryptamine Hs Full agonist 5.5 – 7.6 pKi 5,23,27
5-CT Hs Full agonist 6.5 pKi 27
m-CPP Rn Partial agonist 6.4 pKi 58
VER-3323 Hs Full agonist 6.4 pKi 27
N-1-isopropyl-5-MeOT Hs Full agonist 6.3 pKi 23
5-HT Rn Full agonist 6.0 – 6.5 pKi 11,58,60
MK-212 Hs Full agonist 6.0 pKi 27
α-methyl-5-HT Rn Full agonist 5.9 pKi 60
SL65.0155 Hs Partial agonist 5.9 pKi 43
8-OH-DPAT Hs Full agonist 5.6 pKi 27
CGS-12066 Hs Full agonist 5.4 pKi 27
LY344864 Hs Full agonist 5.4 pKi 49
quinpirole Hs Full agonist 5.0 – 5.5 pKi 27,41
pindolol Hs Full agonist 5.0 pKi 27
lorcaserin Hs Full agonist 6.8 pEC50 65
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
[11C]MDL100907 Hs Antagonist - -
[18F]altanserin Hs Antagonist - -
[3H]RP62203 Rn Antagonist 9.9 pKd 35
[3H]ketanserin Hs Antagonist 8.6 – 9.7 pKd 27,56
[3H]N-methylspiperone Rn Antagonist 9.1 pKd 60
[3H]ketanserin Rn Antagonist 8.8 pKd 60
AC-90179 Hs Inverse agonist 9.7 pKi 66
risperidone Hs Inverse agonist 9.3 – 10.0 pKi 28,30,59
ritanserin Hs Antagonist 9.4 pKi 57
sertindole Hs Antagonist 9.2 – 9.4 pKi 28,30,59
LY86057 Hs Antagonist 9.2 pKi 23
ritanserin Rn Antagonist 9.2 pKi 57,60
ziprasidone Hs Antagonist 8.8 – 9.5 pKi 28,30,59
spiperone Rn Antagonist 9.0 – 9.2 pKi 11,60
9-OH-risperidone Hs Antagonist 9.0 pKi 59
amoxapine Rn Antagonist 9.0 pKi 55
methysergide Rn Antagonist 8.4 – 9.5 pKi 11,29
clozapine Rn Inverse agonist 8.9 pKi 11
ketanserin Hs Antagonist 8.1 – 9.7 pKi 7,27,56
cyamemazine Hs Antagonist 8.8 pKi 21
ketanserin Rn Antagonist 8.6 – 9.0 pKi 11,60
chlorpromazine Rn Inverse agonist 8.7 pKi 11
mianserin Rn Antagonist 8.4 – 9.0 pKi 11,55
mianserin Hs Antagonist 7.7 – 9.6 pKi 27,29,42
olanzapine Hs Antagonist 8.6 – 8.7 pKi 28,30,59
(+)-butaclamol Hs Antagonist 8.6 pKi 5
mesulergine Rn Antagonist 8.6 pKi 23
metergoline Hs Antagonist 8.6 pKi 27
spiperone Hs Antagonist 7.8 – 9.4 pKi 5,27,62
zotepine Hs Antagonist 8.6 pKi 59
amesergide Rn Antagonist 8.5 pKi 23
LY215840 Rn Antagonist 8.5 pKi 23
LY53857 Rn Antagonist 8.5 pKi 23
methiothepin Hs Antagonist 8.5 pKi 27
risperidone Rn Antagonist 8.5 pKi 11
sarpogrelate Hs Antagonist 8.5 pKi 56
amitriptyline Rn Antagonist 8.4 pKi 55
LY108742 Rn Antagonist 8.4 pKi 23
