Nomenclature: 5-HT2A receptor

Family: 5-Hydroxytryptamine receptors

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Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 471 13q14-q21 HTR2A 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled 68
Mouse 7 471 14 D2 Htr2a 5-hydroxytryptamine (serotonin) receptor 2A 16,75
Rat 7 471 15q11 Htr2a 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled 19
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 Ligands
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 4
pKd 9.1 [4]
[3H](+)DOB Hs Full agonist 9.1 pKd 37,67
pKd 9.1 [37,67]
5-HT Hs Full agonist 8.9 pKd 67
pKd 8.9 [67]
asenapine Hs Full agonist 9.6 pKi 63
pKi 9.6 [63]
LSD Hs Full agonist 9.4 pKi 1
pKi 9.4 [1]
methylergonovine Hs Full agonist 9.4 pKi 31
pKi 9.4 [31]
(R)-DOI Hs Full agonist 9.2 – 9.3 pKi 31,40,52
pKi 9.2 – 9.3 [31,52]
pKi 9.2 [40]
(+)-LSD Hs Full agonist 9.1 pKi 31
pKi 9.1 [31]
DOB Hs Full agonist 8.9 – 9.2 pKi 31,48
pKi 8.9 – 9.2 [31,48]
(+)-DOI Hs Full agonist 9.0 pKi 31
pKi 9.0 [31]
S 16924 Hs Full agonist 9.0 pKi 43
pKi 9.0 [43]
ergotamine Hs Partial agonist 9.0 pKi 31
pKi 9.0 [31]
5-MeOT Hs Full agonist 8.9 pKi 27
pKi 8.9 [27]
AL-37350A Hs Full agonist 8.7 pKi 40
pKi 8.7 [40]
lisuride Hs Partial agonist 8.6 pKi 45
pKi 8.6 [45]
ergometrine Rn Full agonist 8.5 pKi 27
pKi 8.5 [27]
LSD Rn Full agonist 8.5 pKi 49
pKi 8.5 [49]
DOI Hs Full agonist 7.4 – 9.2 pKi 6,48,67
pKi 7.4 – 9.2 [6,48,67]
terguride Hs Partial agonist 8.3 pKi 45
pKi 8.3 [45]
cabergoline Hs Full agonist 8.2 pKi 45
pKi 8.2 [45]
5-MeOT Rn Full agonist 8.1 pKi 27
pKi 8.1 [27]
pergolide Hs Full agonist 8.1 pKi 45
pKi 8.1 [45]
ergotamine Rn Partial agonist 8.0 pKi 62
pKi 8.0 [62]
methylergonovine Rn Full agonist 7.9 pKi 62
pKi 7.9 [62]
GR-127935 Hs Full agonist 7.8 pKi 21,58
pKi 7.8 [21,58]
aripiprazole Hs Full agonist 7.5 – 8.1 pKi 34,66
pKi 7.5 – 8.1 [34,66]
methysergide Rn Partial agonist 7.8 pKi 62
pKi 7.8 [62]
DOB Rn Full agonist 7.8 pKi 13
pKi 7.8 [13]
α-methyl-5-HT Hs Full agonist 7.8 pKi 31
pKi 7.8 [31]
aripiprazole Rn Full agonist 7.7 pKi 66
pKi 7.7 [66]
org 37684 Hs Full agonist 7.5 pKi 31
pKi 7.5 [31]
TFMPP Hs Full agonist 7.5 pKi 31
pKi 7.5 [31]
org 12962 Hs Full agonist 7.5 pKi 31
pKi 7.5 [31]
Ro 60-0175 Hs Full agonist 7.4 pKi 31
pKi 7.4 [31]
N-1-isopropyl-5-MeOT Rn Full agonist 7.4 pKi 27
pKi 7.4 [27]
SB 216641 Hs Full agonist 7.3 pKi 58
pKi 7.3 [58]
BW723C86 Hs Full agonist 7.2 pKi 31
pKi 7.2 [31]
5-HT Hs Full agonist 6.0 – 8.4 pKi 1,6,27,31,40,67
pKi 6.0 – 8.4 [1,6,27,31,40,67]
