Top ▲

5-HT2A receptor

Click here for help

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
CNS: parahippocampal gyrus and neocortical regions (superficial and middle laminae) > dentate gyrus, hippocampus (all fields), subiculum.
Species:  Human
Technique:  in situ hybridisation.
References:  11
Atrium, coronary artery > ventricle wall, epicardium.
Species:  Human
Technique:  RT-PCR.
References:  63
Spinal cord: dorsal horn.
Species:  Human
Technique:  Radioligand binding.
References:  45
Sciatic nerve and Schwann cells.
Species:  Rat
Technique:  Immunohistochemistry.
References:  24
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
Renal artery.
Species:  Rat
Technique:  Western blotting and immunohistochemistry.
References:  98
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  91
Medulla oblongata and lamina IX of the spinal cord.
Species:  Rat
Technique:  in situ hybridisation.
References:  21
Lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  70
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
Expression Datasets Click here for help

Show »

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]

There should be a chart of expression data here, you may need to enable JavaScript!
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

Show »

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

Show »

1. Ahern GP. (2011) 5-HT and the immune system. Curr Opin Pharmacol, 11 (1): 29-33. [PMID:21393060]

2. Almaula N, Ebersole BJ, Zhang D, Weinstein H, Sealfon SC. (1996) Mapping the binding site pocket of the serotonin 5-Hydroxytryptamine2A receptor. Ser3.36(159) provides a second interaction site for the protonated amine of serotonin but not of lysergic acid diethylamide or bufotenin. J Biol Chem, 271 (25): 14672-5. [PMID:8663249]

3. Banes A, Florian JA, Watts SW. (1999) Mechanisms of 5-hydroxytryptamine(2A) receptor activation of the mitogen-activated protein kinase pathway in vascular smooth muscle. J Pharmacol Exp Ther, 291 (3): 1179-87. [PMID:10565840]

4. Blair JB, Kurrasch-Orbaugh D, Marona-Lewicka D, Cumbay MG, Watts VJ, Barker EL, Nichols DE. (2000) Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. J Med Chem, 43 (24): 4701-10. [PMID:11101361]

5. Boehme SA, Lio FM, Sikora L, Pandit TS, Lavrador K, Rao SP, Sriramarao P. (2004) Cutting edge: serotonin is a chemotactic factor for eosinophils and functions additively with eotaxin. J Immunol, 173 (6): 3599-603. [PMID:15356103]

6. Bonhaus DW, Weinhardt KK, Taylor M, DeSouza A, McNeeley PM, Szczepanski K, Fontana DJ, Trinh J, Rocha CL, Dawson MW et al.. (1997) RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. Neuropharmacology, 36 (4-5): 621-9. [PMID:9225287]

7. Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S. (2002) Pharmacology of flibanserin. CNS Drug Rev, 8 (2): 117-42. [PMID:12177684]

8. Branchek T, Adham N, Macchi M, Kao HT, Hartig PR. (1990) [3H]-DOB(4-bromo-2,5-dimethoxyphenylisopropylamine) and [3H] ketanserin label two affinity states of the cloned human 5-hydroxytryptamine2 receptor. Mol Pharmacol, 38 (5): 604-9. [PMID:2233697]

9. Bromidge SM, Dabbs S, Davies DT, Davies S, Duckworth DM, Forbes IT, Gaster LM, Ham P, Jones GE, King FD et al.. (2000) Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J Med Chem, 43 (6): 1123-34. [PMID:10737744]

10. Bryant HU, Nelson DL, Button D, Cole HW, Baez MB, Lucaites VL, Wainscott DB, Whitesitt C, Reel J, Simon R et al.. (1996) A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines. Life Sci, 59 (15): 1259-68. [PMID:8845011]

11. Burnet PW, Eastwood SL, Lacey K, Harrison PJ. (1995) The distribution of 5-HT1A and 5-HT2A receptor mRNA in human brain. Brain Res, 676 (1): 157-68. [PMID:7796165]

