5-HT<sub>2A</sub> receptor | 5-Hydroxytryptamine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

5-HT2A receptor

Target id: 6

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.  » Email us

   GtoImmuPdb view: OFF :     5-HT2A receptor has curated GtoImmuPdb data

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 receptor 2A 85
Mouse 7 471 14 D2 Htr2a 5-hydroxytryptamine (serotonin) receptor 2A 20,94
Rat 7 471 15q11 Htr2a 5-hydroxytryptamine receptor 2A 24
Previous and Unofficial Names
'D' receptor | 5Ht-2 | serotonin 5HT-2 receptor | serotonin receptor 2A | 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled
Database Links
Specialist databases
GPCRDB 5ht2a_human (Hs), 5ht2a_mouse (Mm), 5ht2a_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
5-hydroxytryptamine

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H](+)DOB Hs Full agonist 9.1 pKd 46,83
pKd 9.1 [46,83]
[125I]DOI Rn Full agonist 9.1 pKd 5
pKd 9.1 [5]
5-hydroxytryptamine Hs Full agonist 8.9 pKd 83
pKd 8.9 [83]
Lysergide Hs Full agonist 9.4 pKi 2
pKi 9.4 [2]
methylergonovine Hs Full agonist 9.4 pKi 38
pKi 9.4 [38]
(R)-DOI Hs Full agonist 9.2 – 9.3 pKi 38,49,63
pKi 9.2 – 9.3 [38,63]
pKi 9.2 [49]
(+)-LSD Hs Full agonist 9.1 pKi 38
pKi 9.1 [38]
brolamfetamine Hs Full agonist 8.9 – 9.2 pKi 38,57
pKi 8.9 – 9.2 [38,57]
ergotamine Hs Partial agonist 9.0 pKi 38
pKi 9.0 [38]
(+)-DOI Hs Full agonist 9.0 pKi 38
pKi 9.0 [38]
S 16924 Hs Full agonist 9.0 pKi 52
pKi 9.0 [52]
5-MeOT Hs Full agonist 8.9 pKi 34
pKi 8.9 [34]
AL-37350A Hs Full agonist 8.7 pKi 49
pKi 8.7 [49]
lisuride Hs Partial agonist 8.6 pKi 54
pKi 8.6 [54]
Lysergide Rn Full agonist 8.5 pKi 58
pKi 8.5 [58]
ergometrine Rn Full agonist 8.5 pKi 34
pKi 8.5 [34]
terguride Hs Partial agonist 8.3 pKi 54
pKi 8.3 [54]
DOI Hs Full agonist 7.4 – 9.2 pKi 9,57,83
pKi 7.4 – 9.2 (Ki 3.98x10-8 – 6.31x10-10 M) [9,57,83]
cabergoline Hs Full agonist 8.2 pKi 54
pKi 8.2 [54]
pergolide Hs Full agonist 8.1 pKi 54
pKi 8.1 [54]
5-MeOT Rn Full agonist 8.1 pKi 34
pKi 8.1 [34]
ergotamine Rn Partial agonist 8.0 pKi 74
pKi 8.0 [74]
methylergonovine Rn Full agonist 7.9 pKi 74
pKi 7.9 [74]
GR 127935 Hs Full agonist 7.8 pKi 26,69
pKi 7.8 [26,69]
aripiprazole Hs Partial agonist 7.5 – 8.1 pKi 41,82
pKi 7.5 – 8.1 [41,82]
methysergide Rn Partial agonist 7.8 pKi 74
pKi 7.8 [74]
α-methyl-5-HT Hs Full agonist 7.8 pKi 38
pKi 7.8 [38]
brolamfetamine Rn Full agonist 7.8 pKi 16
pKi 7.8 [16]
aripiprazole Rn Partial agonist 7.7 pKi 82
pKi 7.7 [82]
TFMPP Hs Full agonist 7.5 pKi 38
pKi 7.5 [38]
Org 12962 Hs Full agonist 7.5 pKi 38
pKi 7.5 [38]
ORG-37684 Hs Full agonist 7.5 pKi 38
pKi 7.5 [38]
N-1-isopropyl-5-MeOT Rn Full agonist 7.4 pKi 34
