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5-HT2A receptor

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 6

Nomenclature: 5-HT2A receptor

Family: 5-Hydroxytryptamine receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 471 13q14.2 HTR2A 5-hydroxytryptamine receptor 2A 90
Mouse 7 471 14 39.37 cM Htr2a 5-hydroxytryptamine (serotonin) receptor 2A 20,100
Rat 7 471 15q11 Htr2a 5-hydroxytryptamine receptor 2A 26
Previous and Unofficial Names Click here for help
'D' receptor | 5Ht-2 | serotonin 5HT-2 receptor | serotonin receptor 2A | 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRdb 5ht2a_human (Hs), 5ht2a_mouse (Mm), 5ht2a_rat (Rn)
Other databases
Alphafold P28223 (Hs), P35363 (Mm), P14842 (Rn)
ChEMBL Target CHEMBL224 (Hs), CHEMBL5377 (Mm), CHEMBL322 (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)
Pharos P28223 (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 Click here for help
5-hydroxytryptamine
tryptamine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H](+)DOB Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 9.1 pKd 49,88
⤷ pKd 9.1 [49,88]
[125I]DOI Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Full agonist 9.1 pKd 4
⤷ pKd 9.1 [4]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 8.9 pKd 88
⤷ pKd 8.9 [88]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.4 pKi 2
⤷ pKi 9.4 [2]
methylergonovine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.4 pKi 41
⤷ pKi 9.4 [41]
(R)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.2 – 9.3 pKi 41,52,68
⤷ pKi 9.2 – 9.3 [41,68]
pKi 9.2 [52]
2C-B Small molecule or natural product Hs Agonist 9.2 pKi 53
⤷ pKi 9.2 (Ki 6.6x10-10 M) [53]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.1 pKi 41
⤷ pKi 9.1 [41]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.9 – 9.2 pKi 41,61
⤷ pKi 8.9 – 9.2 [41,61]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 9.0 pKi 41
⤷ pKi 9.0 [41]
(+)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 41
⤷ pKi 9.0 [41]
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 56
⤷ pKi 9.0 [56]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.9 pKi 36
⤷ pKi 8.9 [36]
AL-37350A Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.7 pKi 52
⤷ pKi 8.7 [52]
NBOMe Small molecule or natural product Rn Agonist 8.7 pKi 22
⤷ pKi 8.7 (Ki 2.2x10-9 M) [22]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.6 pKi 58
⤷ pKi 8.6 [58]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.5 pKi 62
⤷ pKi 8.5 [62]
ergometrine Small molecule or natural product Approved drug Rn Full agonist 8.5 pKi 36
⤷ pKi 8.5 [36]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.3 pKi 58
⤷ pKi 8.3 [58]
DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 – 9.2 pKi 8,61,88
⤷ pKi 7.4 – 9.2 (Ki 3.98x10-8 – 6.31x10-10 M) [8,61,88]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.2 pKi 58
⤷ pKi 8.2 [58]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.1 pKi 58
⤷ pKi 8.1 [58]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.1 pKi 36
⤷ pKi 8.1 [36]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 8.0 pKi 78
⤷ pKi 8.0 [78]
methylergonovine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.9 pKi 78
⤷ pKi 7.9 [78]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 28,74
⤷ pKi 7.8 [28,74]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.5 – 8.1 pKi 44,87
⤷ pKi 7.5 – 8.1 [44,87]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.8 pKi 78
⤷ pKi 7.8 [78]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 41
⤷ pKi 7.8 [41]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.8 pKi 16
⤷ pKi 7.8 [16]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.7 pKi 87
⤷ pKi 7.7 [87]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 41
⤷ pKi 7.5 [41]
Org 12962 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 41
⤷ pKi 7.5 [41]
ORG-37684 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 41
⤷ pKi 7.5 [41]
N-1-isopropyl-5-MeOT Small molecule or natural product Rn Full agonist 7.4 pKi 36
⤷ pKi 7.4 [36]
Ro 60-0175 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 41
⤷ pKi 7.4 [41]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 pKi 74
⤷ pKi 7.3 [74]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 6.0 – 8.4 pKi 2,8,36,41,52,88
⤷ pKi 6.0 – 8.4 [2,8,36,41,52,88]
BW723C86 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pKi 41
⤷ pKi 7.2 [41]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 – 7.5 pKi 41,61,88
