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5-HT2C receptor

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Target id: 8

Nomenclature: 5-HT2C 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 7 458 Xq23 HTR2C 5-hydroxytryptamine receptor 2C 73
Mouse 7 459 X 68.46 cM Htr2c 5-hydroxytryptamine (serotonin) receptor 2C 24,79
Rat 7 460 Xq34 Htr2c 5-hydroxytryptamine receptor 2C 4
Previous and Unofficial Names Click here for help
5-HT1C [56] | 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 Click here for help
Specialist databases
GPCRdb 5ht2c_human (Hs), 5ht2c_mouse (Mm), 5ht2c_rat (Rn)
Other databases
Alphafold P28335 (Hs), P34968 (Mm), P08909 (Rn)
ChEMBL Target CHEMBL225 (Hs), CHEMBL3006 (Mm), CHEMBL324 (Rn)
DrugBank Target P28335 (Hs)
Ensembl Gene ENSG00000147246 (Hs), ENSMUSG00000041380 (Mm), ENSRNOG00000030877 (Rn)
Entrez Gene 3358 (Hs), 15560 (Mm), 25187 (Rn)
Human Protein Atlas ENSG00000147246 (Hs)
KEGG Gene hsa:3358 (Hs), mmu:15560 (Mm), rno:25187 (Rn)
OMIM 312861 (Hs)
Pharos P28335 (Hs)
RefSeq Nucleotide NM_000868 (Hs), NM_008312 (Mm), NM_012765 (Rn)
RefSeq Protein NP_000859 (Hs), NP_032338 (Mm), NP_036897 (Rn)
UniProtKB P28335 (Hs), P34968 (Mm), P08909 (Rn)
Wikipedia HTR2C (Hs)
Natural/Endogenous Ligands Click here for help
5-hydroxytryptamine