12. Bymaster FP, Dreshfield-Ahmad LJ, Threlkeld PG, Shaw JL, Thompson L, Nelson DL, Hemrick-Luecke SK, Wong DT. (2001) Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology, 25 (6): 871-80. [PMID:11750180]

13. Chambers JJ, Parrish JC, Jensen NH, Kurrasch-Orbaugh DM, Marona-Lewicka D, Nichols DE. (2003) Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands. J Med Chem, 46 (16): 3526-35. [PMID:12877591]

14. Choi S, Haggart D, Toll L, Cuny GD. (2004) Synthesis, receptor binding and functional studies of mesoridazine stereoisomers. Bioorg Med Chem Lett, 14 (17): 4379-82. [PMID:15357957]

15. Day M, Olson PA, Platzer J, Striessnig J, Surmeier DJ. (2002) Stimulation of 5-HT(2) receptors in prefrontal pyramidal neurons inhibits Ca(v)1.2 L type Ca(2+) currents via a PLCbeta/IP3/calcineurin signaling cascade. J Neurophysiol, 87 (5): 2490-504. [PMID:11976386]

16. Egan CT, Herrick-Davis K, Teitler M. (1998) Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs. J Pharmacol Exp Ther, 286 (1): 85-90. [PMID:9655845]

17. Fernández J, Alonso JM, Andrés JI, Cid JM, Díaz A, Iturrino L, Gil P, Megens A, Sipido VK, Trabanco AA. (2005) Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. J Med Chem, 48 (6): 1709-12. [PMID:15771415]

18. Fiorica-Howells E, Hen R, Gingrich J, Li Z, Gershon MD. (2002) 5-HT(2A) receptors: location and functional analysis in intestines of wild-type and 5-HT(2A) knockout mice. Am J Physiol Gastrointest Liver Physiol, 282 (5): G877-93. [PMID:11960784]

19. Fiorino F, Magli E, Kędzierska E, Ciano A, Corvino A, Severino B, Perissutti E, Frecentese F, Di Vaio P, Saccone I et al.. (2017) New 5-HT1A, 5HT2Aand 5HT2Creceptor ligands containing a picolinic nucleus: Synthesis, in vitro and in vivo pharmacological evaluation. Bioorg Med Chem, 25 (20): 5820-5837. [PMID:28943244]

20. Foguet M, Nguyen H, Le H, Lübbert H. (1992) Structure of the mouse 5-HT1C, 5-HT2 and stomach fundus serotonin receptor genes. Neuroreport, 3 (4): 345-8. [PMID:1381232]

21. Fonseca MI, Ni YG, Dunning DD, Miledi R. (2001) Distribution of serotonin 2A, 2C and 3 receptor mRNA in spinal cord and medulla oblongata. Brain Res Mol Brain Res, 89 (1-2): 11-9. [PMID:11311971]

22. Fu H, Rong J, Chen Z, Zhou J, Collier T, Liang SH. (2022) Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors. J Med Chem, 65 (16): 10755-10808. [PMID:35939391]

23. Gacsályi I, Nagy K, Pallagi K, Lévay G, Hársing Jr LG, Móricz K, Kertész S, Varga P, Haller J, Gigler G et al.. (2013) Egis-11150: a candidate antipsychotic compound with procognitive efficacy in rodents. Neuropharmacology, 64: 254-63. [PMID:22824189]

24. Gaietta GM, Yoder EJ, Deerinck T, Kinder K, Hanono A, Han A, Wu C, Ellisman MH. (2003) 5-HT2a receptors in rat sciatic nerves and Schwann cell cultures. J Neurocytol, 32 (4): 373-80. [PMID:14724380]

25. Gardell LR, Vanover KE, Pounds L, Johnson RW, Barido R, Anderson GT, Veinbergs I, Dyssegaard A, Brunmark P, Tabatabaei A et al.. (2007) ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental models. J Pharmacol Exp Ther, 322 (2): 862-70. [PMID:17519387]

