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

5-HT2C receptor

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

   GtoImmuPdb view: OFF :     5-HT2C receptor has curated GtoImmuPdb data

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 458 Xq24 HTR2C 5-hydroxytryptamine receptor 2C 73
Mouse 7 459 X D-F4 Htr2c 5-hydroxytryptamine (serotonin) receptor 2C 24,78
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 Units 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 Units 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 77
pKi 7.4 [77]
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 Hs Inverse agonist 5.5 pKi 56
pKi 5.5 [56]
SB 243213 Hs Antagonist 9.0 pEC50 7
pEC50 9.0 [7]
View species-specific antagonist tables
Antagonist Comments
Mirtazapine is an antagonist of α2-adrenoceptors and serotonin 5-HT2A and 5-HT2C receptors.
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.
Cell Type Associations
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   macrophage (CL:0000235)
References:  71
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  17-18,42
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  42
Tissue Distribution
Resting lymphocytes.
Species:  Human
Technique:  RT-PCR.
References:  43
CNS: choroid plexuses, retrosplenial, piriform and entorhinal cortex, anterior olfactory nucleus, lateral septal nucleus, subthalamic nucleus, amygdala, subiculum and ventral part of CA3, lateral habenula, substantia nigra pars compacta, several brainstem nuclei and the whole grey matter of the spinal cord.
Species:  Rat
Technique:  in situ hybridisation.
References:  58
Medulla oblongata and grey matter of the spinal cord.