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
[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 3
⤷ pKd 9.1 [3]
[125I]DOI Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.7 – 9.0 pKd 22
⤷ pKd 8.7 – 9.0 (Kd 2x10-9 – 1.1x10-9 M) [22]
YM348 Small molecule or natural product Hs Full agonist 9.0 pKi 37
⤷ pKi 9.0 [37]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 8.7 pKi 66
⤷ pKi 8.7 [66]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.7 pKi 38
⤷ pKi 8.7 [38]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 – 9.0 pKi 22,38
⤷ pKi 8.2 – 9.0 [22,38]
AL-37350A Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.5 pKi 44
⤷ pKi 8.5 [44]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.2 – 8.6 pKi 20
⤷ pKi 8.2 – 8.6 [20]
methylergonovine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.3 pKi 38
⤷ pKi 8.3 [38]
VER-3323 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 pKi 38
⤷ pKi 8.2 [38]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.9 – 8.3 pKi 20,22,48
⤷ pKi 7.9 – 8.3 [20,22,48]
(+)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.1 pKi 38
⤷ pKi 8.1 [38]
ORG-37684 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.1 pKi 38
⤷ pKi 8.1 [38]
(R)-DOI Small molecule or natural product Click here for species-specific activity table 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 Small molecule or natural product Click here for species-specific activity table 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 Small molecule or natural product Click here for species-specific activity table 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 Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.9 pKi 66
⤷ pKi 7.9 [66]
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 66
⤷ pKi 7.9 [66]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.8 – 8.9 pKi 20,38,51
⤷ pKi 6.8 – 8.9 [20,38,51]
Org 12962 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 38
⤷ pKi 7.8 [38]
lorcaserin 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 Full agonist 7.8 pKi 75
⤷ pKi 7.8 [75]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 – 8.6 pKi 22,38
⤷ pKi 6.9 – 8.6 [22,38]
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 6.8 – 8.6 pKi 20,22,37-38,44
⤷ pKi 6.8 – 8.6 [20,22,37-38,44]
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.7 pKi 46
⤷ pKi 7.7 [46]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.6 pKi 40
⤷ pKi 7.6 [40]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table 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 Small molecule or natural product Hs Full agonist 6.7 – 8.0 pKi 19
⤷ pKi 6.7 – 8.0 (Ki 1.99x10-7 – 1x10-8 M) [19]
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 6.7 – 7.9 pKi 32,66
⤷ pKi 6.7 – 7.9 [32,66]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.7 – 7.8 pKi 20
⤷ pKi 6.7 – 7.8 [20]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 7.2 pKi 66
⤷ pKi 7.2 [66]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.5 – 7.8 pKi 20,38
⤷ pKi 6.5 – 7.8 [20,38]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.0 pKi 61
⤷ pKi 7.0 [61]
BW723C86 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 – 7.1 pKi 38,67
⤷ pKi 6.9 – 7.1 [38,67]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.8 pKi 38
⤷ pKi 6.8 [38]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 pKi 61
⤷ pKi 6.8 [61]
quipazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.9 – 7.3 pKi 20,22,38
⤷ pKi 5.9 – 7.3 [20,22,38]
5-MeO-DMT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.2 – 7.0 pKi 22
⤷ pKi 6.2 – 7.0 [22]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.6 pKi 32
⤷ pKi 6.6 [32]
oxymetazoline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.3 – 6.8 pKi 22
⤷ pKi 6.3 – 6.8 [22]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 6.5 pKi 48
⤷ pKi 6.5 [48]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.6 – 7.2 pKi 20,38
⤷ pKi 5.6 – 7.2 [20,38]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 6.3 pKi 32
⤷ pKi 6.3 [32]
MK-212 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 – 7.0 pKi 20,38,67
⤷ pKi 5.6 – 7.0 [20,38,67]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 6.2 pKi 61
⤷ pKi 6.2 [61]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.2 pKi 48
⤷ pKi 6.2 [48]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 6.1 pKi 48
⤷ pKi 6.1 [48]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.2 – 6.7 pKi 20,38
⤷ pKi 5.2 – 6.7 [20,38]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 pKi 38
⤷ pKi 5.6 [38]
CGS-12066 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 pKi 38
⤷ pKi 5.6 [38]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.5 pKi 57
⤷ pKi 5.5 [57]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.3 pKi 50
⤷ pKi 5.3 [50]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.0 – 5.5 pKi 38,48
⤷ pKi 5.0 – 5.5 [38,48]
lorcaserin 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 Full agonist 8.1 pEC50 75
⤷ pEC50 8.1 [75]
lorcaserin 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 Agonist 8.2 pIC50 72
⤷ pIC50 8.2 (IC50 5.8x10-9 M) [72]
Description: IP accumulation assay.
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive 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 Value Parameter Reference
[3H]mesulergine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive 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 Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.3 pKi 32
⤷ pKi 9.3 [32]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Inverse agonist 9.2 pKi 32
⤷ pKi 9.2 [32]
sertindole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 9.0 – 9.2 pKi 34,40
⤷ pKi 9.0 – 9.2 [34,40]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.8 – 9.4 pKi 32,55
⤷ pKi 8.8 – 9.4 [32,55]
SB 228357 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 – 9.1 pKi 7,65
⤷ pKi 9.0 – 9.1 [7,65]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.7 – 9.3 pKi 30,38-39
⤷ pKi 8.7 – 9.3 [30,38-39]
FR260010 Small molecule or natural product Hs Antagonist 9.0 pKi 31
