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

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5-HT2A receptor

  Target has curated data in GtoImmuPdb

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

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 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 107 (Hs), 10620 (Mm), 12687 (Rn)
DrugBank Target P28223 (Hs)
Ensembl Gene ENSG00000102468 (Hs), ENSMUSG00000034997 (Mm), ENSRNOG00000010063 (Rn)
Entrez Gene 3356 (Hs), 15558 (Mm), 29595 (Rn)
Human Protein Atlas ENSG00000102468 (Hs)
KEGG Gene hsa:3356 (Hs), mmu:15558 (Mm), rno:29595 (Rn)
OMIM 182135 (Hs)
RefSeq Nucleotide NM_000621 (Hs), NM_172812 (Mm), NM_017254 (Rn)
RefSeq Protein NP_000612 (Hs), NP_766400 (Mm), NP_058950 (Rn)
UniProtKB P28223 (Hs), P35363 (Mm), P14842 (Rn)
Wikipedia HTR2A (Hs)
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 Parameter 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 Parameter 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