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5-HT2C receptor

Family: 5-Hydroxytryptamine receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
Biologically Significant Variants
General Comments
References
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 (serotonin) receptor 2C, G protein-coupled 67
Mouse 7 459 X D-F4 Htr2c 5-hydroxytryptamine (serotonin) receptor 2C 22,71
Rat 7 460 Xq34-q35.1 Htr2c 5-hydroxytryptamine (serotonin) receptor 2C, G protein-coupled 4
Previous and Unofficial Names
Names References
5-HT1C 52
HTR1C
5-HT2C
5-hydroxytryptamine (serotonin) receptor 2C
5-HTR2C
5HT-1C
5-HT-1C
5-HT1C
5-hydroxytryptamine receptor 1C
5-hydroxytryptamine receptor 2C
serotonin 1c receptor
serotonin receptor 2C
5-HT2C receptor
5-HT2cR
5HT1c
SR1
Database Links
ChEMBL Target 108 (Hs), 11864 (Mm), 12689 (Rn)
DrugBank Target 590 (Hs)
Ensembl ENSG00000147246 (Hs), ENSMUSG00000041380 (Mm), ENSRNOG00000030877 (Rn)
Entrez Gene 3358 (Hs), 15560 (Mm), 25187 (Rn)
GeneCards HTR2C (Hs)
GenitoUrinary Development Molecular Anatomy Project Htr2c (Mm)
HomoloGene 20242 (Hs)
Human Protein Reference Database 02429 (Hs)
InterPro P28335 (Hs), P34968 (Mm), P08909 (Rn)
KEGG Gene hsa:3358 (Hs), mmu:15560 (Mm), rno:25187 (Rn)
OMIM 312861 (Hs)
PharmGKB Gene PA194 (Hs)
PhosphoSitePlus P28335 (Hs), P34968 (Mm), P08909 (Rn)
Protein Ontology (PRO) PRO:000001168 (Hs)
RefSeq Nucleotide NM_000868 (Hs), NM_008312 (Mm), NM_012765 (Rn)
RefSeq Protein NP_000859 (Hs), NP_032338 (Mm), NP_036897 (Rn)
TreeFam ENSG00000147246 (Hs), ENSMUSG00000041380 (Mm), ENSRNOG00000030877 (Rn)
UniGene Hs. 149037 (Hs)
UniProt P28335 (Hs), P34968 (Mm), P08909 (Rn)
Wikipedia 5-HT2C receptor
5-Hydroxytryptamine receptors
Search for 3D structures on the PDB
Search by keyword: 5-Hydroxytryptamine receptors 5-HT2C receptor Search by accession number: P08909, P28335, P34968
Natural/Endogenous Ligand(s)
5-HT
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]LSD Hs Agonist - -
[125I]DOI Rn Full agonist 9.1 pKd 3
[125I]DOI Hs Full agonist 8.7 – 9.0 pKd 20
YM348 Hs Full agonist 9.0 pKi 35
ergotamine Hs Partial agonist 8.7 pKi 36
methysergide Rn Partial agonist 8.7 pKi 63
(+)-LSD Hs Full agonist 8.2 – 9.0 pKi 20,36
AL-37350A Hs Full agonist 8.5 pKi 41
(R)-DOI Hs Full agonist 8.4 pKi 41
LSD Hs Full agonist 8.2 – 8.6 pKi 19
methylergonovine Hs Full agonist 8.3 pKi 36
VER-3323 Hs Full agonist 8.2 pKi 36
(+)-DOI Hs Full agonist 8.1 pKi 36
lisuride Hs Partial agonist 7.9 – 8.3 pKi 19-20,45
org 37684 Hs Full agonist 8.1 pKi 36
(R)-DOI Hs Full agonist 7.4 – 8.7 pKi 20,36,48
Ro 60-0175 Hs Full agonist 7.7 – 8.2 pKi 35-36
DOI Hs Full agonist 7.2 – 8.6 pKi 19,48,64
ergotamine Rn Partial agonist 7.9 pKi 63
methylergonovine Rn Full agonist 7.9 pKi 63
DOB Hs Full agonist 6.8 – 8.9 pKi 19,36,48
lorcaserin Hs Full agonist 7.8 pKi 68
org 12962 Hs Full agonist 7.8 pKi 36
α-methyl-5-HT Hs Full agonist 6.9 – 8.6 pKi 20,36
5-HT Hs Full agonist 6.8 – 8.6 pKi 19-20,35-36,41
S 16924 Hs Full agonist 7.7 pKi 43
aripiprazole Hs Full agonist 7.6 pKi 38
m-CPP Hs Partial agonist 6.5 – 8.5 pKi 19-20,35-36,48,64
WAY-163909 Hs Full agonist 6.7 – 8.0 pKi 18
5-HT Rn Full agonist 6.7 – 7.9 pKi 30,63
5-MeOT Hs Full agonist 6.7 – 7.8 pKi 19
m-CPP Rn Partial agonist 7.2 pKi 63
TFMPP Hs Full agonist 6.5 – 7.8 pKi 19,36
BW723C86 Hs Full agonist 6.9 – 7.1 pKi 36,64