26. Garlow SJ, Chin AC, Marinovich AM, Heller MR, Ciaranello RD. (1994) Cloning and functional promoter mapping of the rat serotonin-2 receptor gene. Mol Cell Neurosci, 5 (3): 291-300. [PMID:8087427]

27. Garnovskaya MN, Nebigil CG, Arthur JM, Spurney RF, Raymond JR. (1995) 5-Hydroxytryptamine2A receptors expressed in rat renal mesangial cells inhibit cyclic AMP accumulation. Mol Pharmacol, 48 (2): 230-7. [PMID:7651356]

28. Gaster LM, Blaney FE, Davies S, Duckworth DM, Ham P, Jenkins S, Jennings AJ, Joiner GF, King FD, Mulholland KR et al.. (1998) The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J Med Chem, 41 (8): 1218-35. [PMID:9548813]

29. Gilet M, Eutamene H, Han H, Kim HW, Bueno L. (2014) Influence of a new 5-HT4 receptor partial agonist, YKP10811, on visceral hypersensitivity in rats triggered by stress and inflammation. Neurogastroenterol Motil, 26 (12): 1761-70. [PMID:25316608]

30. Glennon RA, Lee M, Rangisetty JB, Dukat M, Roth BL, Savage JE, McBride A, Rauser L, Hufeisen S, Lee DK. (2000) 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem, 43 (5): 1011-8. [PMID:10715164]

31. Hall H, Farde L, Halldin C, Lundkvist C, Sedvall G. (2000) Autoradiographic localization of 5-HT(2A) receptors in the human brain using [(3)H]M100907 and [(11)C]M100907. Synapse, 38 (4): 421-31. [PMID:11044889]

32. Hamada S, Senzaki K, Hamaguchi-Hamada K, Tabuchi K, Yamamoto H, Yamamoto T, Yoshikawa S, Okano H, Okado N. (1998) Localization of 5-HT2A receptor in rat cerebral cortex and olfactory system revealed by immunohistochemistry using two antibodies raised in rabbit and chicken. Brain Res Mol Brain Res, 54 (2): 199-211. [PMID:9555012]

33. Hameg A, Bayle F, Nuss P, Dupuis P, Garay RP, Dib M. (2003) Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol, 65 (3): 435-40. [PMID:12527336]

34. Ishibashi T, Horisawa T, Tokuda K, Ishiyama T, Ogasa M, Tagashira R, Matsumoto K, Nishikawa H, Ueda Y, Toma S et al.. (2010) Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther, 334 (1): 171-81. [PMID:20404009]

35. John GW, Pauwels PJ, Perez M, Halazy S, Le Grand B, Verscheure Y, Valentin JP, Palmier C, Wurch T, Chopin P et al.. (1999) F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine. J Pharmacol Exp Ther, 290 (1): 83-95. [PMID:10381763]

36. Johnson MP, Loncharich RJ, Baez M, Nelson DL. (1994) Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines. Mol Pharmacol, 45 (2): 277-86. [PMID:8114677]

37. Kaplan AL, Confair DN, Kim K, Barros-Álvarez X, Rodriguiz RM, Yang Y, Kweon OS, Che T, McCorvy JD, Kamber DN et al.. (2022) Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity. Nature, 610 (7932): 582-591. [PMID:36171289]

38. Kawano H, Tsuji H, Nishimura H, Kimura S, Yano S, Ukimura N, Kunieda Y, Yoshizumi M, Sugano T, Nakagawa K et al.. (2001) Serotonin induces the expression of tissue factor and plasminogen activator inhibitor-1 in cultured rat aortic endothelial cells. Blood, 97 (6): 1697-702. [PMID:11238110]

39. Kennett GA, Wood MD, Bright F, Cilia J, Piper DC, Gager T, Thomas D, Baxter GS, Forbes IT, Ham P et al.. (1996) In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties. Br J Pharmacol, 117 (3): 427-434. [PMID:8821530]

40. Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, Avenell KY, Stean T, Upton N, Bromidge S et al.. (1997) SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology, 36 (4-5): 609-20. [PMID:9225286]

41. Knight AR, Misra A, Quirk K, Benwell K, Revell D, Kennett G, Bickerdike M. (2004) Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol, 370 (2): 114-23. [PMID:15322733]

42. Kongsamut S, Kang J, Chen XL, Roehr J, Rampe D. (2002) A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs. Eur J Pharmacol, 450 (1): 37-41. [PMID:12176106]

43. Kovács A, Gacsályi I, Wellmann J, Schmidt E, Szücs Z, Dubreuil V, Nicolas JP, Boutin J, Bózsing D, Egyed A et al.. (2003) Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther, 17 (5-6): 427-34. [PMID:15107597]

44. Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL. (2003) H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology, 28 (3): 519-26. [PMID:12629531]

45. Laporte AM, Doyen C, Nevo IT, Chauveau J, Hauw JJ, Hamon M. (1996) Autoradiographic mapping of serotonin 5-HT1A, 5-HT1D, 5-HT2A and 5-HT3 receptors in the aged human spinal cord. J Chem Neuroanat, 11 (1): 67-75. [PMID:8841890]

46. Leopoldo M, Lacivita E, Contino M, Colabufo NA, Berardi F, Perrone R. (2007) Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem, 50 (17): 4214-21. [PMID:17649988]

47. Li N, Wallén NH, Ladjevardi M, Hjemdahl P. (1997) Effects of serotonin on platelet activation in whole blood. Blood Coagul Fibrinolysis, 8 (8): 517-23. [PMID:9491270]

48. Li P, Zhang Q, Robichaud AJ, Lee T, Tomesch J, Yao W, Beard JD, Snyder GL, Zhu H, Peng Y et al.. (2014) Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. J Med Chem, 57 (6): 2670-82. [PMID:24559051]

49. Lopez-Gimenez JF, Villazon M, Brea J, Loza MI, Palacios JM, Mengod G, Vilaro MT. (2001) Multiple conformations of native and recombinant human 5-hydroxytryptamine(2a) receptors are labeled by agonists and discriminated by antagonists. Mol Pharmacol, 60: 690-699. [PMID:11562430]

50. Lucaites VL, Nelson DL, Wainscott DB, Baez M. (1996) Receptor subtype and density determine the coupling repertoire of the 5-HT2 receptor subfamily. Life Sci, 59 (13): 1081-95. [PMID:8809227]

51. Malgouris C, Flamand F, Doble A. (1993) Autoradiographic studies of RP 62203, a potent 5-HT2 receptor antagonist. Pharmacological characterization of [3H]RP 62203 binding in the rat brain. Eur J Pharmacol, 233 (1): 37-45. [PMID:8472747]

52. May JA, Chen HH, Rusinko A, Lynch VM, Sharif NA, McLaughlin MA. (2003) A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. J Med Chem, 46 (19): 4188-95. [PMID:12954071]

53. McLean TH, Parrish JC, Braden MR, Marona-Lewicka D, Gallardo-Godoy A, Nichols DE. (2006) 1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists. J Med Chem, 49 (19): 5794-803. [PMID:16970404]

54. Mijnster MJ, Raimundo AG, Koskuba K, Klop H, Docter GJ, Groenewegen HJ, Voorn P. (1997) Regional and cellular distribution of serotonin 5-hydroxytryptamine2a receptor mRNA in the nucleus accumbens, olfactory tubercle, and caudate putamen of the rat. J Comp Neurol, 389 (1): 1-11. [PMID:9390756]

55. Millan MJ, Gobert A, Lejeune F, Dekeyne A, Newman-Tancredi A, Pasteau V, Rivet JM, Cussac D. (2003) The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways. J Pharmacol Exp Ther, 306 (3): 954-64. [PMID:12750432]