pKi 7.4 [34]
Ro 60-0175 Hs Full agonist 7.4 pKi 38
pKi 7.4 [38]
SB 216641 Hs Full agonist 7.3 pKi 69
pKi 7.3 [69]
5-hydroxytryptamine Hs Full agonist 6.0 – 8.4 pKi 2,9,34,38,49,83
pKi 6.0 – 8.4 [2,9,34,38,49,83]
BW723C86 Hs Full agonist 7.2 pKi 38
pKi 7.2 [38]
m-chlorophenylpiperazine Hs Partial agonist 6.8 – 7.5 pKi 38,57,83
pKi 6.8 – 7.5 [38,57,83]
tryptamine Rn Full agonist 7.1 pKi 34
pKi 7.1 [34]
DOI Rn Full agonist 7.1 pKi 81
pKi 7.1 [81]
N-1-isopropyltryptamine Rn Full agonist 7.1 pKi 34
pKi 7.1 [34]
bromocriptine Hs Partial agonist 7.0 pKi 54
pKi 7.0 [54]
quetiapine Hs Full agonist 7.0 pKi 76
pKi 7.0 [76]
RU 24969 Hs Full agonist 6.9 pKi 38
pKi 6.9 [38]
quipazine Hs Full agonist 6.9 pKi 38
pKi 6.9 [38]
DOM Rn Full agonist 6.8 pKi 16
pKi 6.8 [16]
lorcaserin Hs Full agonist 6.8 pKi 88
pKi 6.8 [88]
donitriptan Hs Full agonist 6.7 pKi 33
pKi 6.7 [33]
BRL-15572 Hs Full agonist 6.6 pKi 69
pKi 6.6 [69]
N-1-isopropyltryptamine Hs Full agonist 6.6 pKi 34
pKi 6.6 [34]
tryptamine Hs Full agonist 5.5 – 7.6 pKi 9,34,38
pKi 5.5 – 7.6 [9,34,38]
5-CT Hs Full agonist 6.5 pKi 38
pKi 6.5 [38]
LP-44 Hs Agonist 6.5 pKi 43
pKi 6.5 (Ki 3.26x10-7 M) [43]
m-chlorophenylpiperazine Rn Partial agonist 6.4 pKi 74
pKi 6.4 [74]
VER-3323 Hs Full agonist 6.4 pKi 38
pKi 6.4 [38]
N-1-isopropyl-5-MeOT Hs Full agonist 6.3 pKi 34
pKi 6.3 [34]
5-hydroxytryptamine Rn Full agonist 6.0 – 6.5 pKi 16,74,81
pKi 6.0 – 6.5 [16,74,81]
relenopride Hs Agonist 6.2 pKi 27
pKi 6.2 (Ki 6x10-7 M) [27]
MK-212 Hs Full agonist 6.0 pKi 38
pKi 6.0 [38]
capeserod Hs Partial agonist 5.9 pKi 56
pKi 5.9 [56]
α-methyl-5-HT Rn Full agonist 5.9 pKi 81
pKi 5.9 [81]
LP-12 Hs Agonist 5.8 pKi 43
pKi 5.8 (Ki 1.464x10-6 M) [43]
8-OH-DPAT Hs Full agonist 5.6 pKi 38
pKi 5.6 [38]
LY344864 Hs Full agonist 5.4 pKi 64
pKi 5.4 [64]
CGS-12066 Hs Full agonist 5.4 pKi 38
pKi 5.4 [38]
quinpirole Hs Full agonist 5.0 – 5.5 pKi 38,54
pKi 5.0 – 5.5 [38,54]
pindolol Hs Full agonist 5.0 pKi 38
pKi 5.0 [38]
lorcaserin Hs Full agonist 6.8 pEC50 88
pEC50 6.8 [88]
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]fananserin Rn Antagonist 9.9 pKd 48
pKd 9.9 (Kd 1.3x10-10 M) [48]
[3H]ketanserin Hs Antagonist 8.6 – 9.7 pKd 38,71
pKd 8.6 – 9.7 (Kd 2.9x10-9 – 2x10-10 M) [38,71]
[3H]N-methylspiperone Rn Antagonist 9.1 pKd 81
pKd 9.1 [81]
[3H]ketanserin Rn Antagonist 8.8 pKd 81
pKd 8.8 [81]
compound 3b [PMID:28943244] Hs Antagonist 10.6 pKi 19
pKi 10.6 (Ki 2.24x10-11 M) [19]
asenapine Hs Antagonist 10.2 pKi 79
pKi 10.2 (Ki 6x10-11 M) [79]
AC-90179 Hs Inverse agonist 9.7 pKi 89
pKi 9.7 [89]
risperidone Hs Inverse agonist 9.3 – 10.0 pKi 39,41,76
pKi 9.3 – 10.0 [39,41,76]
pimavanserin Hs Inverse agonist 9.3 pKi 23,89