⤷ pKi 6.8 – 7.5 [41,61,88]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 7.1 pKi 36
⤷ pKi 7.1 [36]
DOI Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.1 pKi 86
⤷ pKi 7.1 [86]
N-1-isopropyltryptamine Small molecule or natural product Rn Full agonist 7.1 pKi 36
⤷ pKi 7.1 [36]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.0 pKi 58
⤷ pKi 7.0 [58]
quetiapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.0 pKi 81
⤷ pKi 7.0 [81]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 41
⤷ pKi 6.9 [41]
quipazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 41
⤷ pKi 6.9 [41]
DOM Small molecule or natural product Rn Full agonist 6.8 pKi 16
⤷ pKi 6.8 [16]
lorcaserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.8 pKi 93
⤷ pKi 6.8 [93]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.7 pKi 35
⤷ pKi 6.7 [35]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Full agonist 6.6 pKi 74
⤷ pKi 6.6 [74]
N-1-isopropyltryptamine Small molecule or natural product Hs Full agonist 6.6 pKi 36
⤷ pKi 6.6 [36]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 5.5 – 7.6 pKi 8,36,41
⤷ pKi 5.5 – 7.6 [8,36,41]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.5 pKi 41
⤷ pKi 6.5 [41]
LP-44 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.5 pKi 46
⤷ pKi 6.5 (Ki 3.26x10-7 M) [46]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 6.4 pKi 78
⤷ pKi 6.4 [78]
VER-3323 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.4 pKi 41
⤷ pKi 6.4 [41]
N-1-isopropyl-5-MeOT Small molecule or natural product Hs Full agonist 6.3 pKi 36
⤷ pKi 6.3 [36]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 6.0 – 6.5 pKi 16,78,86
⤷ pKi 6.0 – 6.5 [16,78,86]
relenopride Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.2 pKi 29
⤷ pKi 6.2 (Ki 6x10-7 M) [29]
MK-212 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.0 pKi 41
⤷ pKi 6.0 [41]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.9 pKi 60
⤷ pKi 5.9 [60]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.9 pKi 86
⤷ pKi 5.9 [86]
LP-12 Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.8 pKi 46
⤷ pKi 5.8 (Ki 1.464x10-6 M) [46]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 pKi 41
⤷ pKi 5.6 [41]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 69
⤷ pKi 5.4 [69]
CGS-12066 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 41
⤷ pKi 5.4 [41]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.0 – 5.5 pKi 41,58
⤷ pKi 5.0 – 5.5 [41,58]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.0 pKi 41
⤷ pKi 5.0 [41]
psilocin Small molecule or natural product Ligand has a PDB structure Hs Agonist 7.6 pEC50 79
⤷ pEC50 7.6 (EC50 2.4x10-8 M) [79]
Description: Determined in an [3H]inositol phosphate accumulation assay in cells stably expressing h5-HT2A.
(R)-70 [PMID: 36171289] Small molecule or natural product Hs Partial agonist 7.0 pEC50 37
⤷ pEC50 7.0 (EC50 1.1x10-7 M) [37]
lorcaserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.8 pEC50 93
⤷ pEC50 6.8 [93]
mescaline Small molecule or natural product Hs Agonist 5.6 pEC50 13
⤷ pEC50 5.6 (EC50 2.6x10-6 M) [13]
Description: Potency determined in an IP3 accumulation assay
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]fananserin Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Antagonist 9.9 pKd 51
⤷ pKd 9.9 (Kd 1.3x10-10 M) [51]
[3H]ketanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Antagonist 8.6 – 9.7 pKd 41,75
⤷ pKd 8.6 – 9.7 (Kd 2.9x10-9 – 2x10-10 M) [41,75]
[3H]N-methylspiperone Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Antagonist 9.1 pKd 86
⤷ pKd 9.1 [86]
[3H]ketanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Rn Antagonist 8.8 pKd 86
⤷ pKd 8.8 [86]
compound 3b [PMID:28943244] Small molecule or natural product Primary target of this compound Hs Antagonist 10.6 pKi 19
⤷ pKi 10.6 (Ki 2.24x10-11 M) [19]
asenapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 10.2 pKi 84
⤷ pKi 10.2 (Ki 6x10-11 M) [84]
MT-1207 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 10.1 pKi 95
⤷ pKi 10.1 (Ki 7.9x10-11 M) [95]
AC-90179 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 9.7 pKi 94
⤷ pKi 9.7 [94]
risperidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 9.3 – 10.0 pKi 42,44,81
⤷ pKi 9.3 – 10.0 [42,44,81]
pimavanserin Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inverse agonist 9.3 pKi 25,94
⤷ pKi 9.3 [25,94]
Description: Ki determined in membrane radioligand binding assay.
