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5-HT2A

Previous and Unofficial Names
'D' receptor
Structural Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Name Reference
Human 7 471 13q14-q21 HTR2A 4
Rat 7 471 15q11 Htr2a 161
Mouse 7 471 14 D2 Htr2a 162-163
Contents:
Previous and Unofficial Names
Structural Information
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Database Links
ChEMBL Target 107 (Hs), 10620 (Mm), 12687 (Rn)
Ensembl ENSG00000102468 (Hs), ENSMUSG00000034997 (Mm), ENSRNOG00000010063 (Rn)
Entrez Gene 3356 (Hs), 15558 (Mm), 29595 (Rn)
GeneCards HTR2A (Hs)
HomoloGene 68073 (Hs)
OMIM 182135 (Hs)
PharmGKB Gene PA193 (Hs)
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)
UniGene Hs. 424980 (Hs)
UniProt P28223 (Hs), P35363 (Mm), P14842 (Rn)
Wikipedia 5-HT2A
Search for 3D structures on the PDB
Search using keywords: 5-Hydroxytryptamine receptors 5-HT2A Search using accession numbers: P14842 || P28223 || P35363
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 62
(+)-[3H]DOB Hs Full agonist 9.1 pKd 183-184
5-HT Hs Full agonist 8.9 pKd 184
ORG-5222 Hs Full agonist 9.6 pKi 65
LSD Hs Full agonist 9.4 pKi 189
methylergonovine Hs Full agonist 9.4 pKi 182
(R)-DOI Hs Full agonist 9.2 – 9.3 pKi 182,185
(R)-DOI Hs Full agonist 9.2 pKi 186
(+)-LSD Hs Full agonist 9.1 pKi 182
DOB Hs Full agonist 8.9 – 9.2 pKi 182,192
(+)-DOI Hs Full agonist 9.0 pKi 182
ergotamine Hs Partial agonist 9.0 pKi 182
S 16924 Hs Full agonist 9.0 pKi 66
5-MeOT Hs Full agonist 8.9 pKi 188
AL-37350A Hs Full agonist 8.7 pKi 186
lisuride Hs Partial agonist 8.6 pKi 69
ergonovine Rn Full agonist 8.5 pKi 188
LSD Rn Full agonist 8.5 pKi 61
DOI Hs Full agonist 7.4 – 9.2 pKi 184,187,192
terguride Hs Partial agonist 8.3 pKi 69
cabergoline Hs Full agonist 8.2 pKi 69
5-MeOT Rn Full agonist 8.1 pKi 188
pergolide Hs Full agonist 8.1 pKi 69
ergotamine Rn Partial agonist 8.0 pKi 190
methylergonovine Rn Full agonist 7.9 pKi 190
α-methyl-5-HT Hs Full agonist 7.8 pKi 182
aripiprazole Hs Full agonist 7.5 – 8.1 pKi 70,193
DOB Rn Full agonist 7.8 pKi 191
GR-127935 Hs Full agonist 7.8 pKi 58,132
methysergide Rn Partial agonist 7.8 pKi 190
aripiprazole Rn Full agonist 7.7 pKi 70
org 12962 Hs Full agonist 7.5 pKi 182
org 37684 Hs Full agonist 7.5 pKi 182
TFMPP Hs Full agonist 7.5 pKi 182
N-1-isopropyl-5-MeOT Rn Full agonist 7.4 pKi 188
Ro 60-0175 Hs Full agonist 7.4 pKi 182
SB 216641 Hs Full agonist 7.3 pKi 58
5-HT Hs Full agonist 6.0 – 8.4 pKi 182,184,186-189
BW723C86 Hs Full agonist 7.2 pKi 182
m-CPP Hs Partial agonist 6.8 – 7.5 pKi 182,184,192
DOI Rn Full agonist 7.1 pKi 181
N-1-isopropyltryptamine Rn Full agonist 7.1 pKi 188
tryptamine Rn Full agonist 7.1 pKi 188
bromocriptine Hs Partial agonist 7.0 pKi 69
quetiapine Hs Full agonist 7.0 pKi 65
quipazine Hs Full agonist 6.9 pKi 182
RU 24969 Hs Full agonist 6.9 pKi 182
DOM Rn Full agonist 6.8 pKi 191
donitriptan Hs Full agonist 6.7 pKi 71
BRL-15572 Hs Full agonist 6.6 pKi 58
N-1-isopropyltryptamine Hs Full agonist 6.6 pKi 188
tryptamine Hs Full agonist 5.5 – 7.6 pKi 182,187-188
5-CT Hs Full agonist 6.5 pKi 182
m-CPP Rn Partial agonist 6.4 pKi 190
VER-3323 Hs Full agonist 6.4 pKi 182
N-1-isopropyl-5-MeOT Hs Full agonist 6.3 pKi 188
5-HT Rn Full agonist 6.0 – 6.5 pKi 181,190-191
MK-212 Hs Full agonist 6.0 pKi 182
α-methyl-5-HT Rn Full agonist 5.9 pKi 181
SL65.0155 Hs Partial agonist 5.9 pKi 67
8-OH-DPAT Hs Full agonist 5.6 pKi 182
CGS-12066 Hs Full agonist 5.4 pKi 182
LY344864 Hs Full agonist 5.4 pKi 64
quinpirole Hs Full agonist 5.0 – 5.5 pKi 69,182
pindolol Hs Full agonist 5.0 pKi 182
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]ketanserin Hs Antagonist 8.9 – 9.7 pKd 184,189,202
