Nomenclature: 5-HT2A receptor

Family: 5-Hydroxytryptamine receptors

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

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 471 13q14-q21 HTR2A 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled 64
Mouse 7 471 14 D2 Htr2a 5-hydroxytryptamine (serotonin) receptor 2A 14,71
Rat 7 471 15q11 Htr2a 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled 17
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
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligand(s)
5-HT
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]DOI Rn Full agonist 9.1 pKd 3
pKd 9.1 [3]
[3H](+)DOB Hs Full agonist 9.1 pKd 34,63
pKd 9.1 [34,63]
5-HT Hs Full agonist 8.9 pKd 63
pKd 8.9 [63]
asenapine Hs Full agonist 9.6 pKi 60
pKi 9.6 [60]
LSD Hs Full agonist 9.4 pKi 1
pKi 9.4 [1]
methylergonovine Hs Full agonist 9.4 pKi 28
pKi 9.4 [28]
(R)-DOI Hs Full agonist 9.2 – 9.3 pKi 28,37,49
pKi 9.2 – 9.3 [28,49]
pKi 9.2 [37]
(+)-LSD Hs Full agonist 9.1 pKi 28
pKi 9.1 [28]
DOB Hs Full agonist 8.9 – 9.2 pKi 28,45
pKi 8.9 – 9.2 [28,45]
(+)-DOI Hs Full agonist 9.0 pKi 28
pKi 9.0 [28]
S 16924 Hs Full agonist 9.0 pKi 40
pKi 9.0 [40]
ergotamine Hs Partial agonist 9.0 pKi 28
pKi 9.0 [28]
5-MeOT Hs Full agonist 8.9 pKi 24
pKi 8.9 [24]
AL-37350A Hs Full agonist 8.7 pKi 37
pKi 8.7 [37]
lisuride Hs Partial agonist 8.6 pKi 42
pKi 8.6 [42]
ergonovine Rn Full agonist 8.5 pKi 24
pKi 8.5 [24]
LSD Rn Full agonist 8.5 pKi 46
pKi 8.5 [46]
DOI Hs Full agonist 7.4 – 9.2 pKi 5,45,63
pKi 7.4 – 9.2 [5,45,63]
terguride Hs Partial agonist 8.3 pKi 42
pKi 8.3 [42]
cabergoline Hs Full agonist 8.2 pKi 42
pKi 8.2 [42]
5-MeOT Rn Full agonist 8.1 pKi 24
pKi 8.1 [24]
pergolide Hs Full agonist 8.1 pKi 42
pKi 8.1 [42]
ergotamine Rn Partial agonist 8.0 pKi 59
pKi 8.0 [59]
methylergonovine Rn Full agonist 7.9 pKi 59
pKi 7.9 [59]
GR-127935 Hs Full agonist 7.8 pKi 19,55
pKi 7.8 [19,55]
aripiprazole Hs Full agonist 7.5 – 8.1 pKi 31,62
pKi 7.5 – 8.1 [31,62]
methysergide Rn Partial agonist 7.8 pKi 59
pKi 7.8 [59]
DOB Rn Full agonist 7.8 pKi 11
pKi 7.8 [11]
α-methyl-5-HT Hs Full agonist 7.8 pKi 28
pKi 7.8 [28]
aripiprazole Rn Full agonist 7.7 pKi 62
pKi 7.7 [62]
org 37684 Hs Full agonist 7.5 pKi 28
pKi 7.5 [28]
TFMPP Hs Full agonist 7.5 pKi 28
pKi 7.5 [28]
org 12962 Hs Full agonist 7.5 pKi 28
pKi 7.5 [28]
Ro 60-0175 Hs Full agonist 7.4 pKi 28
pKi 7.4 [28]
N-1-isopropyl-5-MeOT Rn Full agonist 7.4 pKi 24
pKi 7.4 [24]
SB 216641 Hs Full agonist 7.3 pKi 55
pKi 7.3 [55]
BW723C86 Hs Full agonist 7.2 pKi 28
pKi 7.2 [28]
5-HT Hs Full agonist 6.0 – 8.4 pKi 1,5,24,28,37,63
pKi 6.0 – 8.4 [1,5,24,28,37,63]
m-CPP Hs Partial agonist 6.8 – 7.5 pKi 28,45,63
pKi 6.8 – 7.5 [28,45,63]
