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

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5-HT2C receptor

target has curated data in GtoImmuPdb

Target id: 8

Nomenclature: 5-HT2C receptor

Family: 5-Hydroxytryptamine receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 458 Xq24 HTR2C 5-hydroxytryptamine receptor 2C 73
Mouse 7 459 X D-F4 Htr2c 5-hydroxytryptamine (serotonin) receptor 2C 24,79
Rat 7 460 Xq34-q35.1 Htr2c 5-hydroxytryptamine receptor 2C 4
Previous and Unofficial Names
5-HT1C [55] | 5-HT2C | HTR1C | 5-HTR2C | 5-hydroxytryptamine receptor 1C | serotonin 1c receptor | serotonin receptor 2C | 5-hydroxytryptamine (serotonin) receptor 2C, G protein-coupled
Database Links
Specialist databases
GPCRDB 5ht2c_human (Hs), 5ht2c_mouse (Mm), 5ht2c_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
5-hydroxytryptamine

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

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
[125I]DOI Rn Full agonist 9.1 pKd 3
pKd 9.1 [3]
[125I]DOI Hs Full agonist 8.7 – 9.0 pKd 22
pKd 8.7 – 9.0 (Kd 2x10-9 – 1.1x10-9 M) [22]
YM348 Hs Full agonist 9.0 pKi 37
pKi 9.0 [37]
methysergide Rn Partial agonist 8.7 pKi 66
pKi 8.7 [66]
ergotamine Hs Partial agonist 8.7 pKi 38
pKi 8.7 [38]
(+)-LSD Hs Full agonist 8.2 – 9.0 pKi 22,38
pKi 8.2 – 9.0 [22,38]
AL-37350A Hs Full agonist 8.5 pKi 44
pKi 8.5 [44]
Lysergide Hs Full agonist 8.2 – 8.6 pKi 20
pKi 8.2 – 8.6 [20]
methylergonovine Hs Full agonist 8.3 pKi 38
pKi 8.3 [38]
VER-3323 Hs Full agonist 8.2 pKi 38
pKi 8.2 [38]
lisuride Hs Partial agonist 7.9 – 8.3 pKi 20,22,48
pKi 7.9 – 8.3 [20,22,48]
(+)-DOI Hs Full agonist 8.1 pKi 38
pKi 8.1 [38]
ORG-37684 Hs Full agonist 8.1 pKi 38
pKi 8.1 [38]
(R)-DOI Hs Full agonist 7.4 – 8.7 pKi 22,38,44,51
pKi 8.4 [44]
pKi 7.4 – 8.7 [22,38,51]
Ro 60-0175 Hs Full agonist 7.7 – 8.2 pKi 37-38
pKi 7.7 – 8.2 (Ki 1.99x10-8 – 6.31x10-9 M) [37-38]
DOI Hs Full agonist 7.2 – 8.6 pKi 20,51,67
pKi 7.2 – 8.6 (Ki 6.31x10-8 – 2.51x10-9 M) [20,51,67]
ergotamine Rn Partial agonist 7.9 pKi 66
pKi 7.9 [66]
methylergonovine Rn Full agonist 7.9 pKi 66
pKi 7.9 [66]
brolamfetamine Hs Full agonist 6.8 – 8.9 pKi 20,38,51
pKi 6.8 – 8.9 [20,38,51]
Org 12962 Hs Full agonist 7.8 pKi 38
pKi 7.8 [38]
lorcaserin Hs Full agonist 7.8 pKi 75
pKi 7.8 [75]
α-methyl-5-HT Hs Full agonist 6.9 – 8.6 pKi 22,38
pKi 6.9 – 8.6 [22,38]
5-hydroxytryptamine Hs Full agonist 6.8 – 8.6 pKi 20,22,37-38,44
pKi 6.8 – 8.6 [20,22,37-38,44]
S 16924 Hs Full agonist 7.7 pKi 46
pKi 7.7 [46]
aripiprazole Hs Partial agonist 7.6 pKi 40
pKi 7.6 [40]
m-chlorophenylpiperazine Hs Partial agonist 6.5 – 8.5 pKi 20,22,37-38,51,67
pKi 6.5 – 8.5 [20,22,37-38,51,67]
WAY-163909 Hs Full agonist 6.7 – 8.0 pKi 19
