Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTWJBZ5)

• DTT Name: 5-HT 2C receptor (HTR2C)
• Synonyms: Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
• Gene Name: HTR2C
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: 5HT2C_HUMAN
• TTD ID: T83813
• Sequence:
  MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
  VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
  PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
  ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
  LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
  QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
  SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
  EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
• Function: 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. G-protein coupled receptor for 5-hydroxytryptamine (serotonin).
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Gap junction (hsa04540)
  Serotonergic synapse (hsa04726)
  Inflammatory mediator regulation of TRP channels (hsa04750)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  Serotonin receptors (R-HSA-390666)

Molecular Interaction Atlas (MIA) of This DTT

6 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lorcaserin	DMG6OYJ	Obesity	5B81	Approved	[2]
Metergolin	DMJFP6G	Hyperprolactinaemia	5A60.1	Approved	[3]
Methysergide	DM1EF73	Migraine	8A80	Approved	[1]
Mirtazapine	DML53ZJ	Depression	6A70-6A7Z	Approved	[4]
Nefazodone	DM4ZS8M	Major depressive disorder	6A70.3	Approved	[5]
Tramadol	DMRQD04	Osteoarthritis	FA00-FA05	Approved	[6]

9 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Eltoprazine	DMW6C81	Attention deficit hyperactivity disorder	6A05.Z	Phase 3	[7]
M100907	DM7ZFBA	Sleep-wake disorder	7A00-7B2Z	Phase 3	[8]
SR46349B	DM1ODMR	Primary insomnia	7A00	Phase 3	[9]
ATHX-105	DM6ABD9	Obesity	5B81	Phase 2	[10]
Nuplazid	DMOJA5G	Alzheimer disease	8A20	Phase 2	[11]
PRX00933	DM1JNDV	Diabetic complication	5A2Y	Phase 2	[12]
Puerarin	DMJIMXH	Alcohol dependence	6C40.2	Phase 2	[13]
Vabicaserin	DM9GZW6	Psychotic disorder	6A20-6A25	Phase 2	[14]
Tedatioxetine	DMV5LGJ	Generalized anxiety disorder	6B00	Phase 1	[15]

39 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aryl piperazine derivative 10	DM5EGBY	N. A.	N. A.	Patented	[16]
Aryl piperazine derivative 8	DM7BRIT	N. A.	N. A.	Patented	[16]
Aryl piperazine derivative 9	DMLKNWF	N. A.	N. A.	Patented	[16]
Benzazepine derivative 1	DMA3BCU	N. A.	N. A.	Patented	[16]
Benzazepine derivative 2	DMKREJ2	N. A.	N. A.	Patented	[16]
Benzazepine derivative 3	DM3BGEN	N. A.	N. A.	Patented	[16]
Benzazepine derivative 4	DMM72LS	N. A.	N. A.	Patented	[16]
Benzazepine derivative 5	DM6XRDH	N. A.	N. A.	Patented	[16]
Benzazepine derivative 6	DMCGX5S	N. A.	N. A.	Patented	[16]
Chromene derivative 1	DM7SOZN	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 1	DMDOQKY	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 10	DMMZ8LE	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 11	DM5BF6H	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 12	DMOG72B	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 13	DME86DP	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 14	DMG1TIF	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 15	DMS3WEJ	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 2	DMDFL6B	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 3	DMG14E3	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 4	DMZVLH2	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 5	DMON5RD	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 6	DM3O7UG	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 7	DMS6HOG	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 8	DMBJH8N	N. A.	N. A.	Patented	[16]
Heteroaryl-azepine derivative 9	DMUZR3X	N. A.	N. A.	Patented	[16]
PMID26609882-Compound-58	DMD3T1Q	N. A.	N. A.	Patented	[16]
PMID26609882-Compound-83	DM6C45G	N. A.	N. A.	Patented	[16]
Pyrimidine derivative 23	DM5MLQU	N. A.	N. A.	Patented	[16]
Pyrimidine derivative 24	DMOQ726	N. A.	N. A.	Patented	[16]
Pyrimidine derivative 25	DM51MFS	N. A.	N. A.	Patented	[16]
Pyrimidine derivative 26	DM90WKN	N. A.	N. A.	Patented	[16]
Pyrimidine derivative 27	DMIQSDW	N. A.	N. A.	Patented	[16]
Pyrimidine derivative 28	DM1D2AS	N. A.	N. A.	Patented	[16]
Pyrimidine derivative 29	DMVOYJ8	N. A.	N. A.	Patented	[16]
Quinoline derivative 2	DMNO2BP	N. A.	N. A.	Patented	[16]
Tricyclic pyrrolidine derivative 1	DMGY3OR	N. A.	N. A.	Patented	[16]
Tricyclic pyrrolidine derivative 2	DMRD1XJ	N. A.	N. A.	Patented	[16]
Tricyclic pyrrolidine derivative 3	DMK2V6H	N. A.	N. A.	Patented	[16]
Tricyclic pyrrolidine derivative 4	DM0JYWT	N. A.	N. A.	Patented	[16]