⤷ pKi 9.0 (Ki 1.1x10-9 M) [31]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.2 – 9.6 pKi 38
⤷ pKi 8.2 – 9.6 [38]
methysergide 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 8.6 – 9.1 pKi 20,38
⤷ pKi 8.6 – 9.1 [20,38]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.8 pKi 38
⤷ pKi 8.8 [38]
mianserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 8.3 – 9.2 pKi 22,38,49
⤷ pKi 8.3 – 9.2 [22,38,49]
SB 221284 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.7 pKi 38
⤷ pKi 8.7 [38]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.7 pKi 55
⤷ pKi 8.7 [55]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.6 pKi 34
⤷ pKi 8.6 [34]
SB 242084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 9.0 pKi 36,38
⤷ pKi 8.2 – 9.0 (Ki 6.31x10-9 – 1x10-9 M) [36,38]
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 Inverse agonist 7.9 – 9.0 pKi 34,40,70
⤷ pKi 7.9 – 9.0 [34,40,70]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.4 pKi 38
⤷ pKi 8.4 [38]
RS-102221 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.4 pKi 5
⤷ pKi 8.4 [5]
RS-102221 Small molecule or natural product Click here for species-specific activity table 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 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.3 pKi 34
⤷ pKi 8.3 [34]
olanzapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 8.1 – 8.4 pKi 34,40,70
⤷ pKi 8.1 – 8.4 [34,40,70]
SDZ SER-082 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.1 pKi 38
⤷ pKi 8.1 [38]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.1 pKi 74
⤷ pKi 8.1 (Ki 8x10-9 M) [74]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure 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 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.9 pKi 30
⤷ pKi 7.9 [30]
loxapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 7.8 – 8.0 pKi 34,40
⤷ pKi 7.8 – 8.0 [34,40]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.6 – 8.2 pKi 34,40
⤷ pKi 7.6 – 8.2 [34,40]
SB 206553 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 – 7.9 pKi 35,38
⤷ pKi 7.8 – 7.9 [35,38]
EGIS-7625 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 39
⤷ pKi 7.7 [39]
SB 215505 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 65
⤷ pKi 7.7 [65]
volinanserin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 – 7.7 pKi 38,65
⤷ pKi 7.5 – 7.7 [38,65]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 7.5 – 7.6 pKi 34,40
⤷ pKi 7.5 – 7.6 [34,40]
mirtazapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.4 pKi 21
⤷ pKi 7.4 (Ki 3.9x10-8 M) [21]
xanomeline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.4 pKi 78
⤷ pKi 7.4 [78]
sarpogrelate Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.4 pKi 63
⤷ pKi 7.4 [63]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 pKi 48
⤷ pKi 7.3 [48]
fluoxetine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.3 pKi 66
⤷ pKi 7.3 [66]
thioridazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.2 – 7.3 pKi 34,40
⤷ pKi 7.2 – 7.3 [34,40]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.8 – 7.5 pKi 8,22,38,63
⤷ pKi 6.8 – 7.5 [8,22,38,63]
S33084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.1 pKi 47
⤷ pKi 7.1 [47]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 pKi 48
⤷ pKi 7.0 [48]
LY334362 Small molecule or natural product Hs Antagonist 7.0 pKi 8
⤷ pKi 7.0 [8]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.9 pKi 40
⤷ pKi 6.9 [40]
glemanserin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.6 pKi 38
⤷ pKi 6.6 [38]
trazodone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.6 pKi 38
⤷ pKi 6.6 [38]
idalopirdine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.6 pKi 41
⤷ pKi 6.6 (Ki 2.5x10-7 M) [41]
trazodone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.4 – 6.7 pKi 55,66
⤷ pKi 6.4 – 6.7 [55,66]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 48
⤷ pKi 6.5 [48]
norfluoxetine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.5 pKi 66
⤷ pKi 6.5 [66]
trifluoperazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.4 pKi 40
⤷ pKi 6.4 [40]
mesoridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.4 pKi 13
⤷ pKi 6.4 (Ki 4.12x10-7 M) [13]
RS-127445 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 38
⤷ pKi 6.3 [38]
MPDT Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.2 pKi 29
⤷ pKi 6.2 [29]
agomelatine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.2 pKi 45
⤷ pKi 6.2 [45]
duloxetine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.0 pKi 11
⤷ pKi 6.0 [11]
SB 224289 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.7 – 6.2 pKi 38,68
⤷ pKi 6.2 [68]
pKi 5.7 [38]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.6 – 6.2 pKi 22,34,38
⤷ pKi 5.6 – 6.2 [22,34,38]
spiramide Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.8 pKi 38
⤷ pKi 5.8 [38]
SB 204741 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 pKi 38
⤷ pKi 5.6 [38]
AC-90179 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 5.5 pKi 57
⤷ pKi 5.5 [57]
SB 243213 Small molecule or natural product Click here for species-specific activity table 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.
Immunopharmacology Comments
The expression of 5-HT2B receptors on immune cells indicates that it plays some part in immune/inflammatory responses [77].
Cell Type Associations
Immuno Cell Type:  T cells
Comment:  Expressed by T cells.
References:  77
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   macrophage (CL:0000235)
References:  71
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  17-18,42
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
References:  42
Tissue Distribution Click here for help
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:  59
Medulla oblongata and grey matter of the spinal cord.
Species:  Rat
Technique:  in situ hybridisation.
References:  26
Lumbar dorsal root ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  58
GABAergic cells of the anterior raphe nuclei.
Species:  Rat
Technique:  Double in situ hybridisation.
References:  69
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]