methysergide Hs Antagonist 8.4 pKi 27
sergolexole Rn Antagonist 8.4 pKi 23
clozapine Hs Inverse agonist 7.6 – 9.0 pKi 27,30,39,59,66
pipamperone Hs Antagonist 8.3 pKi 59
ritanserin Hs Antagonist 8.3 pKi 27
perphenazine Hs Antagonist 8.2 pKi 30
roxindole Hs Antagonist 8.2 pKi 41
chlorpromazine Hs Inverse agonist 8.1 pKi 30
loxapine Hs Inverse agonist 8.1 pKi 30
amesergide Hs Antagonist 8.0 pKi 23
fluspirilene Hs Antagonist 8.0 pKi 59
trazodone Rn Antagonist 7.7 – 8.2 pKi 55,58
LY215840 Hs Antagonist 7.9 pKi 23
trifluoperazine Hs Antagonist 7.9 pKi 30
LY86057 Rn Antagonist 7.8 pKi 23
sergolexole Hs Antagonist 7.7 pKi 23
thioridazine Hs Antagonist 7.4 – 8.0 pKi 28,30
AMI-193 Hs Antagonist 7.6 pKi 27
LY53857 Hs Antagonist 7.6 pKi 23
MDL-11,939 Hs Antagonist 7.6 pKi 27
fluphenazine Hs Antagonist 7.5 pKi 30
haloperidol Rn Antagonist 7.4 pKi 11
trazodone Hs Antagonist 7.4 pKi 27
pimozide Hs Antagonist 7.1 – 7.7 pKi 28,30
thiothixene Hs Antagonist 7.3 pKi 30
mesulergine Hs Antagonist 7.0 – 7.5 pKi 27,62
LY314228 Hs Antagonist 7.2 pKi 7
haloperidol Hs Antagonist 6.7 – 7.3 pKi 30,39,59,66
LY320954 Hs Antagonist 7.0 pKi 7
SB 228357 Hs Antagonist 6.9 – 7.0 pKi 6,57
apomorphine Hs Antagonist 6.9 pKi 41
LY063518 Hs Antagonist 6.9 pKi 7
xanomeline Hs Antagonist 6.9 pKi 67
bufotenine Hs Antagonist 6.8 pKi 1
RS-102221 Rn Antagonist 6.8 pKi 4
SB 215505 Hs Antagonist 6.8 pKi 57
SB 243213 Hs Antagonist 6.8 pKi 6
quetiapine Hs Antagonist 6.4 – 7.0 pKi 28,30
EGIS-7625 Rn Antagonist 6.5 pKi 29
fluoxetine Rn Antagonist 6.5 pKi 58
L-741,626 Hs Antagonist 6.5 pKi 40
molindone Hs Antagonist 6.5 pKi 30
SB 242084 Hs Antagonist 6.1 – 6.8 pKi 26-27
duloxetine Hs Antagonist 6.3 pKi 9
MPDT Rn Antagonist 6.3 pKi 19
SB 221284 Hs Antagonist 6.3 pKi 27
SDZ SER-082 Hs Antagonist 6.3 pKi 27
EGIS-7625 Hs Antagonist 6.2 pKi 29
norfluoxetine Rn Antagonist 6.2 pKi 58
RS-127445 Hs Antagonist 6.0 pKi 27
S33084 Hs Antagonist 6.0 pKi 40
RS-102221 Hs Antagonist 5.5 – 6.0 pKi 4,27
SB 206553 Hs Antagonist 5.6 – 5.8 pKi 25,27
agomelatine Hs Antagonist 5.4 pKi 38
SB 224289 Hs Antagonist 5.3 pKi 27
pindolol Hs Antagonist 5.0 pKi 27
MDL-100,907 Hs Antagonist 6.5 – 9.3 pIC50 27,33,57
View species-specific antagonist tables