GR-127935 Hs Partial agonist 7.0 pKi 57
RU 24969 Hs Full agonist 6.8 pKi 36
SB 216641 Hs Partial agonist 6.8 pKi 57
quipazine Hs Full agonist 5.9 – 7.3 pKi 19-20,36
5-MeO-DMT Hs Full agonist 6.2 – 7.0 pKi 20
DOB Rn Full agonist 6.6 pKi 30
oxymetazoline Hs Full agonist 6.3 – 6.8 pKi 20
pergolide Hs Partial agonist 6.5 pKi 45
tryptamine Hs Full agonist 5.6 – 7.2 pKi 19,36
5-MeOT Rn Full agonist 6.3 pKi 30
MK-212 Hs Full agonist 5.6 – 7.0 pKi 19,36,64
BRL-15572 Hs Partial agonist 6.2 pKi 57
cabergoline Hs Full agonist 6.2 pKi 45
bromocriptine Hs Partial agonist 6.1 pKi 45
5-CT Hs Full agonist 5.2 – 6.7 pKi 19,36
8-OH-DPAT Hs Full agonist 5.6 pKi 36
CGS-12066 Hs Full agonist 5.6 pKi 36
LY344864 Hs Full agonist 5.5 pKi 53
SL65.0155 Hs Partial agonist 5.3 pKi 47
quinpirole Hs Full agonist 5.0 – 5.5 pKi 36,45
lorcaserin Hs Full agonist 8.1 pEC50 68
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 9.3 – 8.7 pKd 20,60
methysergide Rn Antagonist 9.3 pKi 30
mesulergine Rn Inverse agonist 9.2 pKi 30
mianserin Rn Antagonist 8.8 – 9.4 pKi 30,59
sertindole Hs Inverse agonist 9.0 – 9.2 pKi 32,38
SB 228357 Hs Antagonist 9.0 – 9.1 pKi 7,62
FR260010 Hs Antagonist 9.0 pKi 29
mesulergine Hs Inverse agonist 8.7 – 9.3 pKi 28,36-37
ritanserin Hs Antagonist 8.2 – 9.6 pKi 36
methysergide Hs Antagonist 8.6 – 9.1 pKi 19,36
metergoline Hs Inverse agonist 8.8 pKi 36
mianserin Hs Inverse agonist 8.3 – 9.2 pKi 20,36,46
amoxapine Rn Antagonist 8.7 pKi 59
SB 221284 Hs Antagonist 8.7 pKi 36
SB 242084 Hs Antagonist 8.2 – 9.0 pKi 34,36
zotepine Hs Inverse agonist 8.6 pKi 32
amitriptyline Rn Antagonist 8.4 pKi 59
methiothepin Hs Inverse agonist 8.4 pKi 36
RS-102221 Rn Antagonist 8.4 pKi 5
RS-102221 Hs Antagonist 8.3 – 8.4 pKi 5,36
tiospirone Hs Inverse agonist 8.3 pKi 32
olanzapine Hs Inverse agonist 8.1 – 8.2 pKi 32,38
ziprasidone Hs Inverse agonist 7.9 – 8.4 pKi 32,38
SDZ SER-082 Hs Antagonist 8.1 pKi 36
clozapine Hs Inverse agonist 7.4 – 8.7 pKi 20,32,36,38,43,69
cyamemazine Hs Antagonist 7.9 pKi 28
loxapine Hs Inverse agonist 7.8 – 8.0 pKi 32,38
chlorpromazine Hs Antagonist 7.6 – 8.2 pKi 32,38
SB 206553 Hs Antagonist 7.8 – 7.9 pKi 33,36
EGIS-7625 Hs Antagonist 7.7 pKi 37
SB 215505 Hs Antagonist 7.7 pKi 62
MDL-100,907 Hs Antagonist 7.5 – 7.7 pKi 36,62
risperidone Hs Inverse agonist 7.5 – 7.6 pKi 32,38
sarpogrelate Hs Antagonist 7.4 pKi 60
xanomeline Hs Antagonist 7.4 pKi 70
fluoxetine Rn Antagonist 7.3 pKi 63
terguride Hs Antagonist 7.3 pKi 45
thioridazine Hs Antagonist 7.2 – 7.3 pKi 32,38
ketanserin Hs Antagonist 6.8 – 7.5 pKi 8,20,36,60
S33084 Hs Antagonist 7.1 pKi 44
apomorphine Hs Antagonist 7.0 pKi 45
LY334362 Hs Antagonist 7.0 pKi 8
perphenazine Hs Antagonist 6.9 pKi 38
MDL-11,939 Hs Antagonist 6.6 pKi 36
trazodone Hs Antagonist 6.6 pKi 36
trazodone Rn Antagonist 6.4 – 6.7 pKi 59,63
norfluoxetine Rn Antagonist 6.5 pKi 63
roxindole Hs Antagonist 6.5 pKi 45
trifluoperazine Hs Antagonist 6.4 pKi 38
RS-127445 Hs Antagonist 6.3 pKi 36
agomelatine Hs Antagonist 6.2 pKi 42
MPDT Rn Antagonist 6.2 pKi 27
SB 224289 Hs Antagonist 6.2 pKi 65
duloxetine Hs Antagonist 6.0 pKi 11
spiperone Hs Antagonist 5.6 – 6.2 pKi 20,32,36
AMI-193 Hs Antagonist 5.8 pKi 36
SB 224289 Hs Antagonist 5.7 pKi 36
SB 204741 Hs Antagonist 5.6 pKi 36
AC-90179 Hs Inverse agonist 5.5 pKi 53
SB 243213 Hs Antagonist 9.0 pEC50 7
View species-specific antagonist tables