56. Millan MJ, Gobert A, Newman-Tancredi A, Audinot V, Lejeune F, Rivet JM, Cussac D, Nicolas JP, Muller O, Lavielle G. (1998) S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison with clozapine and haloperidol. J Pharmacol Exp Ther, 286 (3): 1341-55. [PMID:9732398]

57. Millan MJ, Gobert A, Newman-Tancredi A, Lejeune F, Cussac D, Rivet JM, Audinot V, Dubuffet T, Lavielle G. (2000) S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626. J Pharmacol Exp Ther, 293 (3): 1048-62. [PMID:10869410]

58. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A. (2002) Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther, 303 (2): 791-804. [PMID:12388666]

59. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Cogé F, Galizzi JP, Boutin JA, Rivet JM et al.. (2000) Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse, 35 (2): 79-95. [PMID:10611634]

60. Moser PC, Bergis OE, Jegham S, Lochead A, Duconseille E, Terranova JP, Caille D, Berque-Bestel I, Lezoualc'h F, Fischmeister R et al.. (2002) SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties. J Pharmacol Exp Ther, 302 (2): 731-41. [PMID:12130738]

61. Nelson DL, Lucaites VL, Wainscott DB, Glennon RA. (1999) Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors. Naunyn Schmiedebergs Arch Pharmacol, 359 (1): 1-6. [PMID:9933142]

62. Nichols DE, Frescas S, Marona-Lewicka D, Kurrasch-Orbaugh DM. (2002) Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD). J Med Chem, 45 (19): 4344-9. [PMID:12213075]

63. Nilsson T, Longmore J, Shaw D, Pantev E, Bard JA, Branchek T, Edvinsson L. (1999) Characterisation of 5-HT receptors in human coronary arteries by molecular and pharmacological techniques. Eur J Pharmacol, 372 (1): 49-56. [PMID:10374714]

64. Ochi T, Sakamoto M, Minamida A, Suzuki K, Ueda T, Une T, Toda H, Matsumoto K, Terauchi Y. (2005) Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent. Bioorg Med Chem Lett, 15 (4): 1055-9. [PMID:15686911]

65. Okamoto K, Imbe H, Morikawa Y, Itoh M, Sekimoto M, Nemoto K, Senba E. (2002) 5-HT2A receptor subtype in the peripheral branch of sensory fibers is involved in the potentiation of inflammatory pain in rats. Pain, 99 (1-2): 133-43. [PMID:12237191]

66. Pälvimäki EP, Roth BL, Majasuo H, Laakso A, Kuoppamäki M, Syvälahti E, Hietala J. (1996) Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor. Psychopharmacology (Berl), 126 (3): 234-40. [PMID:8876023]

67. Parker CA, Gunn RN, Rabiner EA, Slifstein M, Comley R, Salinas C, Johnson CN, Jakobsen S, Houle S, Laruelle M et al.. (2012) Radiosynthesis and characterization of 11C-GSK215083 as a PET radioligand for the 5-HT6 receptor. J Nucl Med, 53 (2): 295-303. [PMID:22223878]

68. Parker MA, Marona-Lewicka D, Lucaites VL, Nelson DL, Nichols DE. (1998) A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor. J Med Chem, 41 (26): 5148-9. [PMID:9857084]

69. Phebus LA, Johnson KW, Zgombick JM, Gilbert PJ, Van Belle K, Mancuso V, Nelson DL, Calligaro DO, Kiefer Jr AD, Branchek TA et al.. (1997) Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci, 61 (21): 2117-26. [PMID:9395253]

70. Pierce PA, Xie GX, Levine JD, Peroutka SJ. (1996) 5-Hydroxytryptamine receptor subtype messenger RNAs in rat peripheral sensory and sympathetic ganglia: a polymerase chain reaction study. Neuroscience, 70 (2): 553-9. [PMID:8848158]