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

Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  10,17
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  17
Tissue Distribution
CNS: parahippocampal gyrus and neocortical regions (superficial and middle laminae) > dentate gyrus, hippocampus (all fields), subiculum.
Species:  Human
Technique:  in situ hybridisation.
References:  8
Atrium, coronary artery > ventricle wall, epicardium.
Species:  Human
Technique:  RT-PCR.
References:  46
Spinal cord: dorsal horn.
Species:  Human
Technique:  Radioligand binding.
References:  31
Sciatic nerve and Schwann cells.
Species:  Rat
Technique:  Immunohistochemistry.
References:  15
CNS: frontal cortex, piriform cortex, ventro-caudal part of CA3, medial mammillary nucleus, pontine nuclei and motor cranial nerve nuclei in the brainstem, and the ventral horn of the spinal cord.
Species:  Rat
Technique:  in situ hybridisation.
References:  52
Renal artery.
Species:  Rat
Technique:  Western blotting and immunohistochemistry.
References:  68
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  64
Medulla oblongata and lamina IX of the spinal cord.
Species:  Rat
Technique:  in situ hybridisation.
References:  14
Lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  50
CNS: striatum (nucleus accumbens, olfactory tubercle, and caudate putamen)
Species:  Rat
Technique:  in situ hybridisation.
References:  37
CNS: olfactory bulb, neocortex, claustrum, piriform cortex, mamillary bodies, pontine nuclei, red nucleus and cranial motor nuclei.
Species:  Rat
Technique:  Immunohistochemistry.
References:  20
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 rat glomerular mesangial cells endogenously expressing the 5-HT2A receptor.
Species:  Rat
Tissue:  Glomerular mesangial cells.
Response measured:  Increase in IP3 levels.
References:  17
Measurement of cAMP levels in rat glomerular mesangial cells endogenously expressing the 5-HT2A receptor.
Species:  Rat
Tissue:  Glomerular mesangial cells.
Response measured:  Inhibition of cAMP accumulation.
References:  17
Measurement of IP levels (and cAMP levels) in AV12 cells transfected with the rat 5-HT2C receptor.
Species:  Rat
Tissue:  AV12 cells.
Response measured:  Increase in IP levels (no change to cAMP).
References:  34
Measurement of intracellular Ca2+ levels using a fluorometric imaging plate reader (FLIPR) in CHO-K1 cells transfected with the human 5-HT2A receptor.
Species:  Human
Tissue:  CHO-K1 cells.
Response measured:  Increase in intracellular [Ca2+].
References:  53
Physiological Functions
Potentiation of inflammatory pain in the periphery.
Species:  Rat
Tissue:  In vivo.
References:  47,51
Contraction.
Species:  Human
Tissue:  Coronary artery.
References:  46
Contraction.
Species:  Rat
Tissue:  Mesenteric artery.
References:  69
Contraction (via MAPK pathway).
Species:  Rat
Tissue:  Aorta.
References:  2
Enhancement of platelet activation induced by ADP and thrombin.
Species:  Human
Tissue:  Whole blood.
References:  32
Procoagulant and fibrinolyic activities.
Species:  Rat
Tissue:  Aortic endothelial cells.
References:  24
Physiological Consequences of Altering Gene Expression
5-HT2A receptor knockout mice exhibit a lack of contraction of colonic smooth muscle in response to 5-HT.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  12
Phenotypes, Alleles and Disease Models Mouse data from MGI

Click here to show/hide data

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Htr2atm1Grch Htr2atm1Grch/Htr2atm1Grch
129S6/SvEvTac-Htr2a		 MGI:109521  MP:0001362 abnormal anxiety-related response PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch Htr2atm1Grch/Htr2atm2Grch
129S6/SvEv-Htr2a Htr2a		 MGI:109521  MP:0001362 abnormal anxiety-related response PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch Htr2atm1Grch/Htr2atm2Grch
involves: 129S6/SvEvTac		 MGI:109521  MP:0001362 abnormal anxiety-related response PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch|Slc6a4+|Slc6a4tm1(cre)Grch Htr2atm1Grch/Htr2atm2Grch,Slc6a4tm1(cre)Grch/Slc6a4+
involves: 129S6/SvEvTac		 MGI:109521  MGI:96285  MP:0001362 abnormal anxiety-related response PMID: 16873667 
Htr2atm1Rhn Htr2atm1Rhn/Htr2atm1Rhn
involves: 129S1/Sv * C57BL/6		 MGI:109521  MP:0000479 abnormal enterocyte morphology PMID: 11960784 
Htr2atm1Rhn Htr2atm1Rhn/Htr2atm1Rhn
involves: 129S1/Sv * C57BL/6		 MGI:109521  MP:0004843 abnormal Paneth cell morphology PMID: 11960784 
Htr2atm1Rhn Htr2atm1Rhn/Htr2atm1Rhn
involves: 129S1/Sv * C57BL/6		 MGI:109521  MP:0000767 abnormal smooth muscle morphology PMID: 11960784 
Htr2atm1Grch Htr2atm1Grch/Htr2atm1Grch
129S6/SvEvTac-Htr2a		 MGI:109521  MP:0001364 decreased anxiety-related response PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch Htr2atm1Grch/Htr2atm2Grch
129S6/SvEv-Htr2a Htr2a		 MGI:109521  MP:0001364 decreased anxiety-related response PMID: 16873667 
Htr2atm1Grch Htr2atm1Grch/Htr2atm1Grch
129S6/SvEvTac-Htr2a		 MGI:109521  MP:0002574 increased vertical activity PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch Htr2atm1Grch/Htr2atm2Grch
129S6/SvEv-Htr2a Htr2a		 MGI:109521  MP:0002574 increased vertical activity PMID: 16873667 