tryptamine Rn Full agonist 7.1 pKi 24
pKi 7.1 [24]
DOI Rn Full agonist 7.1 pKi 61
pKi 7.1 [61]
N-1-isopropyltryptamine Rn Full agonist 7.1 pKi 24
pKi 7.1 [24]
quetiapine Hs Full agonist 7.0 pKi 60
pKi 7.0 [60]
bromocriptine Hs Partial agonist 7.0 pKi 42
pKi 7.0 [42]
RU 24969 Hs Full agonist 6.9 pKi 28
pKi 6.9 [28]
quipazine Hs Full agonist 6.9 pKi 28
pKi 6.9 [28]
lorcaserin Hs Full agonist 6.8 pKi 66
pKi 6.8 [66]
DOM Rn Full agonist 6.8 pKi 11
pKi 6.8 [11]
donitriptan Hs Full agonist 6.7 pKi 23
pKi 6.7 [23]
BRL-15572 Hs Full agonist 6.6 pKi 55
pKi 6.6 [55]
N-1-isopropyltryptamine Hs Full agonist 6.6 pKi 24
pKi 6.6 [24]
tryptamine Hs Full agonist 5.5 – 7.6 pKi 5,24,28
pKi 5.5 – 7.6 [5,24,28]
5-CT Hs Full agonist 6.5 pKi 28
pKi 6.5 [28]
m-CPP Rn Partial agonist 6.4 pKi 59
pKi 6.4 [59]
VER-3323 Hs Full agonist 6.4 pKi 28
pKi 6.4 [28]
N-1-isopropyl-5-MeOT Hs Full agonist 6.3 pKi 24
pKi 6.3 [24]
5-HT Rn Full agonist 6.0 – 6.5 pKi 11,59,61
pKi 6.0 – 6.5 [11,59,61]
MK-212 Hs Full agonist 6.0 pKi 28
pKi 6.0 [28]
SL65.0155 Hs Partial agonist 5.9 pKi 44
pKi 5.9 [44]
α-methyl-5-HT Rn Full agonist 5.9 pKi 61
pKi 5.9 [61]
8-OH-DPAT Hs Full agonist 5.6 pKi 28
pKi 5.6 [28]
CGS-12066 Hs Full agonist 5.4 pKi 28
pKi 5.4 [28]
LY344864 Hs Full agonist 5.4 pKi 50
pKi 5.4 [50]
(-)-quinpirole Hs Full agonist 5.0 – 5.5 pKi 28,42
pKi 5.0 – 5.5 [28,42]
pindolol Hs Full agonist 5.0 pKi 28
pKi 5.0 [28]
lorcaserin Hs Full agonist 6.8 pEC50 66
pEC50 6.8 [66]
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]RP62203 Rn Antagonist 9.9 pKd 36
pKd 9.9 (Kd 1.3x10-10 M) [36]
[3H]ketanserin Hs Antagonist 8.6 – 9.7 pKd 28,57
pKd 8.6 – 9.7 (Kd 2x10-10 – 2.9x10-9 M) [28,57]
[3H]N-methylspiperone Rn Antagonist 9.1 pKd 61
pKd 9.1 [61]
[3H]ketanserin Rn Antagonist 8.8 pKd 61
pKd 8.8 [61]
AC-90179 Hs Inverse agonist 9.7 pKi 67
pKi 9.7 [67]
risperidone Hs Inverse agonist 9.3 – 10.0 pKi 29,31,60
pKi 9.3 – 10.0 [29,31,60]
sertindole Hs Antagonist 9.2 – 9.4 pKi 29,31,60
pKi 9.2 – 9.4 [29,31,60]
LY86057 Hs Antagonist 9.2 pKi 24
pKi 9.2 [24]
ritanserin Rn Antagonist 9.2 pKi 58,61
pKi 9.2 [58,61]
ziprasidone Hs Antagonist 8.8 – 9.5 pKi 29,31,60
pKi 8.8 – 9.5 [29,31,60]
spiperone Rn Antagonist 9.0 – 9.2 pKi 11,61
pKi 9.0 – 9.2 [11,61]
amoxapine Rn Antagonist 9.0 pKi 56
pKi 9.0 [56]
9-OH-risperidone Hs Antagonist 9.0 pKi 60
pKi 9.0 [60]
methysergide Rn Antagonist 8.4 – 9.5 pKi 11,30
pKi 8.4 – 9.5 [11,30]
ketanserin Hs Antagonist 8.1 – 9.7 pKi 7,28,57
pKi 8.1 – 9.7 [7,28,57]
clozapine Rn Inverse agonist 8.9 pKi 11
pKi 8.9 [11]
ritanserin Hs Antagonist 8.3 – 9.4 pKi 28,58
pKi 9.4 [58]
pKi 8.3 [28]
cyamemazine Hs Antagonist 8.8 pKi 22
pKi 8.8 [22]
ketanserin Rn Antagonist 8.6 – 9.0 pKi 11,61