[3H]-N-methylspiperone Rn Antagonist 9.1 pKd 181
[3H]ketanserin Rn Antagonist 8.8 pKd 181
AC-90179 Hs Inverse agonist 9.7 pKi 194
risperidone Hs Inverse agonist 9.3 – 10.0 pKi 65,193,206
ritanserin Hs Antagonist 9.4 pKi 197
sertindole Hs Antagonist 9.2 – 9.4 pKi 65,193,206
LY86057 Hs Antagonist 9.2 pKi 188
ritanserin Rn Antagonist 9.2 pKi 181,197
ziprasidone Hs Antagonist 8.8 – 9.5 pKi 65,193,206
spiperone Rn Antagonist 9.0 – 9.2 pKi 181,191
9-OH-risperidone Hs Antagonist 9.0 pKi 65
amoxapine Rn Antagonist 9.0 pKi 204
methysergide Rn Antagonist 8.4 – 9.5 pKi 191,195
clozapine Rn Inverse agonist 8.9 pKi 191
ketanserin Hs Antagonist 8.1 – 9.7 pKi 55,182,184,196,202
cyamemazine Hs Antagonist 8.8 pKi 55
ketanserin Rn Antagonist 8.6 – 9.0 pKi 181,191
chlorpromazine Rn Inverse agonist 8.7 pKi 191
mianserin Rn Antagonist 8.4 – 9.0 pKi 191,204
mianserin Hs Antagonist 7.7 – 9.6 pKi 54,182,195
olanzapine Hs Antagonist 8.6 – 8.7 pKi 65,193,206
(+)-butaclamol Hs Antagonist 8.6 pKi 187
mesulergine Rn Antagonist 8.6 pKi 188
metergoline Hs Antagonist 8.6 pKi 182
spiperone Hs Antagonist 7.8 – 9.4 pKi 182,184,187
zotepine Hs Antagonist 8.6 pKi 65
amesergide Rn Antagonist 8.5 pKi 188
LY215840 Rn Antagonist 8.5 pKi 188
LY53857 Rn Antagonist 8.5 pKi 188
methiothepin Hs Antagonist 8.5 pKi 182
risperidone Rn Antagonist 8.5 pKi 191
sarpogrelate Hs Antagonist 8.5 pKi 202
amitriptyline Rn Antagonist 8.4 pKi 204
LY108742 Rn Antagonist 8.4 pKi 188
methysergide Hs Antagonist 8.4 pKi 182
sergolexole Rn Antagonist 8.4 pKi 188
clozapine Hs Inverse agonist 7.6 – 9.0 pKi 65-66,182,193-194
pipamperone Hs Antagonist 8.3 pKi 65
ritanserin Hs Antagonist 8.3 pKi 182
perphenazine Hs Antagonist 8.2 pKi 193
roxindole Hs Antagonist 8.2 pKi 69
chlorpromazine Hs Inverse agonist 8.1 pKi 193
loxapine Hs Inverse agonist 8.1 pKi 193
amesergide Hs Antagonist 8.0 pKi 188
fluspirilene Hs Antagonist 8.0 pKi 65
trazodone Rn Antagonist 7.7 – 8.2 pKi 190,204
LY215840 Hs Antagonist 7.9 pKi 188
trifluoperazine Hs Antagonist 7.9 pKi 193
LY86057 Rn Antagonist 7.8 pKi 188
sergolexole Hs Antagonist 7.7 pKi 188
thioridazine Hs Antagonist 7.4 – 8.0 pKi 193,206
AMI-193 Hs Antagonist 7.6 pKi 182
LY53857 Hs Antagonist 7.6 pKi 188
MDL-11,939 Hs Antagonist 7.6 pKi 182
fluphenazine Hs Antagonist 7.5 pKi 193
haloperidol Rn Antagonist 7.4 pKi 191
trazodone Hs Antagonist 7.4 pKi 182
pimozide Hs Antagonist 7.1 – 7.7 pKi 193,206
thiothixene Hs Antagonist 7.3 pKi 193
mesulergine Hs Antagonist 7.0 – 7.5 pKi 182,184
LY314228 Hs Antagonist 7.2 pKi 196
haloperidol Hs Antagonist 6.7 – 7.3 pKi 65-66,193-194
LY320954 Hs Antagonist 7.0 pKi 196
SB 228357 Hs Antagonist 6.9 – 7.0 pKi 197,200
apomorphine Hs Antagonist 6.9 pKi 69
LY063518 Hs Antagonist 6.9 pKi 196
xanomeline Hs Antagonist 6.9 pKi 73
bufotenine Hs Antagonist 6.8 pKi 189
RS-102221 Rn Antagonist 6.8 pKi 198
SB 215505 Hs Antagonist 6.8 pKi 197
SB 243213 Hs Antagonist 6.8 pKi 200
quetiapine Hs Antagonist 6.4 – 7.0 pKi 193,206
EGIS-7625 Rn Antagonist 6.5 pKi 195
fluoxetine Rn Antagonist 6.5 pKi 190
L-741,626 Hs Antagonist 6.5 pKi 75
molindone Hs Antagonist 6.5 pKi 193
SB 242084 Hs Antagonist 6.1 – 6.8 pKi 182,201
duloxetine Hs Antagonist 6.3 pKi 205
MPDT Rn Antagonist 6.3 pKi 59
SB 221284 Hs Antagonist 6.3 pKi 182
SDZ SER-082 Hs Antagonist 6.3 pKi 182
EGIS-7625 Hs Antagonist 6.2 pKi 195
norfluoxetine Rn Antagonist 6.2 pKi 190
RS-127445 Hs Antagonist 6.0 pKi 182
S33084 Hs Antagonist 6.0 pKi 75
RS-102221 Hs Antagonist 5.5 – 6.0 pKi 182,198
SB 206553 Hs Antagonist 5.6 – 5.8 pKi 182,199
agomelatine Hs Antagonist 5.4 pKi 203
SB 224289 Hs Antagonist 5.3 pKi 182
pindolol Hs Antagonist 5.0 pKi 182
MDL-100,907 Hs Antagonist 6.5 – 9.3 pIC50 182-183,197
View species-specific antagonist tables