REFERENCES

Show »

1. Almaula, N., Ebersole, B. J., Zhang, D., Weinstein, H. and Sealfon, S. C. (1996) Mapping the binding site pocket of the serotonin 5-Hydroxytryptamine2A receptor. Ser3.36(159) provides a second interaction site for the protonated amine of serotonin but not of lysergic acid diethylamide or bufotenin. J Biol Chem, 271: 14672-14675. [PMID:8663249]

2. Banes, A., Florian, J. A. and Watts, S. W. (1999) Mechanisms of 5-hydroxytryptamine(2A) receptor activation of the mitogen-activated protein kinase pathway in vascular smooth muscle. J Pharmacol Exp Ther, 291: 1179-1187. [PMID:10565840]

3. 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]

4. Bonhaus, D. W., Weinhardt, K. K., Taylor, M., DeSouza, A., McNeeley, P. M., Szczepanski, K., Fontana, D. J., Trinh, J., Rocha, C. L., Dawson, M. W., Flippin, L. A. and Eglen, R. M. (1977) RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. Neuropharmacology, 36: 621-9. [PMID:9225287]

5. Branchek, T., Adham, N., Macchi, M., Kao, H. T. and Hartig, P. R. (1990) [3H]-DOB(4-bromo-2,5-dimethoxyphenylisopropylamine) and [3H] ketanserin label two affinity states of the cloned human 5-hydroxytryptamine2 receptor. Mol Pharmacol, 38: 604-609. [PMID:2233697]

6. Bromidge, S. M., Dabbs, S., Davies, D. T., Davies, S., Duckworth, D. M., Forbes, I. T., Gaster, L. M., Ham, P., Jones, G. E., King, F. D., Mulholland, K. R., Saunders, D. V., Wyman, P. A., Blaney, F. E., Clarke, S. E., Blackburn, T. P., Holland, V., Kennett, G. A., Lightowler, S., Middlemiss, D. N., Trail, B., Riley, G. J. and Wood, M. D. (2000) Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J Med Chem, 43: 1123-1134. [PMID:10737744]

7. Bryant, H. U., Nelson, D. L., Button, D., Cole, H. W., Baez, M. B., Lucaites, V. L., Wainscott, D. B., Whitesitt, C., Reel, J., Simon, R. and Koppel, G. A. (1996) A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines. Life Sci, 59: 1259-1268. [PMID:8845011]

8. 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]

9. Bymaster, F. P., Dreshfield-Ahmad, L. J., Threlkeld, P. G., Shaw, J. L., Thompson, L., Nelson, D. L., Hemrick-Luecke, S. K. and Wong, D. T. (2001) Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology, 25: 871-880. [PMID:11750180]

10. Day, M., Olson, P. A., Platzer, J., Striessnig, J. and Surmeier, D. J. (2002) Stimulation of 5-HT(2) receptors in prefrontal pyramidal neurons inhibits Ca(v)1.2 L type Ca(2+) currents via a PLCbeta/IP3/calcineurin signaling cascade. J Neurophysiol, 87: 2490-2504. [PMID:11976386]

11. Egan, C. T., Herrick-Davis, K. and Teitler, M. (1998) Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs. J Pharmacol Exp Ther, 286: 85-90. [PMID:9655845]