lumateperone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 9.3 pKi 48,89
⤷ pKi 9.3 (Ki 5x10-10 M) [48,89]
sertindole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.2 – 9.4 pKi 42,44,81
⤷ pKi 9.2 – 9.4 [42,44,81]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.2 pKi 76,86
⤷ pKi 9.2 [76,86]
LY86057 Small molecule or natural product Hs Antagonist 9.2 pKi 36
⤷ pKi 9.2 [36]
ziprasidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.8 – 9.5 pKi 42,44,81,84
⤷ pKi 8.8 – 9.5 [42,44,81,84]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.0 – 9.2 pKi 16,86
⤷ pKi 9.0 – 9.2 [16,86]
[11C]GSK215083 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.1 pKi 67
⤷ pKi 9.1 (Ki 7.9x10-10 M) [67]
blonanserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.1 pKi 64
⤷ pKi 9.1 (Ki 8.1x10-10 M) [64]
9-OH-risperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 pKi 81
⤷ pKi 9.0 [81]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 9.0 pKi 66
⤷ pKi 9.0 [66]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.4 – 9.5 pKi 16,43
⤷ pKi 8.4 – 9.5 [16,43]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.9 pKi 16
⤷ pKi 8.9 [16]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.1 – 9.7 pKi 10,41,75
⤷ pKi 8.1 – 9.7 (Ki 7.94x10-9 – 1.99x10-10 M) [10,41,75]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.3 – 9.4 pKi 41,76
⤷ pKi 9.4 [76]
pKi 8.3 [41]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 33
⤷ pKi 8.8 [33]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.6 – 9.0 pKi 16,86
⤷ pKi 8.6 – 9.0 [16,86]
olanzapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.6 – 8.9 pKi 42,44,81,84
⤷ pKi 8.6 – 8.9 [42,44,81,84]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.7 pKi 16
⤷ pKi 8.7 [16]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.4 – 9.0 pKi 16,66
⤷ pKi 8.4 – 9.0 [16,66]
lurasidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.7 pKi 34
⤷ pKi 8.7 (Ki 2.03x10-9 M) [34]
mianserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.7 – 9.6 pKi 41,43,59
⤷ pKi 7.7 – 9.6 [41,43,59]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 8
⤷ pKi 8.6 [8]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.8 – 9.4 pKi 8,41,88
⤷ pKi 7.8 – 9.4 [8,41,88]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.6 pKi 81
⤷ pKi 8.6 [81]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 41
⤷ pKi 8.6 [41]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.6 pKi 36
⤷ pKi 8.6 [36]
BF-1 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 80
⤷ pKi 8.6 [80]
EGIS-11150 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 23
⤷ pKi 8.5 (Ki 3.1x10-9 M) [23]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 41
⤷ pKi 8.5 [41]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.5 pKi 16
⤷ pKi 8.5 [16]
LY215840 Small molecule or natural product Rn Antagonist 8.5 pKi 36
⤷ pKi 8.5 [36]
LY53857 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.5 pKi 36
⤷ pKi 8.5 [36]
amesergide Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.5 pKi 36
⤷ pKi 8.5 [36]
sarpogrelate Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.5 pKi 75
⤷ pKi 8.5 [75]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.4 pKi 41
⤷ pKi 8.4 [41]
LY108742 Small molecule or natural product Rn Antagonist 8.4 pKi 36
⤷ pKi 8.4 [36]
sergolexole Small molecule or natural product Rn Antagonist 8.4 pKi 36
⤷ pKi 8.4 [36]
clozapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 7.6 – 9.0 pKi 41,44,56,81,94
⤷ pKi 7.6 – 9.0 [41,44,56,81,94]
pipamperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 81
⤷ pKi 8.3 [81]
nefazodone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.2 pKi 83
⤷ pKi 8.2 (Ki 5.8x10-9 M) [83]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 pKi 58
⤷ pKi 8.2 [58]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.2 pKi 44
⤷ pKi 8.2 [44]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.0 – 8.4 pKi 66,92
⤷ pKi 8.4 [66]
pKi 8.0 (Ki 1.1x10-8 M) [92]
chlorpromazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.1 pKi 44
⤷ pKi 8.1 [44]
loxapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 8.1 pKi 44
⤷ pKi 8.1 [44]
fluspirilene Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.0 pKi 81
⤷ pKi 8.0 [81]
amesergide Small molecule or natural product Hs Antagonist 8.0 pKi 36
⤷ pKi 8.0 [36]
trazodone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.7 – 8.2 pKi 66,78
⤷ pKi 7.7 – 8.2 [66,78]
LY215840 Small molecule or natural product Hs Antagonist 7.9 pKi 36
⤷ pKi 7.9 [36]
trifluoperazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.9 pKi 44
⤷ pKi 7.9 [44]
LY86057 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.8 pKi 36
⤷ pKi 7.8 [36]
thioridazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.4 – 8.0 pKi 42,44
⤷ pKi 7.4 – 8.0 [42,44]
sergolexole Small molecule or natural product Hs Antagonist 7.7 pKi 36
⤷ pKi 7.7 [36]
spiramide Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.6 pKi 41
⤷ pKi 7.6 [41]
LY53857 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.6 pKi 36
⤷ pKi 7.6 [36]
glemanserin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.6 pKi 41
⤷ pKi 7.6 [41]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.5 pKi 44
⤷ pKi 7.5 [44]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.4 pKi 16
⤷ pKi 7.4 [16]
trazodone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.4 pKi 41
⤷ pKi 7.4 [41]
pimozide Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.1 – 7.7 pKi 42,44
⤷ pKi 7.1 – 7.7 [42,44]
flibanserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.3 pKi 7
⤷ pKi 7.3 (Ki 4.9x10-8 M) [7]
thiothixene Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.3 pKi 44
⤷ pKi 7.3 [44]
mesoridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 pKi 14
⤷ pKi 7.3 (Ki 5.5x10-8 M) [14]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.0 – 7.5 pKi 41,88
⤷ pKi 7.0 – 7.5 [41,88]
LY314228 Small molecule or natural product Hs Antagonist 7.2 pKi 10
⤷ pKi 7.2 [10]
mirtazapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.2 pKi 17
⤷ pKi 7.2 (Ki 6.9x10-8 M) [17]
haloperidol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.7 – 7.3 pKi 44,56,81,84,94
⤷ pKi 6.7 – 7.3 [44,56,81,84,94]
LY320954 Small molecule or natural product Hs Antagonist 7.0 pKi 10
⤷ pKi 7.0 [10]
SB 228357 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.9 – 7.0 pKi 9,76
⤷ pKi 6.9 – 7.0 [9,76]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.9 pKi 58
⤷ pKi 6.9 [58]
xanomeline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.9 pKi 96
⤷ pKi 6.9 [96]
LY063518 Small molecule or natural product Hs Antagonist 6.9 pKi 10
⤷ pKi 6.9 [10]
bufotenine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 2
⤷ pKi 6.8 [2]
RS-102221 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.8 pKi 6
⤷ pKi 6.8 [6]
SB 215505 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 76
⤷ pKi 6.8 [76]
SB 243213 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 9
⤷ pKi 6.8 [9]
quetiapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.4 – 7.0 pKi 42,44
⤷ pKi 6.4 – 7.0 [42,44]
EGIS-7625 Small molecule or natural product Rn Antagonist 6.5 pKi 43
⤷ pKi 6.5 [43]
L-741,626 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 57
⤷ pKi 6.5 [57]
fluoxetine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.5 pKi 78
⤷ pKi 6.5 [78]
molindone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.5 pKi 44
⤷ pKi 6.5 [44]
SB 242084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 – 6.8 pKi 40-41
⤷ pKi 6.1 – 6.8 [40-41]
MPDT Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.3 pKi 30
⤷ pKi 6.3 [30]
SB 221284 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 41
⤷ pKi 6.3 [41]
SDZ SER-082 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 41
⤷ pKi 6.3 [41]
duloxetine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.3 pKi 12
⤷ pKi 6.3 [12]
EGIS-7625 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 43
⤷ pKi 6.2 [43]