71. Pierce PA, Xie GX, Peroutka SJ, Green PG, Levine JD. (1995) 5-Hydroxytryptamine-induced synovial plasma extravasation is mediated via 5-hydroxytryptamine2A receptors on sympathetic efferent terminals. J Pharmacol Exp Ther, 275 (1): 502-8. [PMID:7562592]

72. Pompeiano M, Palacios JM, Mengod G. (1994) Distribution of the serotonin 5-HT2 receptor family mRNAs: comparison between 5-HT2A and 5-HT2C receptors. Brain Res Mol Brain Res, 23 (1-2): 163-78. [PMID:8028479]

73. Porter RH, Benwell KR, Lamb H, Malcolm CS, Allen NH, Revell DF, Adams DR, Sheardown MJ. (1999) Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells. Br J Pharmacol, 128 (1): 13-20. [PMID:10498829]

74. Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Göthert M, Jones BJ, Roberts C, Watson JM, Middlemiss DN. (1997) SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol, 356 (3): 312-20. [PMID:9303567]

75. Rashid M, Manivet P, Nishio H, Pratuangdejkul J, Rajab M, Ishiguro M, Launay JM, Nagatomo T. (2003) Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci, 73 (2): 193-207. [PMID:12738034]

76. Reavill C, Kettle A, Holland V, Riley G, Blackburn TP. (1999) Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol, 126 (3): 572-4. [PMID:10188965]

77. Rosier A, Dupont P, Peuskens J, Bormans G, Vandenberghe R, Maes M, de Groot T, Schiepers C, Verbruggen A, Mortelmans L. (1996) Visualisation of loss of 5-HT2A receptors with age in healthy volunteers using [18F]altanserin and positron emission tomographic imaging. Psychiatry Res, 68 (1): 11-22. [PMID:9027929]

78. Rothman RB, Baumann MH, Savage JE, Rauser L, McBride A, Hufeisen SJ, Roth BL. (2000) Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation, 102 (23): 2836-41. [PMID:11104741]

79. Sard H, Kumaran G, Morency C, Roth BL, Toth BA, He P, Shuster L. (2005) SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. Bioorg Med Chem Lett, 15 (20): 4555-9. [PMID:16061378]

80. Schmitz B, Ullmer C, Segelcke D, Gwarek M, Zhu XR, Lübbert H. (2015) BF-1--a novel selective 5-HT2B receptor antagonist blocking neurogenic dural plasma protein extravasation in guinea pigs. Eur J Pharmacol, 751: 73-80. [PMID:25666387]

81. Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE. (1996) Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl.), 124 (1-2): 57-73. [PMID:8935801]

82. Seeman P, Chau-Wong M, Tedesco J, Wong K. (1975) Brain receptors for antipsychotic drugs and dopamine: direct binding assays. Proc Natl Acad Sci USA, 72 (11): 4376-80. [PMID:1060115]

83. Seo HJ, Park EJ, Kim MJ, Kang SY, Lee SH, Kim HJ, Lee KN, Jung ME, Lee M, Kim MS et al.. (2011) Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter. J Med Chem, 54 (18): 6305-18. [PMID:21823597]

84. Shahid M, Walker GB, Zorn SH, Wong EH. (2009) Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol (Oxford), 23 (1): 65-73. [PMID:18308814]

85. Shajib MS, Khan WI. (2015) The role of serotonin and its receptors in activation of immune responses and inflammation. Acta Physiol (Oxf), 213 (3): 561-74. [PMID:25439045]

86. Shapiro DA, Kristiansen K, Kroeze WK, Roth BL. (2000) Differential modes of agonist binding to 5-hydroxytryptamine(2A) serotonin receptors revealed by mutation and molecular modeling of conserved residues in transmembrane region 5. Mol Pharmacol, 58 (5): 877-86. [PMID:11040033]

87. Shapiro DA, Renock S, Arrington E, Chiodo LA, Liu LX, Sibley DR, Roth BL, Mailman R. (2003) Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology. Neuropsychopharmacology, 28 (8): 1400-11. [PMID:12784105]