12. Fiorica-Howells, E., Hen, R., Gingrich, J., Li, Z. and Gershon, M. D. (2002) 5-HT(2A) receptors: location and functional analysis in intestines of wild-type and 5-HT(2A) knockout mice. Am J Physiol Gastrointest Liver Physiol, 282: G877-G893. [PMID:11960784]

13. Foguet, M., Nguyen, H., Le, H. and Lubbert, H. (1992) Structure of the mouse 5-HT1C, 5-HT2 and stomach fundus serotonin receptor genes. Neuroreport, 3: 345-348. [PMID:1381232]

14. Fonseca, M. I., Ni, Y. G., Dunning, D. D. and Miledi, R. (2001) Distribution of serotonin 2A, 2C and 3 receptor mRNA in spinal cord and medulla oblongata. Brain Res Mol Brain Res, 89: 11-19. [PMID:11311971]

15. Gaietta, G. M., Yoder, E. J., Deerinck, T., Kinder, K., Hanono, A., Han, A., Wu, C. and Ellisman, M. H. (2003) 5-HT2a receptors in rat sciatic nerves and Schwann cell cultures. J Neurocytol, 32: 373-380. [PMID:14724380]

16. Garlow, S. J., Chin, A. C., Marinovich, A. M., Heller, M. R. and Ciaranello, R. D. (1994) Cloning and functional promoter mapping of the rat serotonin-2 receptor gene. Mol Cell Neurosci, 5: 291-300. [PMID:8087427]

17. Garnovskaya, M. N., Nebigil, C. G., Arthur, J. M., Spurney, R. F. and Raymond, J. R. (1995) 5-Hydroxytryptamine2A receptors expressed in rat renal mesangial cells inhibit cyclic AMP accumulation. Mol Pharmacol, 48: 230-237. [PMID:7651356]

18. Gaster, L. M., Blaney, F. E., Davies, S., Duckworth, D. M., Ham, P., Jenkins, S., Jennings, A. J., Joiner, G. F., King, F. D., Mulholland, K. R., Wyman, P. A., Hagan, J. J., Hatcher, J., Jones, B. J., Middlemiss, D. N., Price, G. W., Riley, G., Roberts, C., Routledge, C., Selkirk, J. and Slade, P. D. (1998) The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J Med Chem, 41: 1218-1235. [PMID:9548813]

19. 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]

20. Hamada, S., Senzaki, K., Hamaguchi-Hamada, K., Tabuchi, K., Yamamoto, H., Yamamoto, T., Yoshikawa, S., Okano, H. and Okado, N. (1998) Localization of 5-HT2A receptor in rat cerebral cortex and olfactory system revealed by immunohistochemistry using two antibodies raised in rabbit and chicken. Brain Res Mol Brain Res, 54: 199-211. [PMID:9555012]

21. 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]

22. 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]

23. Johnson, M. P., Loncharich, R. J., Baez, M. and Nelson, D. L. (1994) Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines. Mol Pharmacol, 45: 277-286. [PMID:8114677]

24. Kawano, H., Tsuji, H., Nishimura, H., Kimura, S., Yano, S., Ukimura, N., Kunieda, Y., Yoshizumi, M., Sugano, T., Nakagawa, K., Masuda, H., Sawada, S. and Nakagawa, M. (2001) Serotonin induces the expression of tissue factor and plasminogen activator inhibitor-1 in cultured rat aortic endothelial cells. Blood, 97: 1697-1702. [PMID:11238110]

25. Kennett, G. A., Wood, M. D., Bright, F., Cilia, J., Piper, D. C., Gager, T., Thomas, D., Baxter, G. S., Forbes, I. T., Ham, P. and Blackburn, T. P. (1996) In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties. Br J Pharmacol, 117: 427-434. [PMID:8821530]

26. Kennett, G. A., Wood, M. D., Bright, F., Trail, B., Riley, G., Holland, V., Avenell, K. Y., Stean, T., Upton, N., Bromidge, S., Forbes, I. T., Brown, A. M., Middlemiss, D. N. and Blackburn, T. P. (1997) SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology, 36: 609-620. [PMID:9225286]

27. Knight, A. R., Misra, A., Quirk, K., Benwell, K., Revell, D., Kennett, G. and Bickerdike, M. (2004) Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol, 370: 114-123. [PMID:15322733]