m-CPP Hs Partial agonist 6.8 – 7.5 pKi 31,48,67
pKi 6.8 – 7.5 [31,48,67]
tryptamine Rn Full agonist 7.1 pKi 27
pKi 7.1 [27]
DOI Rn Full agonist 7.1 pKi 65
pKi 7.1 [65]
N-1-isopropyltryptamine Rn Full agonist 7.1 pKi 27
pKi 7.1 [27]
quetiapine Hs Full agonist 7.0 pKi 63
pKi 7.0 [63]
bromocriptine Hs Partial agonist 7.0 pKi 45
pKi 7.0 [45]
RU 24969 Hs Full agonist 6.9 pKi 31
pKi 6.9 [31]
quipazine Hs Full agonist 6.9 pKi 31
pKi 6.9 [31]
lorcaserin Hs Full agonist 6.8 pKi 70
pKi 6.8 [70]
DOM Rn Full agonist 6.8 pKi 13
pKi 6.8 [13]
donitriptan Hs Full agonist 6.7 pKi 26
pKi 6.7 [26]
BRL-15572 Hs Full agonist 6.6 pKi 58
pKi 6.6 [58]
N-1-isopropyltryptamine Hs Full agonist 6.6 pKi 27
pKi 6.6 [27]
tryptamine Hs Full agonist 5.5 – 7.6 pKi 6,27,31
pKi 5.5 – 7.6 [6,27,31]
5-CT Hs Full agonist 6.5 pKi 31
pKi 6.5 [31]
m-CPP Rn Partial agonist 6.4 pKi 62
pKi 6.4 [62]
VER-3323 Hs Full agonist 6.4 pKi 31
pKi 6.4 [31]
N-1-isopropyl-5-MeOT Hs Full agonist 6.3 pKi 27
pKi 6.3 [27]
5-HT Rn Full agonist 6.0 – 6.5 pKi 13,62,65
pKi 6.0 – 6.5 [13,62,65]
MK-212 Hs Full agonist 6.0 pKi 31
pKi 6.0 [31]
SL65.0155 Hs Partial agonist 5.9 pKi 47
pKi 5.9 [47]
α-methyl-5-HT Rn Full agonist 5.9 pKi 65
pKi 5.9 [65]
8-OH-DPAT Hs Full agonist 5.6 pKi 31
pKi 5.6 [31]
CGS-12066 Hs Full agonist 5.4 pKi 31
pKi 5.4 [31]
LY344864 Hs Full agonist 5.4 pKi 53
pKi 5.4 [53]
quinpirole Hs Full agonist 5.0 – 5.5 pKi 31,45
pKi 5.0 – 5.5 [31,45]
pindolol Hs Full agonist 5.0 pKi 31
pKi 5.0 [31]
lorcaserin Hs Full agonist 6.8 pEC50 70
pEC50 6.8 [70]
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 39
pKd 9.9 (Kd 1.3x10-10 M) [39]
[3H]ketanserin Hs Antagonist 8.6 – 9.7 pKd 31,60
pKd 8.6 – 9.7 (Kd 2x10-10 – 2.9x10-9 M) [31,60]
[3H]N-methylspiperone Rn Antagonist 9.1 pKd 65
pKd 9.1 [65]
[3H]ketanserin Rn Antagonist 8.8 pKd 65
pKd 8.8 [65]
AC-90179 Hs Inverse agonist 9.7 pKi 71
pKi 9.7 [71]
risperidone Hs Inverse agonist 9.3 – 10.0 pKi 32,34,63
pKi 9.3 – 10.0 [32,34,63]
sertindole Hs Antagonist 9.2 – 9.4 pKi 32,34,63
pKi 9.2 – 9.4 [32,34,63]
LY86057 Hs Antagonist 9.2 pKi 27
pKi 9.2 [27]
ritanserin Rn Antagonist 9.2 pKi 61,65
pKi 9.2 [61,65]
ziprasidone Hs Antagonist 8.8 – 9.5 pKi 32,34,63
pKi 8.8 – 9.5 [32,34,63]
spiperone Rn Antagonist 9.0 – 9.2 pKi 13,65
pKi 9.0 – 9.2 [13,65]
amoxapine Rn Antagonist 9.0 pKi 59
pKi 9.0 [59]
9-OH-risperidone Hs Antagonist 9.0 pKi 63
pKi 9.0 [63]
methysergide Rn Antagonist 8.4 – 9.5 pKi 13,33
pKi 8.4 – 9.5 [13,33]
ketanserin Hs Antagonist 8.1 – 9.7 pKi 8,31,60
pKi 8.1 – 9.7 [8,31,60]