88. Sleight AJ, Stam NJ, Mutel V, Vanderheyden PM. (1996) Radiolabelling of the human 5-HT2A receptor with an agonist, a partial agonist and an antagonist: effects on apparent agonist affinities. Biochem Pharmacol, 51 (1): 71-6. [PMID:8534270]

89. Snyder GL, Vanover KE, Zhu H, Miller DB, O'Callaghan JP, Tomesch J, Li P, Zhang Q, Krishnan V, Hendrick JP et al.. (2015) Functional profile of a novel modulator of serotonin, dopamine, and glutamate neurotransmission. Psychopharmacology (Berl.), 232 (3): 605-21. [PMID:25120104]

90. Stam NJ, Van Huizen F, Van Alebeek C, Brands J, Dijkema R, Tonnaer JA, Olijve W. (1992) Genomic organization, coding sequence and functional expression of human 5-HT2 and 5-HT1A receptor genes. Eur J Pharmacol, 227 (2): 153-62. [PMID:1330647]

91. Stefulj J, Jernej B, Cicin-Sain L, Rinner I, Schauenstein K. (2000) mRNA expression of serotonin receptors in cells of the immune tissues of the rat. Brain Behav Immun, 14 (3): 219-24. [PMID:10970681]

92. Sánchez C, Hyttel J. (1999) Comparison of the effects of antidepressants and their metabolites on reuptake of biogenic amines and on receptor binding. Cell Mol Neurobiol, 19 (4): 467-89. [PMID:10379421]

93. Thomsen WJ, Grottick AJ, Menzaghi F, Reyes-Saldana H, Espitia S, Yuskin D, Whelan K, Martin M, Morgan M, Chen W et al.. (2008) Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. J Pharmacol Exp Ther, 325 (2): 577-87. [PMID:18252809]

94. Vanover KE, Harvey SC, Son T, Bradley SR, Kold H, Makhay M, Veinbergs I, Spalding TA, Weiner DM, Andersson CM et al.. (2004) Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist. J Pharmacol Exp Ther, 310 (3): 943-51. [PMID:15102927]

95. Wang P, Zhu H, Tian JS, Zhu W, Xu S, Yao H, Liu J, Zhu Z, Miao CY, Xu J. (2024) Discovery of MT-1207: A Novel, Potent Multitarget Inhibitor as a Promising Clinical Candidate for the Treatment of Hypertension. J Med Chem, 67 (18): 16128-16144. [PMID:38968440]

96. Watson J, Brough S, Coldwell MC, Gager T, Ho M, Hunter AJ, Jerman J, Middlemiss DN, Riley GJ, Brown AM. (1998) Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors. Br J Pharmacol, 125 (7): 1413-20. [PMID:9884068]

97. Watts SW, Gilbert L, Webb RC. (1995) 5-Hydroxytryptamine2B receptor mediates contraction in the mesenteric artery of mineralocorticoid hypertensive rats. Hypertension, 26 (6 Pt 2): 1056-9. [PMID:7498967]

98. Watts SW, Thompson JM. (2004) Characterization of the contractile 5-hydroxytryptamine receptor in the renal artery of the normotensive rat. J Pharmacol Exp Ther, 309 (1): 165-72. [PMID:14724222]

99. Xu X, Wei Y, Guo Q, Zhao S, Liu Z, Xiao T, Liu Y, Qiu Y, Hou Y, Zhang G et al.. (2018) Pharmacological Characterization of H05, a Novel Serotonin and Noradrenaline Reuptake Inhibitor with Moderate 5-HT2A Antagonist Activity for the Treatment of Depression. J Pharmacol Exp Ther, 365 (3): 624-635. [PMID:29615471]

100. Yang W, Chen K, Lan NC, Gallaher TK, Shih JC. (1992) Gene structure and expression of the mouse 5-HT2 receptor. J Neurosci Res, 33 (2): 196-204. [PMID:1333538]

Contributors

Show »

How to cite this page