28. Kongsamut, S., Kang, J., Chen, X. L., Roehr, J. and Rampe, D. (2002) A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs. Eur J Pharmacol, 450: 37-41. [PMID:12176106]

29. Kovacs, A., Gacsalyi, I., Wellmann, J., Schmidt, E., Szucs, Z., Dubreuil, V., Nicolas, J. P., Boutin, J., Bozsing, D., Egyed, A., Tihanyi, K., Spedding, M. and Szenasi, G. (2003) Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther, 17: 427-434. [PMID:15107597]

30. Kroeze, W. K., Hufeisen, S. J., Popadak, B. A., Renock, S. M., Steinberg, S., Ernsberger, P., Jayathilake, K., Meltzer, H. Y. and Roth, B. L. (2003) H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology, 28: 519-526. [PMID:12629531]

31. 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]

32. Li, N., Wallen, N. H., Ladjevardi, M. and Hjemdahl, P. (1997) Effects of serotonin on platelet activation in whole blood. Blood Coagul Fibrinolysis, 8: 517-523. [PMID:9491270]

33. Lopez-Gimenez, J. F., Villazon, M., Brea, J., Loza, M. I., Palacios, J. M., Mengod, G. and Vilaro, M. T. (2001) Multiple conformations of native and recombinant human 5-hydroxytryptamine(2a) receptors are labeled by agonists and discriminated by antagonists. Mol Pharmacol, 60: 690-699. [PMID:11562430]

34. Lucaites, V. L., Nelson, D. L., Wainscott, D. B. and Baez, M. (1996) Receptor subtype and density determine the coupling repertoire of the 5-HT2 receptor subfamily. Life Sci, 59: 1081-1095. [PMID:8809227]

35. Malgouris, C; Flamand, F; Doble, A. (1993) Autoradiographic studies of RP 62203, a potent 5-HT2 receptor antagonist. Pharmacological characterization of [3H]RP 62203 binding in the rat brain. Eur. J. Pharmacol., 233 (1): 37-45. [PMID:8472747]

36. May, J. A., Chen, H. H., Rusinko, A., Lynch, V. M., Sharif, N. A. and McLaughlin, M. A. (2003) A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. J Med Chem, 46: 4188-4195. [PMID:12954071]

37. Mijnster, M. J., Raimundo, A. G., Koskuba, K., Klop, H., Docter, G. J., Groenewegen, H. J. and Voorn, P. (1997) Regional and cellular distribution of serotonin 5-hydroxytryptamine2a receptor mRNA in the nucleus accumbens, olfactory tubercle, and caudate putamen of the rat. J Comp Neurol, 389: 1-11. [PMID:9390756]

38. Millan, M. J., Gobert, A., Lejeune, F., Dekeyne, A., Newman-Tancredi, A., Pasteau, V., Rivet, J. M. and Cussac, D. (2003) The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways. J Pharmacol Exp Ther, 306: 954-964. [PMID:12750432]

39. 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]

40. 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]

41. 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]

42. 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]

43. 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]

44. Nelson, D. L., Lucaites, V. L., Wainscott, D. B. and Glennon, R. A. (1999) Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors. Naunyn Schmiedebergs Arch Pharmacol, 359: 1-6. [PMID:9933142]

45. 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]

46. 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]

47. Okamoto, K., Imbe, H., Morikawa, Y., Itoh, M., Sekimoto, M., Nemoto, K. and Senba, E. (2002) 5-HT2A receptor subtype in the peripheral branch of sensory fibers is involved in the potentiation of inflammatory pain in rats. Pain, 99: 133-143. [PMID:12237191]

48. Parker, M. A., Marona-Lewicka, D., Lucaites, V. L., Nelson, D. L. and Nichols, D. E. (1998) A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor. J Med Chem, 41: 5148-5149. [PMID:9857084]

49. 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]

50. 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]

51. Pierce, P. A., Xie, G. X., Peroutka, S. J., Green, P. G. and Levine, J. D. (1995) 5-Hydroxytryptamine-induced synovial plasma extravasation is mediated via 5-hydroxytryptamine2A receptors on sympathetic efferent terminals. J Pharmacol Exp Ther, 275: 502-508. [PMID:7562592]