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Functional Assays Click here for help
Measurement of IP and IP3 levels in AV12 cells transfected with the mouse 5-HT2C receptor.
Species:  Mouse
Tissue:  AV12 cells.
Response measured:  IP and IP3 production.
References:  42
Measurement of cAMP levels in AV12 cells transfected with the mouse 5-HT2C receptor.
Species:  Mouse
Tissue:  AV12 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  42
Measurement of cAMP levels in AV12 cells transfected with the human 5-HT2C receptor.
Species:  Human
Tissue:  AV12 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  42
Measurement of intracellular Ca2+ levels using a fluorometric imaging plate reader (FLIPR) in CHO-K1 cells transfected with the human 5-HT2C receptor.
Species:  Human
Tissue:  CHO-K1 cells.
Response measured:  Increase in intracellular [Ca2+].
References:  60
Measurement of phosphatidylinositol turnover in rat choroid plexus.
Species:  Rat
Tissue:  Choroid plexus.
Response measured:  Stimulation of phosphatidylinositol turnover.
References:  17
Physiological Functions Click here for help
Analgesia.
Species:  Mouse
Tissue:  In vivo.
References:  14
Anxiety.
Species:  Rat
Tissue:  In vivo.
References:  1,28
Hyperlocomotion.
Species:  Rat
Tissue:  In vivo.
References:  25
Decrease in food intake.
Species:  Rat
Tissue:  In vivo.
References:  25
Regulation of sleep.
Species:  Mouse
Tissue:  In vivo.
References:  27
Regulation of the response to repeated stress.
Species:  Mouse
Tissue:  In vivo.
References:  16
Physiological Consequences of Altering Gene Expression Click here for help
5-HT2C receptor knockout mice have increased susceptibility to audiogenic epileptic seizures.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  6
5-HT2C receptor knockout mice exhibit increased food intake followed by the development of late-onset obesity. They also have reduced β3-adrenoceptor levels in white adipose tissue, linked to enhanced adiposity.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  54
5-HT2C receptor knockout mice exhibit abnormal wakefulness and rapid eye movement sleep (REM).
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  27
5-HT2C receptor knockout mice display symptoms of obsessive-compulsive disorder (OCD).
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  15
5-HT2C receptor knockout mice exhibit hyperresponsiveness to repeated stress.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  16
Young 5-HT2C receptor knockout mice exhibit increased activity levels which compensates for the parallel increase in food intake. However in older knockout mice, reductions in the energy cost of physical activity lead to an inability to compensate for increased food intake and late-onset obesity is observed.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  53
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
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0009642 abnormal blood homeostasis PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0005535 abnormal body temperature PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0005266 abnormal metabolism PMID: 19036977 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001492 abnormal pilomotor reflex PMID: 20394819 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0003638 abnormal response/metabolism to endogenous compounds PMID: 9771748 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0001413 abnormal response to new environment PMID: 9844009 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0001463 abnormal spatial learning PMID: 9844009 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0008752 abnormal tumor necrosis factor level PMID: 9771748 
Htr2ctm1Knk Htr2ctm1Knk/Htr2ctm1Knk
B6.Cg-Htr2c		 MGI:96281  MP:0001258 decreased body length PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0001258 decreased body length PMID: 19036977 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001258 decreased body length PMID: 20394819 
Htr2ctm1Knk Htr2ctm1Knk/Htr2ctm1Knk
B6.Cg-Htr2c		 MGI:96281  MP:0006086 decreased body mass index PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0006086 decreased body mass index PMID: 19036977 
Htr2ctm1Knk|Mc4rtm1Lowl Htr2ctm1Knk/Y,Mc4rtm1Lowl/Mc4rtm1Lowl
involves: 129S4/SvJae * C57BL/6		 MGI:96281  MGI:99457  MP:0006086 decreased body mass index PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Htr2ctm1Knk
B6.Cg-Htr2c		 MGI:96281  MP:0001262 decreased body weight PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0001262 decreased body weight PMID: 19036977 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001262 decreased body weight PMID: 20394819 
Htr2c+|Htr2ctm1.1Eme Htr2ctm1.1Eme/Htr2c+
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001262 decreased body weight PMID: 20394819 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Htr2ctm1.1Eme
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001262 decreased body weight PMID: 20394819 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0001780 decreased brown adipose tissue amount PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0005179 decreased circulating cholesterol level PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0005560 decreased circulating glucose level PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0002727 decreased circulating insulin level PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0004701 decreased circulating insulin-like growth factor I level PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0005668 decreased circulating leptin level PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0002644 decreased circulating triglyceride level PMID: 19036977 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0003910 decreased eating behavior PMID: 20394819 
Htr2c+|Htr2ctm1.1Eme Htr2ctm1.1Eme/Htr2c+
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0003910 decreased eating behavior PMID: 20394819 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0010053 decreased grip strength PMID: 20394819 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0003961 decreased lean body mass PMID: 19038216 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0010025 decreased total body fat amount PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0001783 decreased white adipose tissue amount PMID: 19036977 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001429 dehydration PMID: 20394819 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0009746 enhanced behavioral response to xenobiotic PMID: 19036977 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001505 hunched posture PMID: 20394819 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0001399 hyperactivity PMID: 19038216 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0001559 hyperglycemia PMID: 9771748 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0001402 hypoactivity PMID: 19036977 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0004144 hypotonia PMID: 20394819 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0009747 impaired behavioral response to xenobiotic PMID: 7700379 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0009747 impaired behavioral response to xenobiotic PMID: 19038216 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001405 