clozapine Rn Inverse agonist 8.9 pKi 13
pKi 8.9 [13]
ritanserin Hs Antagonist 8.3 – 9.4 pKi 31,61
pKi 9.4 [61]
pKi 8.3 [31]
cyamemazine Hs Antagonist 8.8 pKi 24
pKi 8.8 [24]
ketanserin Rn Antagonist 8.6 – 9.0 pKi 13,65
pKi 8.6 – 9.0 [13,65]
mianserin Rn Antagonist 8.4 – 9.0 pKi 13,59
pKi 8.4 – 9.0 [13,59]
chlorpromazine Rn Inverse agonist 8.7 pKi 13
pKi 8.7 [13]
lurasidone Rn Antagonist 8.69 pKi 25
pKi 8.69 (Ki 2.03x10-9 M) [25]
mianserin Hs Antagonist 7.7 – 9.6 pKi 31,33,46
pKi 7.7 – 9.6 [31,33,46]
olanzapine Hs Antagonist 8.6 – 8.7 pKi 32,34,63
pKi 8.6 – 8.7 [32,34,63]
zotepine Hs Antagonist 8.6 pKi 63
pKi 8.6 [63]
spiperone Hs Antagonist 7.8 – 9.4 pKi 6,31,67
pKi 7.8 – 9.4 [6,31,67]
(+)-butaclamol Hs Antagonist 8.6 pKi 6
pKi 8.6 [6]
metergoline Hs Antagonist 8.6 pKi 31
pKi 8.6 [31]
mesulergine Rn Antagonist 8.6 pKi 27
pKi 8.6 [27]
risperidone Rn Antagonist 8.5 pKi 13
pKi 8.5 [13]
methiothepin Hs Antagonist 8.5 pKi 31
pKi 8.5 [31]
sarpogrelate Hs Antagonist 8.5 pKi 60
pKi 8.5 [60]
LY215840 Rn Antagonist 8.5 pKi 27
pKi 8.5 [27]
LY53857 Rn Antagonist 8.5 pKi 27
pKi 8.5 [27]
amesergide Rn Antagonist 8.5 pKi 27
pKi 8.5 [27]
LY108742 Rn Antagonist 8.4 pKi 27
pKi 8.4 [27]
sergolexole Rn Antagonist 8.4 pKi 27
pKi 8.4 [27]
amitriptyline Rn Antagonist 8.4 pKi 59
pKi 8.4 [59]
methysergide Hs Antagonist 8.4 pKi 31
pKi 8.4 [31]
pipamperone Hs Antagonist 8.3 pKi 63
pKi 8.3 [63]
clozapine Hs Inverse agonist 7.6 – 9.0 pKi 31,34,43,63,71
pKi 7.6 – 9.0 [31,34,43,63,71]
nefazodone Hs Antagonist 8.24 pKi 64
pKi 8.24 (Ki 5.8x10-9 M) [64]
perphenazine Hs Antagonist 8.2 pKi 34
pKi 8.2 [34]
roxindole Hs Antagonist 8.2 pKi 45
pKi 8.2 [45]
chlorpromazine Hs Inverse agonist 8.1 pKi 34
pKi 8.1 [34]
loxapine Hs Inverse agonist 8.1 pKi 34
pKi 8.1 [34]
fluspirilene Hs Antagonist 8.0 pKi 63
pKi 8.0 [63]
amesergide Hs Antagonist 8.0 pKi 27
pKi 8.0 [27]
trazodone Rn Antagonist 7.7 – 8.2 pKi 59,62
pKi 7.7 – 8.2 [59,62]
trifluoperazine Hs Antagonist 7.9 pKi 34
pKi 7.9 [34]
LY215840 Hs Antagonist 7.9 pKi 27
pKi 7.9 [27]
LY86057 Rn Antagonist 7.8 pKi 27
pKi 7.8 [27]
sergolexole Hs Antagonist 7.7 pKi 27
pKi 7.7 [27]
thioridazine Hs Antagonist 7.4 – 8.0 pKi 32,34
pKi 7.4 – 8.0 [32,34]
spiramide Hs Antagonist 7.6 pKi 31
pKi 7.6 [31]
LY53857 Hs Antagonist 7.6 pKi 27
pKi 7.6 [27]
glemanserin Hs Antagonist 7.6 pKi 31
pKi 7.6 [31]
fluphenazine Hs Antagonist 7.5 pKi 34
pKi 7.5 [34]
trazodone Hs Antagonist 7.4 pKi 31
pKi 7.4 [31]
haloperidol Rn Antagonist 7.4 pKi 13
pKi 7.4 [13]
pimozide Hs Antagonist 7.1 – 7.7 pKi 32,34