52. Pompeiano, M., Palacios, J. M. and Mengod, G. (1994) Distribution of the serotonin 5-HT2 receptor family mRNAs: comparison between 5-HT2A and 5-HT2C receptors. Brain Res Mol Brain Res, 23: 163-178. [PMID:8028479]

53. Porter, R. H., Benwell, K. R., Lamb, H., Malcolm, C. S., Allen, N. H., Revell, D. F., Adams, D. R. and Sheardown, M. J. (1999) Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells. Br J Pharmacol, 128: 13-20. [PMID:10498829]

54. 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]

55. Pälvimäki, E. P., Roth, B. L., Majasuo, H., Laakso, A., Kuoppamäki, M., Syvälahti, E. and Hietala, J. (1996) Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor. Psychopharmacology (Berl), 126: 234-240. [PMID:8876023]

56. Rashid, M., Manivet, P., Nishio, H., Pratuangdejkul, J., Rajab, M., Ishiguro, M., Launay, J. M. and Nagatomo, T. (2003) Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci, 73: 193-207. [PMID:12738034]

57. Reavill, C., Kettle, A., Holland, V., Riley, G. and Blackburn, T. P. (1999) Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol, 126: 572-574. [PMID:10188965]

58. Rothman, R. B., Baumann, M. H., Savage, J. E., Rauser, L., McBride, A., Hufeisen, S. J. and Roth, B. L. (2000) Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation, 102: 2836-2841. [PMID:11104741]

59. 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]

60. Shapiro, D. A., Kristiansen, K., Kroeze, W. K. and Roth, B. L. (2000) Differential modes of agonist binding to 5-hydroxytryptamine(2A) serotonin receptors revealed by mutation and molecular modeling of conserved residues in transmembrane region 5. Mol Pharmacol, 58: 877-886. [PMID:11040033]

61. 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]

62. Sleight, A. J., Stam, N. J., Mutel, V. and Vanderheyden, P. M. (1996) Radiolabelling of the human 5-HT2A receptor with an agonist, a partial agonist and an antagonist: effects on apparent agonist affinities. Biochem Pharmacol, 51: 71-76. [PMID:8534270]

63. 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]

64. Stefulj, J., Jernej, B., Cicin-Sain, L., Rinner, I. and Schauenstein, K. (2000) mRNA expression of serotonin receptors in cells of the immune tissues of the rat. Brain Behav Immun, 14: 219-224. [PMID:10970681]

65. Thomsen, WJ; Grottick, AJ; Menzaghi, F; Reyes-Saldana, H; Espitia, S; Yuskin, D; Whelan, K; Martin, M; Morgan, M; Chen, W; et al.. (2008) Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. J. Pharmacol. Exp. Ther., 325 (2): 577-87. [PMID:18252809]

66. Vanover, K. E., Harvey, S. C., Son, T., Bradley, S. R., Kold, H., Makhay, M., Veinbergs, I., Spalding, T. A., Weiner, D. M., Andersson, C. M., Tolf, B. R., Brann, M. R., Hacksell, U. and Davis, R. E. (2004) Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-aceta mide hydrochloride]: a selective serotonin 2A receptor inverse agonist. J Pharmacol Exp Ther, 310: 943-951. [PMID:15102927]

67. 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]

68. Watts, S. W. and Thompson, J. M. (2004) Characterization of the contractile 5-hydroxytryptamine receptor in the renal artery of the normotensive rat. J Pharmacol Exp Ther, 309: 165-172. [PMID:14724222]

69. Watts, S. W., Gilbert, L. and Webb, R. C. (1995) 5-Hydroxytryptamine2B receptor mediates contraction in the mesenteric artery of mineralocorticoid hypertensive rats. Hypertension, 26: 1056-1059. [PMID:7498967]

70. Yang, W., Chen, K., Lan, N. C., Gallaher, T. K. and Shih, J. C. (1992) Gene structure and expression of the mouse 5-HT2 receptor. J Neurosci Res, 33: 196-204. [PMID:1333538]

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-HT2A receptor. Last modified on 12/02/2013. Accessed on 26/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=6.


Contact us | Print | Back to top | Help