impaired coordination PMID: 20394819 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0005293 impaired glucose tolerance PMID: 9771748 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0008965 increased basal metabolism PMID: 19036977 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0001260 increased body weight PMID: 7700379 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0005123 increased circulating growth hormone level PMID: 19036977 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0002079 increased circulating insulin level PMID: 9771748 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0005669 increased circulating leptin level PMID: 9771748 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0005669 increased circulating leptin level PMID: 19038216 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0003909 increased eating behavior PMID: 19038216 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0003909 increased eating behavior PMID: 20394819 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0004889 increased energy expenditure PMID: 20394819 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0009288 increased epididymal fat pad weight PMID: 7700379 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0009288 increased epididymal fat pad weight PMID: 9771748 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0001441 increased grooming behavior PMID: 7700379 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0005458 increased percent body fat PMID: 19038216 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0008873 increased physiological sensitivity to xenobiotic PMID: 19036977 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0009302 increased renal fat pad weight PMID: 7700379 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0009302 increased renal fat pad weight PMID: 9771748 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0009766 increased sensitivity to xenobiotic induced morbidity/mortality PMID: 19036977 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0003212 increased susceptibility to age related obesity PMID: 9771748 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0005658 increased susceptibility to diet-induced obesity PMID: 9771748 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0005658 increased susceptibility to diet-induced obesity PMID: 19038216 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0002906 increased susceptibility to pharmacologically induced seizures PMID: 7700379 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0000008 increased white adipose tissue amount PMID: 7700379 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0000008 increased white adipose tissue amount PMID: 9771748 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0000008 increased white adipose tissue amount PMID: 19038216 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0005331 insulin resistance PMID: 9771748 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0008569 lethality at weaning PMID: 20394819 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0000421 mottled coat PMID: 20394819 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0001433 polyphagia PMID: 7700379 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0001433 polyphagia PMID: 9771748 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0001433 polyphagia PMID: 19036977 
Htr2ctm1Knk|Mc4rtm1Lowl Htr2ctm1Knk/Y,Mc4rtm1Lowl/Mc4rtm1Lowl
involves: 129S4/SvJae * C57BL/6		 MGI:96281  MGI:99457  MP:0001433 polyphagia PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0001732 postnatal growth retardation PMID: 19036977 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Y
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001732 postnatal growth retardation PMID: 20394819 
Htr2c+|Htr2ctm1.1Eme Htr2ctm1.1Eme/Htr2c+
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001732 postnatal growth retardation PMID: 20394819 
Htr2ctm1.1Eme Htr2ctm1.1Eme/Htr2ctm1.1Eme
involves: 129S4/SvJae * 129S6/SvEvTac * C57BL/6		 MGI:96281  MP:0001732 postnatal growth retardation PMID: 20394819 
Htr2ctm1Knk Htr2ctm1Knk/Htr2ctm1Knk
B6.Cg-Htr2c		 MGI:96281  MP:0002082 postnatal lethality PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0002082 postnatal lethality PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
C.Cg-Htr2c		 MGI:96281  MP:0008489 postnatal slow weight gain PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Htr2ctm1Knk
C.Cg-Htr2c		 MGI:96281  MP:0008489 postnatal slow weight gain PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Htr2ctm1Knk
B6.Cg-Htr2c		 MGI:96281  MP:0008489 postnatal slow weight gain PMID: 19036977 
Htr2ctm1Knk Htr2ctm1Knk/Y
B6.Cg-Htr2c		 MGI:96281  MP:0008489 postnatal slow weight gain PMID: 19036977 
Htr2c+|Htr2ctm1Knk Htr2ctm1Knk/Htr2c+
B6.Cg-Htr2c		 MGI:96281  MP:0008489 postnatal slow weight gain PMID: 19036977 
Htr2ctm1Knk|Htr2ctm2Knk Htr2ctm1Knk/Htr2ctm2Knk
B6.Cg-Htr2c/Htr2c		 MGI:96281  MP:0008489 postnatal slow weight gain PMID: 19036977 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0002083 premature death PMID: 7700379 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0002083 premature death PMID: 19038216 
Htr2ctm1Jke|Tg(Pomc1-cre)16Lowl Htr2ctm1Jke/Y,Tg(Pomc1-cre)16Lowl/0
B6.Cg-Htr2c Tg(Pomc1-cre)16Lowl		 MGI:3640615  MGI:96281  MP:0002083 premature death PMID: 19038216 
Htr2ctm1Jul Htr2ctm1Jul/Y
B6.129S-Htr2c		 MGI:96281  MP:0001473 reduced long term potentiation PMID: 9844009 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0000951 sporadic seizures PMID: 7700379 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0003997 tonic-clonic seizures PMID: 7700379 
Htr2ctm1Jke Htr2ctm1Jke/Y
B6.Cg-Htr2c		 MGI:96281  MP:0003997 tonic-clonic seizures PMID: 19038216 
Htr2ctm1Jke|Tg(Pomc1-cre)16Lowl Htr2ctm1Jke/Y,Tg(Pomc1-cre)16Lowl/0
B6.Cg-Htr2c Tg(Pomc1-cre)16Lowl		 MGI:3640615  MGI:96281  MP:0003997 tonic-clonic seizures PMID: 19038216 
Htr2ctm1Jul Htr2ctm1Jul/Y
either: (involves: 129S2/SvPas * C57BL/6J * DBA/2) or (involves: 129S4/SvJae * C57BL/6J * DBA/2)		 MGI:96281  MP:0002826 tonic seizures PMID: 7700379 
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Description:  A -759T allele within the promoter region of the HTR2C gene has a higher transcriptional activity than the more common -759C allele. Hence, a higher frequency of the -759T allele leads to higher basal expression of 5-HT2C receptors and subsequent protection against antipsychotic-induced weight gain.
References:  9
Type:  RNA editing
Species:  Human
Description:  RNA editing of the 5-HT2C receptor results in the expression of 14 different isoforms in the human brain. The isoforms have different levels of constitutive activity, with the unedited receptor displaying the highest degree and the fully edited receptor displaying no constitutive activity. RNA editing alters receptor-mediated activation of G13 and arachidonic acid production. 5-HT has lower affinity and potency for the fully edited isoform. Atypical antipsychotic drugs display inverse agonist activity at the unedited isoform of the human 5-HT2C receptor.
References:  2,10,23,33-34,52,62,64
General Comments
A non-functional short (248aa) splice-variant of the h 5-HT2C receptor has been described [12].