pKi 6.7 – 8.0 (Ki 1.99x10-7 – 1x10-8 M) [19]
5-hydroxytryptamine Rn Full agonist 6.7 – 7.9 pKi 32,66
pKi 6.7 – 7.9 [32,66]
5-MeOT Hs Full agonist 6.7 – 7.8 pKi 20
pKi 6.7 – 7.8 [20]
m-chlorophenylpiperazine Rn Partial agonist 7.2 pKi 66
pKi 7.2 [66]
TFMPP Hs Full agonist 6.5 – 7.8 pKi 20,38
pKi 6.5 – 7.8 [20,38]
GR 127935 Hs Partial agonist 7.0 pKi 60
pKi 7.0 [60]
BW723C86 Hs Full agonist 6.9 – 7.1 pKi 38,67
pKi 6.9 – 7.1 [38,67]
RU 24969 Hs Full agonist 6.8 pKi 38
pKi 6.8 [38]
SB 216641 Hs Partial agonist 6.8 pKi 60
pKi 6.8 [60]
quipazine Hs Full agonist 5.9 – 7.3 pKi 20,22,38
pKi 5.9 – 7.3 [20,22,38]
5-MeO-DMT Hs Full agonist 6.2 – 7.0 pKi 22
pKi 6.2 – 7.0 [22]
brolamfetamine Rn Full agonist 6.6 pKi 32
pKi 6.6 [32]
oxymetazoline Hs Full agonist 6.3 – 6.8 pKi 22
pKi 6.3 – 6.8 [22]
pergolide Hs Partial agonist 6.5 pKi 48
pKi 6.5 [48]
tryptamine Hs Full agonist 5.6 – 7.2 pKi 20,38
pKi 5.6 – 7.2 [20,38]
5-MeOT Rn Full agonist 6.3 pKi 32
pKi 6.3 [32]
MK-212 Hs Full agonist 5.6 – 7.0 pKi 20,38,67
pKi 5.6 – 7.0 [20,38,67]
BRL-15572 Hs Partial agonist 6.2 pKi 60
pKi 6.2 [60]
cabergoline Hs Full agonist 6.2 pKi 48
pKi 6.2 [48]
bromocriptine Hs Partial agonist 6.1 pKi 48
pKi 6.1 [48]
5-CT Hs Full agonist 5.2 – 6.7 pKi 20,38
pKi 5.2 – 6.7 [20,38]
8-OH-DPAT Hs Full agonist 5.6 pKi 38
pKi 5.6 [38]
CGS-12066 Hs Full agonist 5.6 pKi 38
pKi 5.6 [38]
LY344864 Hs Full agonist 5.5 pKi 56
pKi 5.5 [56]
capeserod Hs Partial agonist 5.3 pKi 50
pKi 5.3 [50]
quinpirole Hs Full agonist 5.0 – 5.5 pKi 38,48
pKi 5.0 – 5.5 [38,48]
lorcaserin Hs Full agonist 8.1 pEC50 75
pEC50 8.1 [75]
lorcaserin Hs Agonist 8.2 pIC50 72
pIC50 8.2 (IC50 5.8x10-9 M) [72]
Description: IP accumulation assay.
[3H]LSD Hs Agonist - -
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
[3H]mesulergine Hs Inverse agonist 8.7 – 9.3 pKd 22,63
pKd 8.7 – 9.3 (Kd 2.2x10-9 – 5x10-10 M) [22,63]
methysergide Rn Antagonist 9.3 pKi 32
pKi 9.3 [32]
mesulergine Rn Inverse agonist 9.2 pKi 32
pKi 9.2 [32]
sertindole Hs Inverse agonist 9.0 – 9.2 pKi 34,40
pKi 9.0 – 9.2 [34,40]
mianserin Rn Antagonist 8.8 – 9.4 pKi 32,62
pKi 8.8 – 9.4 [32,62]
SB 228357 Hs Antagonist 9.0 – 9.1 pKi 7,65
pKi 9.0 – 9.1 [7,65]
mesulergine Hs Inverse agonist 8.7 – 9.3 pKi 30,38-39
pKi 8.7 – 9.3 [30,38-39]
FR260010 Hs Antagonist 9.0 pKi 31
pKi 9.0 (Ki 1.1x10-9 M) [31]
ritanserin Hs Antagonist 8.2 – 9.6 pKi 38
pKi 8.2 – 9.6 [38]
methysergide Hs Antagonist 8.6 – 9.1 pKi 20,38
pKi 8.6 – 9.1 [20,38]
metergoline Hs Inverse agonist 8.8 pKi 38
pKi 8.8 [38]
mianserin Hs Inverse agonist 8.3 – 9.2 pKi 22,38,49
pKi 8.3 – 9.2 [22,38,49]
SB 221284 Hs Antagonist 8.7 pKi 38
pKi 8.7 [38]
amoxapine Rn Antagonist 8.7 pKi 62
pKi 8.7 [62]
zotepine Hs Inverse agonist 8.6 pKi 34