pKi 8.6 – 9.0 [11,61]
mianserin Rn Antagonist 8.4 – 9.0 pKi 11,56
pKi 8.4 – 9.0 [11,56]
chlorpromazine Rn Inverse agonist 8.7 pKi 11
pKi 8.7 [11]
mianserin Hs Antagonist 7.7 – 9.6 pKi 28,30,43
pKi 7.7 – 9.6 [28,30,43]
olanzapine Hs Antagonist 8.6 – 8.7 pKi 29,31,60
pKi 8.6 – 8.7 [29,31,60]
zotepine Hs Antagonist 8.6 pKi 60
pKi 8.6 [60]
spiperone Hs Antagonist 7.8 – 9.4 pKi 5,28,63
pKi 7.8 – 9.4 [5,28,63]
(+)-butaclamol Hs Antagonist 8.6 pKi 5
pKi 8.6 [5]
metergoline Hs Antagonist 8.6 pKi 28
pKi 8.6 [28]
mesulergine Rn Antagonist 8.6 pKi 24
pKi 8.6 [24]
risperidone Rn Antagonist 8.5 pKi 11
pKi 8.5 [11]
methiothepin Hs Antagonist 8.5 pKi 28
pKi 8.5 [28]
sarpogrelate Hs Antagonist 8.5 pKi 57
pKi 8.5 [57]
LY215840 Rn Antagonist 8.5 pKi 24
pKi 8.5 [24]
LY53857 Rn Antagonist 8.5 pKi 24
pKi 8.5 [24]
amesergide Rn Antagonist 8.5 pKi 24
pKi 8.5 [24]
LY108742 Rn Antagonist 8.4 pKi 24
pKi 8.4 [24]
sergolexole Rn Antagonist 8.4 pKi 24
pKi 8.4 [24]
amitriptyline Rn Antagonist 8.4 pKi 56
pKi 8.4 [56]
methysergide Hs Antagonist 8.4 pKi 28
pKi 8.4 [28]
pipamperone Hs Antagonist 8.3 pKi 60
pKi 8.3 [60]
clozapine Hs Inverse agonist 7.6 – 9.0 pKi 28,31,40,60,67
pKi 7.6 – 9.0 [28,31,40,60,67]
perphenazine Hs Antagonist 8.2 pKi 31
pKi 8.2 [31]
roxindole Hs Antagonist 8.2 pKi 42
pKi 8.2 [42]
chlorpromazine Hs Inverse agonist 8.1 pKi 31
pKi 8.1 [31]
loxapine Hs Inverse agonist 8.1 pKi 31
pKi 8.1 [31]
fluspirilene Hs Antagonist 8.0 pKi 60
pKi 8.0 [60]
amesergide Hs Antagonist 8.0 pKi 24
pKi 8.0 [24]
trazodone Rn Antagonist 7.7 – 8.2 pKi 56,59
pKi 7.7 – 8.2 [56,59]
trifluoperazine Hs Antagonist 7.9 pKi 31
pKi 7.9 [31]
LY215840 Hs Antagonist 7.9 pKi 24
pKi 7.9 [24]
LY86057 Rn Antagonist 7.8 pKi 24
pKi 7.8 [24]
sergolexole Hs Antagonist 7.7 pKi 24
pKi 7.7 [24]
thioridazine Hs Antagonist 7.4 – 8.0 pKi 29,31
pKi 7.4 – 8.0 [29,31]
spiramide Hs Antagonist 7.6 pKi 28
pKi 7.6 [28]
LY53857 Hs Antagonist 7.6 pKi 24
pKi 7.6 [24]
MDL-11,939 Hs Antagonist 7.6 pKi 28
pKi 7.6 [28]
fluphenazine Hs Antagonist 7.5 pKi 31
pKi 7.5 [31]
trazodone Hs Antagonist 7.4 pKi 28
pKi 7.4 [28]
haloperidol Rn Antagonist 7.4 pKi 11
pKi 7.4 [11]
pimozide Hs Antagonist 7.1 – 7.7 pKi 29,31
pKi 7.1 – 7.7 [29,31]
thiothixene Hs Antagonist 7.3 pKi 31
pKi 7.3 [31]
mesulergine Hs Antagonist 7.0 – 7.5 pKi 28,63
pKi 7.0 – 7.5 [28,63]
LY314228 Hs Antagonist 7.2 pKi 7
pKi 7.2 [7]
mirtazapine Hs Antagonist 7.16 pKi 12
pKi 7.16 (Ki 6.9x10-8 M) [12]
LY320954 Hs Antagonist 7.0 pKi 7
pKi 7.0 [7]
haloperidol Hs Antagonist 6.7 – 7.3 pKi 31,40,60,67
pKi 6.7 – 7.3 [31,40,60,67]
SB 228357 Hs Antagonist 6.9 – 7.0 pKi 6,58
pKi 6.9 – 7.0 [6,58]
LY063518 Hs Antagonist 6.9 pKi 7
pKi 6.9 [7]
apomorphine