Target Information

Target General Infomation
Target ID
T83813
Former ID
TTDS00105
Target Name
5-hydroxytryptamine 2C receptor
Gene Name
HTR2C
Synonyms
5-HT-2C; 5-HT2C receptor; 5HT-1C; Serotonin receptor; Serotonin receptor 2C; HTR2C
Target Type
Successful
Disease Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Aggressive non-hodgkin's lymphoma [ICD9: 200, 201, 202, 202.8, 208.9; ICD10: C81, C81-C86, C82-C85, C91-C95]
Depression [ICD9: 311; ICD10: F30-F39]
Drug abuse [ICD9: 303-304; ICD10: F10-F19]
Generalized anxiety disorder; Major depressive disorder [ICD9:300, 300.02, 311, 296.2, 296.3, 710.0; ICD10: F32, F40-F42, F41.1, F33, M32]
Migraine headaches [ICD9: 346; ICD10: G43]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Mood disorder [ICD10: F30-F39]
Metabolic disorders [ICD9: 270-279; ICD10: E70-E89]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Obesity [ICD9: 278; ICD10: E66]
Obesity; Diabetes [ICD9: 250, 278; ICD10: E08-E13, E66]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29]
Sleep initiation and maintenance disorders; Primary insomnia; Schizophrenia [ICD9: 295, 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F20, F51.0, G47.0]
Unspecified [ICD code not available]
Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1- 2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis.
BioChemical Class
GPCR rhodopsin
Target Validation
T83813
UniProt ID
P28335
Sequence
MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
Drugs and Mode of Action
Drug(s) Lorcaserin Drug Info Approved Obesity [1], [2]
Methysergide Drug Info Approved Migraine headaches [3], [4]
Mirtazapine Drug Info Approved Depression [5], [6]
Nefazodone Drug Info Approved Major depressive disorder [7]
Tramadol Drug Info Approved Pain [8], [9]
SR46349B Drug Info Phase 3 Sleep initiation and maintenance disorders; Primary insomnia; Schizophrenia [10]
VOLINANSERIN Drug Info Phase 3 Discovery agent [11], [12]
ATHX-105 Drug Info Phase 2 Obesity [13]
Eltoprazine Drug Info Phase 2 Aggressive non-hodgkin's lymphoma [14]
PRX00933 Drug Info Phase 2 Obesity; Diabetes [15]
Puerarin Drug Info Phase 2 Alcohol use disorders [16]
Vabicaserin Drug Info Phase 2 Psychotic disorders [17]
Lorcaserin Drug Info Phase 1 Drug abuse [18], [2]
Tedatioxetine Drug Info Phase 1 Generalized anxiety disorder; Major depressive disorder [19]
Nefazodone Drug Info Withdrawn from market Depression [5], [20]
Deramciclane Drug Info Discontinued in Phase 3 Anxiety disorder [21], [22]
Ritanserin Drug Info Discontinued in Phase 3 Anxiety disorder [23], [24]
MCPP Drug Info Discontinued in Phase 2 Mood disorder [25]
R-1065 Drug Info Discontinued in Phase 1 Obesity [26]
SB-247853 Drug Info Discontinued in Phase 1 Anxiety disorder [27]
ICI-169369 Drug Info Terminated Anxiety disorder [28], [29]
LY53857 Drug Info Terminated Discovery agent [30], [31]
Org-37684 Drug Info Terminated Anxiety disorder [32], [33]
Ro-60-0175 Drug Info Terminated Discovery agent [34], [35]
SDZ-SER-082 Drug Info Terminated Neurological disease [36], [37]
Agonist (+)-LSD Drug Info [38]
3,4-Methylenedioxymethamphetamine Drug Info [39]
5-CT Drug Info [40]
5-HT 2c receptor agonists (obesity/schizophrenia), Galenea Drug Info [41]
5-HT2c agonists (metabolic disorders), Boehringer Drug Info [41]
AL-37350A Drug Info [42]
alpha-methyl-5-HT Drug Info [38]
ATHX-105 Drug Info [43]
BRL-15572 Drug Info [44]
BW723C86 Drug Info [45]
CP-809101 Drug Info [41]
CSC-500297 Drug Info [41]
Lorcaserin Drug Info [18], [46]
m-chlorophenylpiperazine Drug Info [47]
MCPP Drug Info [48], [7]
Org 12962 Drug Info [49]
Org-37684 Drug Info [50]
PRX00933 Drug Info [15]
R-1065 Drug Info [51]
SB 216641 Drug Info [44]
SB 243213 Drug Info [52]
SB-247853 Drug Info [53], [7]
TFMPP Drug Info [40]
TQ-1017 Drug Info [7]
WAY-163909 Drug Info [54]
[125I]DOI Drug Info [38]
[3H]LSD Drug Info [41]
Inhibitor (+/-)-nantenine Drug Info [55]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine Drug Info [56]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info [56]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info [56]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info [56]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info [57]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine Drug Info [58]
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine Drug Info [58]
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine Drug Info [58]
(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine Drug Info [58]
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine Drug Info [58]
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine Drug Info [58]