norfluoxetine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.2 pKi 78
⤷ pKi 6.2 [78]
S33084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 57
⤷ pKi 6.0 [57]
RS-127445 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 41
⤷ pKi 6.0 [41]
RS-102221 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.5 – 6.0 pKi 6,41
⤷ pKi 5.5 – 6.0 [6,41]
SB 206553 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 – 5.8 pKi 39,41
⤷ pKi 5.6 – 5.8 [39,41]
agomelatine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.4 pKi 55
⤷ pKi 5.4 [55]
SB 224289 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.3 pKi 41
⤷ pKi 5.3 [41]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.0 pKi 41
⤷ pKi 5.0 [41]
perospirone Small molecule or natural product Approved drug Rn Antagonist 4.7 pKi 82
⤷ pKi 4.7 (Ki 1.8x10-5 M) [82]
MT-1207 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.5 pIC50 95
⤷ pIC50 9.5 (IC50 2.9x10-10 M) [95]
volinanserin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 – 9.3 pIC50 41,49,76
⤷ pIC50 6.5 – 9.3 [41,49,76]
H05 Small molecule or natural product Hs Antagonist 7.2 pIC50 99
⤷ pIC50 7.2 (IC50 6.037x10-8 M) [99]
[18F]altanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist - - 77
⤷ [77]
[11C]volinanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist - - 31
⤷ [31]
View species-specific antagonist tables
Antagonist Comments
Mirtazapine is an antagonist of α2-adrenoceptors and serotonin 5-HT2A and 5-HT2C receptors. The approved drug mesoridazine, although consisting of 4 stereoisomers, appears to be selective for the 5-HT2A receptor [14], especially when examining the data for the two highest affinity isomers, compounds 2 and 5. Across the 3 serotonin receptors tested, compounds 2 and 5 have the same order of potency (2A>1A>2C). The data shown in the table above is for compound 2. Mesoridazine is also a selective antagonist of the dopamine D2 receptor. Mianserin has activity across several families of GPCRs, including the histamine H1 receptor, 5-HT receptors and α-adrenoceptors, but may have additional actions. The 5-HT2A, 2B and 2C receptors have been tagged as the primary targets of this drug in view of their high affinity. This does not preclude clinically relevant actions at other molecular targets. Although pimavanserin is an inverse agonist, it is listed in the antagonist table as it will behave as such in most experiments.
Immunopharmacology Comments
The chemoattractant properties of 5-HT on human eosinophils is mediated by 5-HT2A receptor [5].
Cell Type Associations
Immuno Cell Type:  T cells
Comment:  Involved in T cell proliferation.
References:  1
Immuno Cell Type:  B cells
Cell Ontology Term:   B cell (CL:0000236)
References:  85
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   eosinophil (CL:0000771)
Comment:  Involved in chemotaxis.
References:  1
Immuno Cell Type:  Dendritic cells
Cell Ontology Term:   dendritic cell (CL:0000451)
Comment:  Involved in chemokine production.
References:  1,85
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   macrophage (CL:0000235)
monocyte (CL:0000576)
Comment:  Involved in chemokine production.
References:  1,85
Immuno Process Associations
Immuno Process:  Barrier integrity
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  15,27
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
References:  27
Tissue Distribution Click here for help
Spinal cord: dorsal horn.
Species:  Human
Technique:  Radioligand binding.
References:  45
Atrium, coronary artery > ventricle wall, epicardium.
Species:  Human
Technique:  RT-PCR.
References:  63
CNS: parahippocampal gyrus and neocortical regions (superficial and middle laminae) > dentate gyrus, hippocampus (all fields), subiculum.
Species:  Human
Technique:  in situ hybridisation.
References:  11
CNS: striatum (nucleus accumbens, olfactory tubercle, and caudate putamen)
Species:  Rat
Technique:  in situ hybridisation.