Explore drug-target interactions for this set of compounds using iPHACE

Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  16-17,39
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  39
Tissue Distribution
Resting lymphocytes.
Species:  Human
Technique:  RT-PCR.
References:  40
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:  55
Medulla oblongata and grey matter of the spinal cord.
Species:  Rat
Technique:  in situ hybridisation.
References:  24
Lumbar dorsal root ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  54
GABAergic cells of the anterior raphe nuclei.
Species:  Rat
Technique:  Double in situ hybridisation.
References:  66
Expression Datasets

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

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Functional Assays
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:  39
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:  39
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:  39
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:  56
Measurement of phosphatidylinositol turnover in rat choroid plexus.
Species:  Rat
Tissue:  Choroid plexus.
Response measured:  Stimulation of phosphatidylinositol turnover.
References:  16
Physiological Functions
Analgesia.
Species:  Mouse
Tissue:  In vivo.
References:  13
Anxiety.
Species:  Rat
Tissue:  In vivo.
References:  1,26
Hyperlocomotion.
Species:  Rat
Tissue:  In vivo.
References:  23
Decrease in food intake.
Species:  Rat
Tissue:  In vivo.
References:  23
Regulation of sleep.
Species:  Mouse
Tissue:  In vivo.
References:  25
Regulation of the response to repeated stress.
Species:  Mouse
Tissue:  In vivo.
References:  14
Physiological Consequences of Altering Gene Expression
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:  51
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:  25
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:  14
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:  50
Phenotypes, Alleles and Disease Models Mouse data from MGI

Click here to show/hide data

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
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.
Type:  Single nucleotide polymorphism.
Species:  Human
References:  9
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.
Type:  RNA editing.
Species:  Human
References:  2,10,21,31-32,49,58,61
General Comments
A non-functional short (248aa) splice-variant of the h 5-HT2C receptor has been described [12].

REFERENCES

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To cite this database page, please use the following:

Rodrigo Andrade, Nicholas M. Barnes, Gordon Baxter, Joel Bockaert, Theresa Branchek, Marlene L. Cohen, Aline Dumuis, Richard M. Eglen, Manfred Göthert, Mark Hamblin, Michel Hamon, Paul R. Hartig, René Hen, Katharine Herrick-Davis, Rebecca Hills, Daniel Hoyer, Patrick P. A. Humphrey, Klaus Peter Latté, Luc Maroteaux, Graeme R. Martin, Derek N. Middlemiss, Ewan Mylecharane, Stephen J. Peroutka, Pramod R. Saxena, Andrew Sleight, Carlos M. Villalon, Frank Yocca.
5-Hydroxytryptamine receptors: 5-HT2C receptor. Last modified on 12/02/2013. Accessed on 20/06/2013. IUPHAR database (IUPHAR-DB), http://iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=8.


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