1-((R)-2-aminopropyl)-1H-indazol-6-ol Drug Info [59]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [59]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info [59]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info [59]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info [59]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info [59]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info [59]
1-(2-Dimethylamino-ethyl)-1H-indol-4-ol Drug Info [60]
1-(piperazin-1-yl)isoquinoline Drug Info [61]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info [60]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info [59]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline Drug Info [61]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info [59]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info [60]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info [60]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol Drug Info [60]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info [60]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol Drug Info [60]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol Drug Info [60]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info [60]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info [60]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [62]
4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Drug Info [61]
4-(piperazin-1-yl)furo[3,2-c]pyridine Drug Info [61]
4-(piperazin-1-yl)thieno[2,3-d]pyrimidine Drug Info [61]
4-(piperazin-1-yl)thieno[3,2-c]pyridine Drug Info [61]
4-(piperazin-1-yl)thieno[3,2-d]pyrimidine Drug Info [61]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [63]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info [63]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info [63]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [63]
5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [58]
5-MEO-DMT Drug Info [59]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info [64]
6-(piperazin-1-yl)-9-propyl-9H-purine Drug Info [61]
6-bromo-2'-de-N-methylaplysinopsin Drug Info [65]
6-bromo-8-(piperazin-1-yl)imidazo[1,2-a]pyrazine Drug Info [61]
6-bromoaplysinopsin Drug Info [65]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [58]
6-methyl-4-(piperazin-1-yl)furo[2,3-d]pyrimidine Drug Info [61]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine Drug Info [64]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine Drug Info [64]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [63]
APLYSINOPSIN Drug Info [58]
BARETTIN Drug Info [66]
CHLOROPHENYLPIPERAZINE Drug Info [67]
Cyclo[(6-bromotryptophan)arginine] Drug Info [66]
N-(6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide Drug Info [68]
N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [58]
N-3'-ethylaplysinopsin Drug Info [65]
OCTOCLOTHEPIN Drug Info [69]
PG-01037 Drug Info [70]
Ro-60-0175 Drug Info [56]
RS-102,221 Drug Info [71]
SB-271046 Drug Info [72]
SEROTONIN Drug Info [66]
VER-2692 Drug Info [73]
VER-3323 Drug Info [74]
VER-5384 Drug Info [74]
VER-5593 Drug Info [74]
VOLINANSERIN Drug Info [75]
WAY-208466 Drug Info [76]
WAY-466 Drug Info [77]
YM-348 Drug Info [64]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info [60]
Antagonist BVT 933 Drug Info [78]
cyamemazine Drug Info [79]
EGIS-7625 Drug Info [80]
Eltoprazine Drug Info [81]
FR260010 Drug Info [82]
LY334362 Drug Info [83]
LY53857 Drug Info [84], [85], [86], [87]
metergoline Drug Info [49]
Methysergide Drug Info [88], [89], [90], [87]
Mirtazapine Drug Info [91], [92]
MPDT Drug Info [93]
Nefazodone Drug Info [91], [94]
norfluoxetine Drug Info [95]
Ritanserin Drug Info [96], [97], [98], [99]
SB 204741 Drug Info [49]
SB 215505 Drug Info [100]
SB 221284 Drug Info [49]
SB 228357 Drug Info [101]
SB 242084 Drug Info [102]
spiramide Drug Info [49]
[3H]mesulergine Drug Info [38]
Modulator Deramciclane Drug Info [103]
ICI-169369 Drug Info
MK-212 Drug Info
Puerarin Drug Info
SDZ-SER-082 Drug Info
SR46349B Drug Info
Tedatioxetine Drug Info [104]
Tramadol Drug Info [105]
Vabicaserin Drug Info [106]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Gap junction
Serotonergic synapse
Inflammatory mediator regulation of TRP channels
PANTHER Pathway 5HT2 type receptor mediated signaling pathway
Reactome Serotonin receptors
G alpha (q) signalling events
WikiPathways Serotonin Receptor 2 and ELK-SRF/GATA4 signaling
Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
References
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REF 3FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 012516.
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