References:  54
CNS: olfactory bulb, neocortex, claustrum, piriform cortex, mamillary bodies, pontine nuclei, red nucleus and cranial motor nuclei.
Species:  Rat
Technique:  Immunohistochemistry.
References:  32
Medulla oblongata and lamina IX of the spinal cord.
Species:  Rat
Technique:  in situ hybridisation.
References:  21
Sciatic nerve and Schwann cells.
Species:  Rat
Technique:  Immunohistochemistry.
References:  24
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  91
Lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  70
Renal artery.
Species:  Rat
Technique:  Western blotting and immunohistochemistry.
References:  98
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:  72
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
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:  27
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:  27
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:  50
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:  73
Physiological Functions Click here for help
Contraction.
Species:  Human
Tissue:  Coronary artery.
References:  63
Contraction.
Species:  Rat
Tissue:  Mesenteric artery.
References:  97
Contraction (via MAPK pathway).
Species:  Rat
Tissue:  Aorta.
References:  3
Enhancement of platelet activation induced by ADP and thrombin.
Species:  Human
Tissue:  Whole blood.
References:  47
Procoagulant and fibrinolyic activities.
Species:  Rat
Tissue:  Aortic endothelial cells.
References:  38
Potentiation of inflammatory pain in the periphery.
Species:  Rat
Tissue:  In vivo.
References:  65,71
Physiological Consequences of Altering Gene Expression Click here for help
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:  18
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Htr2atm1Grch Htr2atm1Grch/Htr2atm1Grch
129S6/SvEvTac-Htr2a		 MGI:109521  MP:0001362 abnormal anxiety-related response PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch Htr2atm1Grch/Htr2atm2Grch
129S6/SvEv-Htr2a Htr2a		 MGI:109521  MP:0001362 abnormal anxiety-related response PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch Htr2atm1Grch/Htr2atm2Grch
involves: 129S6/SvEvTac		 MGI:109521  MP:0001362 abnormal anxiety-related response PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch|Slc6a4+|Slc6a4tm1(cre)Grch Htr2atm1Grch/Htr2atm2Grch,Slc6a4tm1(cre)Grch/Slc6a4+
involves: 129S6/SvEvTac		 MGI:109521  MGI:96285  MP:0001362 abnormal anxiety-related response PMID: 16873667 
Htr2atm1Rhn Htr2atm1Rhn/Htr2atm1Rhn
involves: 129S1/Sv * C57BL/6		 MGI:109521  MP:0000479 abnormal enterocyte morphology PMID: 11960784 
Htr2atm1Rhn Htr2atm1Rhn/Htr2atm1Rhn
involves: 129S1/Sv * C57BL/6		 MGI:109521  MP:0004843 abnormal Paneth cell morphology PMID: 11960784 
Htr2atm1Rhn Htr2atm1Rhn/Htr2atm1Rhn
involves: 129S1/Sv * C57BL/6		 MGI:109521  MP:0000767 abnormal smooth muscle morphology PMID: 11960784 
Htr2atm1Grch Htr2atm1Grch/Htr2atm1Grch
129S6/SvEvTac-Htr2a		 MGI:109521  MP:0001364 decreased anxiety-related response PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch Htr2atm1Grch/Htr2atm2Grch
129S6/SvEv-Htr2a Htr2a		 MGI:109521  MP:0001364 decreased anxiety-related response PMID: 16873667 
Htr2atm1Grch Htr2atm1Grch/Htr2atm1Grch
129S6/SvEvTac-Htr2a		 MGI:109521  MP:0002574 increased vertical activity PMID: 16873667 
Htr2atm1Grch|Htr2atm2Grch Htr2atm1Grch/Htr2atm2Grch
129S6/SvEv-Htr2a Htr2a		 MGI:109521  MP:0002574 increased vertical activity PMID: 16873667 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Alcohol dependence
Disease Ontology: DOID:0050741
OMIM: 103780
Disease:  Major depressive disorder; MDD
Disease Ontology: DOID:1470
OMIM: 608516
Disease:  Obsessive-compulsive disorder; OCD
Disease Ontology: DOID:10933
OMIM: 164230
Disease:  Schizophrenia
Disease Ontology: DOID:5419
OMIM: 181500
Orphanet: ORPHA3140

References

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