pKi 9.3 [23,89]
Description: Ki determined in membrane radioligand binding assay.
lumateperone Hs Antagonist 9.3 pKi 45,84
pKi 9.3 (Ki 5x10-10 M) [45,84]
sertindole Hs Antagonist 9.2 – 9.4 pKi 39,41,76
pKi 9.2 – 9.4 [39,41,76]
ritanserin Rn Antagonist 9.2 pKi 72,81
pKi 9.2 [72,81]
LY86057 Hs Antagonist 9.2 pKi 34
pKi 9.2 [34]
ziprasidone Hs Antagonist 8.8 – 9.5 pKi 39,41,76,79
pKi 8.8 – 9.5 [39,41,76,79]
spiperone Rn Antagonist 9.0 – 9.2 pKi 16,81
pKi 9.0 – 9.2 [16,81]
[11C]GSK215083 Hs Antagonist 9.1 pKi 62
pKi 9.1 (Ki 7.9x10-10 M) [62]
blonanserin Hs Antagonist 9.1 pKi 60
pKi 9.1 (Ki 8.1x10-10 M) [60]
9-OH-risperidone Hs Antagonist 9.0 pKi 76
pKi 9.0 [76]
amoxapine Rn Antagonist 9.0 pKi 70
pKi 9.0 [70]
methysergide Rn Antagonist 8.4 – 9.5 pKi 16,40
pKi 8.4 – 9.5 [16,40]
clozapine Rn Inverse agonist 8.9 pKi 16
pKi 8.9 [16]
ketanserin Hs Antagonist 8.1 – 9.7 pKi 11,38,71
pKi 8.1 – 9.7 (Ki 7.94x10-9 – 1.99x10-10 M) [11,38,71]
ritanserin Hs Antagonist 8.3 – 9.4 pKi 38,72
pKi 9.4 [72]
pKi 8.3 [38]
cyamemazine Hs Antagonist 8.8 pKi 31
pKi 8.8 [31]
ketanserin Rn Antagonist 8.6 – 9.0 pKi 16,81
pKi 8.6 – 9.0 [16,81]
olanzapine Hs Antagonist 8.6 – 8.9 pKi 39,41,76,79
pKi 8.6 – 8.9 [39,41,76,79]
chlorpromazine Rn Inverse agonist 8.7 pKi 16
pKi 8.7 [16]
mianserin Rn Antagonist 8.4 – 9.0 pKi 16,70
pKi 8.4 – 9.0 [16,70]
lurasidone Rn Antagonist 8.7 pKi 32
pKi 8.7 (Ki 2.03x10-9 M) [32]
mianserin Hs Antagonist 7.7 – 9.6 pKi 38,40,55
pKi 7.7 – 9.6 [38,40,55]
(+)-butaclamol Hs Antagonist 8.6 pKi 9
pKi 8.6 [9]
spiperone Hs Antagonist 7.8 – 9.4 pKi 9,38,83
pKi 7.8 – 9.4 [9,38,83]
zotepine Hs Antagonist 8.6 pKi 76
pKi 8.6 [76]
metergoline Hs Antagonist 8.6 pKi 38
pKi 8.6 [38]
mesulergine Rn Antagonist 8.6 pKi 34
pKi 8.6 [34]
BF-1 Hs Antagonist 8.6 pKi 75
pKi 8.6 [75]
methiothepin Hs Antagonist 8.5 pKi 38
pKi 8.5 [38]
risperidone Rn Antagonist 8.5 pKi 16
pKi 8.5 [16]
LY215840 Rn Antagonist 8.5 pKi 34
pKi 8.5 [34]
LY53857 Rn Antagonist 8.5 pKi 34
pKi 8.5 [34]
amesergide Rn Antagonist 8.5 pKi 34
pKi 8.5 [34]
sarpogrelate Hs Antagonist 8.5 pKi 71
pKi 8.5 [71]
methysergide Hs Antagonist 8.4 pKi 38
pKi 8.4 [38]
LY108742 Rn Antagonist 8.4 pKi 34
pKi 8.4 [34]
sergolexole Rn Antagonist 8.4 pKi 34
pKi 8.4 [34]
clozapine Hs Inverse agonist 7.6 – 9.0 pKi 38,41,52,76,89
pKi 7.6 – 9.0 [38,41,52,76,89]
pipamperone Hs Antagonist 8.3 pKi 76
pKi 8.3 [76]
nefazodone Hs Antagonist 8.2 pKi 78
pKi 8.2 (Ki 5.8x10-9 M) [78]
roxindole Hs Antagonist 8.2 pKi 54
pKi 8.2 [54]
perphenazine Hs Antagonist 8.2 pKi 41
pKi 8.2 [41]
amitriptyline Rn Antagonist 8.0 – 8.4 pKi 70,87
pKi 8.4 [70]
pKi 8.0 (Ki 1.1x10-8 M) [87]
chlorpromazine Hs Inverse agonist 8.1 pKi 41
pKi 8.1 [41]
loxapine