pKi 8.6 [34]
SB 242084 Hs Antagonist 8.2 – 9.0 pKi 36,38
pKi 8.2 – 9.0 (Ki 6.31x10-9 – 1x10-9 M) [36,38]
ziprasidone Hs Inverse agonist 7.9 – 9.0 pKi 34,40,70
pKi 7.9 – 9.0 [34,40,70]
methiothepin Hs Inverse agonist 8.4 pKi 38
pKi 8.4 [38]
RS-102221 Rn Antagonist 8.4 pKi 5
pKi 8.4 [5]
RS-102221 Hs Antagonist 8.3 – 8.4 pKi 5,38
pKi 8.3 – 8.4 (Ki 5.01x10-9 – 3.98x10-9 M) [5,38]
tiospirone Hs Inverse agonist 8.3 pKi 34
pKi 8.3 [34]
olanzapine Hs Inverse agonist 8.1 – 8.4 pKi 34,40,70
pKi 8.1 – 8.4 [34,40,70]
SDZ SER-082 Hs Antagonist 8.1 pKi 38
pKi 8.1 [38]
amitriptyline Rn Antagonist 8.1 pKi 74
pKi 8.1 (Ki 8x10-9 M) [74]
clozapine Hs Inverse agonist 7.4 – 8.7 pKi 22,34,38,40,46,76
pKi 7.4 – 8.7 [22,34,38,40,46,76]
cyamemazine Hs Antagonist 7.9 pKi 30
pKi 7.9 [30]
loxapine Hs Inverse agonist 7.8 – 8.0 pKi 34,40
pKi 7.8 – 8.0 [34,40]
chlorpromazine Hs Antagonist 7.6 – 8.2 pKi 34,40
pKi 7.6 – 8.2 [34,40]
SB 206553 Hs Antagonist 7.8 – 7.9 pKi 35,38
pKi 7.8 – 7.9 [35,38]
EGIS-7625 Hs Antagonist 7.7 pKi 39
pKi 7.7 [39]
SB 215505 Hs Antagonist 7.7 pKi 65
pKi 7.7 [65]
volinanserin Hs Antagonist 7.5 – 7.7 pKi 38,65
pKi 7.5 – 7.7 [38,65]
risperidone Hs Inverse agonist 7.5 – 7.6 pKi 34,40
pKi 7.5 – 7.6 [34,40]
mirtazapine Hs Antagonist 7.4 pKi 21
pKi 7.4 (Ki 3.9x10-8 M) [21]
xanomeline Hs Antagonist 7.4 pKi 78
pKi 7.4 [78]
sarpogrelate Hs Antagonist 7.4 pKi 63
pKi 7.4 [63]
terguride Hs Antagonist 7.3 pKi 48
pKi 7.3 [48]
fluoxetine Rn Antagonist 7.3 pKi 66
pKi 7.3 [66]
thioridazine Hs Antagonist 7.2 – 7.3 pKi 34,40
pKi 7.2 – 7.3 [34,40]
ketanserin Hs Antagonist 6.8 – 7.5 pKi 8,22,38,63
pKi 6.8 – 7.5 [8,22,38,63]
S33084 Hs Antagonist 7.1 pKi 47
pKi 7.1 [47]
apomorphine Hs Antagonist 7.0 pKi 48
pKi 7.0 [48]
LY334362 Hs Antagonist 7.0 pKi 8
pKi 7.0 [8]
perphenazine Hs Antagonist 6.9 pKi 40
pKi 6.9 [40]
glemanserin Hs Antagonist 6.6 pKi 38
pKi 6.6 [38]
trazodone Hs Antagonist 6.6 pKi 38
pKi 6.6 [38]
idalopirdine Hs Antagonist 6.6 pKi 41
pKi 6.6 (Ki 2.5x10-7 M) [41]
trazodone Rn Antagonist 6.4 – 6.7 pKi 62,66
pKi 6.4 – 6.7 [62,66]
roxindole Hs Antagonist 6.5 pKi 48
pKi 6.5 [48]
norfluoxetine Rn Antagonist 6.5 pKi 66
pKi 6.5 [66]
trifluoperazine Hs Antagonist 6.4 pKi 40
pKi 6.4 [40]
mesoridazine Hs Antagonist 6.4 pKi 13
pKi 6.4 (Ki 4.12x10-7 M) [13]
RS-127445 Hs Antagonist 6.3 pKi 38
pKi 6.3 [38]
MPDT Rn Antagonist 6.2 pKi 29
pKi 6.2 [29]
agomelatine Hs Antagonist 6.2 pKi 45
pKi 6.2 [45]
duloxetine Hs Antagonist 6.0 pKi 11
pKi 6.0 [11]
SB 224289 Hs Antagonist 5.7 – 6.2 pKi 38,68
pKi 6.2 [68]
pKi 5.7 [38]
spiperone Hs Antagonist 5.6 – 6.2 pKi 22,34,38
pKi 5.6 – 6.2 [22,34,38]
spiramide Hs Antagonist 5.8 pKi 38
pKi 5.8 [38]
SB 204741 Hs Antagonist 5.6 pKi 38
pKi 5.6 [38]
AC-90179