References

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1. Bagdy G, Graf M, Anheuer ZE, Modos EA, Kantor S. (2001) Anxiety-like effects induced by acute fluoxetine, sertraline or m-CPP treatment are reversed by pretreatment with the 5-HT2C receptor antagonist SB-242084 but not the 5-HT1A receptor antagonist WAY-100635. Int J Neuropsychopharmacol, 4 (4): 399-408. [PMID:11806866]

2. Berg KA, Cropper JD, Niswender CM, Sanders-Bush E, Emeson RB, Clarke WP. (2001) RNA-editing of the 5-HT(2C) receptor alters agonist-receptor-effector coupling specificity. Br J Pharmacol, 134 (2): 386-92. [PMID:11564657]

3. 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]

4. Boddeke HW, Hoffman BJ, Palacios JM, Knot H, Hoyer D. (1993) Characterization of functional responses in A9 cells transfected with cloned rat 5-HT1C receptors. Naunyn Schmiedebergs Arch Pharmacol, 347 (2): 119-24. [PMID:8474532]

5. 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]

6. Brennan TJ, Seeley WW, Kilgard M, Schreiner CE, Tecott LH. (1997) Sound-induced seizures in serotonin 5-HT2c receptor mutant mice. Nat Genet, 16 (4): 387-90. [PMID:9241279]

7. 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]

8. 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]

9. Buckland PR, Hoogendoorn B, Guy CA, Smith SK, Coleman SL, O'Donovan MC. (2005) Low gene expression conferred by association of an allele of the 5-HT2C receptor gene with antipsychotic-induced weight gain. Am J Psychiatry, 162 (3): 613-5. [PMID:15741483]

10. Burns CM, Chu H, Rueter SM, Hutchinson LK, Canton H, Sanders-Bush E, Emeson RB. (1997) Regulation of serotonin-2C receptor G-protein coupling by RNA editing. Nature, 387 (6630): 303-8. [PMID:9153397]

11. 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]

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