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

Primary Transduction Mechanisms
Transducer Effector/Response
Phospholipase C stimulation
References:  164-165
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  164
Tissue Distribution
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:  169
CNS: striatum (nucleus accumbens, olfactory tubercle, and caudate putamen)
Species:  Rat
Technique:  in situ hybridisation.
References:  170
CNS: olfactory bulb, neocortex, claustrum, piriform cortex, mamillary bodies, pontine nuclei, red nucleus and cranial motor nuclei.
Species:  Rat
Technique:  Immunohistochemistry.
References:  171
Atrium, coronary artery > ventricle wall, epicardium.
Species:  Human
Technique:  RT-PCR.
References:  29
Sciatic nerve and Schwann cells.
Species:  Rat
Technique:  Immunohistochemistry.
References:  172
Lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  33
Renal artery.
Species:  Rat
Technique:  Western blotting and immunohistochemistry.
References:  173
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  116
CNS: parahippocampal gyrus and neocortical regions (superficial and middle laminae) > dentate gyrus, hippocampus (all fields), subiculum.
Species:  Human
Technique:  in situ hybridisation.
References:  31
Medulla oblongata and lamina IX of the spinal cord.
Species:  Rat
Technique:  in situ hybridisation.
References:  174
Spinal cord: dorsal horn.
Species:  Human
Technique:  Radioligand binding.
References:  30
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:  164
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:  164
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:  167
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:  168
Physiological Functions
Contraction.
Species:  Human
Tissue:  Coronary artery.
References:  29
Contraction.
Species:  Rat
Tissue:  Mesenteric artery.
References:  175
Contraction (via MAPK pathway).
Species:  Rat
Tissue:  Aorta.
References:  176
Enhancement of platelet activation induced by ADP and thrombin.
Species:  Human
Tissue:  Whole blood.
References:  177
Procoagulant and fibrinolyic activities.
Species:  Rat
Tissue:  Aortic endothelial cells.
References:  178
Potentiation of inflammatory pain in the periphery.
Species:  Rat
Tissue:  In vivo.
References:  179-180
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:  166

To cite this receptor data 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. Last modified on 2010-06-28. Accessed on 2010-09-03. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=6.


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