10 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Deramciclane	DM8DUZT	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[17]
Ritanserin	DM0X36Y	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[18]
MCPP	DMIG5W8	Mood disorder	6A60-6E23	Discontinued in Phase 2	[19]
R-1065	DMHPV1D	Obesity	5B81	Discontinued in Phase 1	[20]
SB-247853	DMOVLDT	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 1	[21]
ICI-169369	DMQ0IOF	Anxiety disorder	6B00-6B0Z	Terminated	[22]
LY53857	DMY71LJ	N. A.	N. A.	Terminated	[23]
Org-37684	DMY3LXH	Anxiety disorder	6B00-6B0Z	Terminated	[24]
Ro-60-0175	DMZSQU8	N. A.	N. A.	Terminated	[25]
SDZ-SER-082	DMXHW91	Neurological disorder	6B60	Terminated	[26]

107 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(+/-)-nantenine	DM0L3GE	Discovery agent	N.A.	Investigative	[27]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine	DMIS39C	Discovery agent	N.A.	Investigative	[25]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine	DMW4ARM	Discovery agent	N.A.	Investigative	[25]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine	DM31SNW	Discovery agent	N.A.	Investigative	[25]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine	DMYALON	Discovery agent	N.A.	Investigative	[25]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine	DMTJI4F	Discovery agent	N.A.	Investigative	[28]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine	DMKZ4C6	Discovery agent	N.A.	Investigative	[29]
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine	DMTZDAJ	Discovery agent	N.A.	Investigative	[29]
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine	DMAU1M5	Discovery agent	N.A.	Investigative	[29]
(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine	DMS2DI9	Discovery agent	N.A.	Investigative	[29]
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine	DM0YELX	Discovery agent	N.A.	Investigative	[29]
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine	DMEIB8F	Discovery agent	N.A.	Investigative	[29]
1-((R)-2-aminopropyl)-1H-indazol-6-ol	DM74R0E	Discovery agent	N.A.	Investigative	[30]
1-((S)-2-aminopropyl)-1H-indazol-6-ol	DMU83KP	Discovery agent	N.A.	Investigative	[30]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol	DMRFJNC	Discovery agent	N.A.	Investigative	[30]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol	DM76JVB	Discovery agent	N.A.	Investigative	[30]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol	DMR2SXL	Discovery agent	N.A.	Investigative	[30]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol	DM8MNZG	Discovery agent	N.A.	Investigative	[30]
1-(2-aminoethyl)-1H-indazol-6-ol	DMKWO6A	Discovery agent	N.A.	Investigative	[30]
1-(2-Dimethylamino-ethyl)-1H-indol-4-ol	DMM3LET	Discovery agent	N.A.	Investigative	[31]
1-(piperazin-1-yl)isoquinoline	DMEP80C	Discovery agent	N.A.	Investigative	[32]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol	DMO7NXE	Discovery agent	N.A.	Investigative	[31]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine	DM1O0JD	Discovery agent	N.A.	Investigative	[30]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline	DML6HSE	Discovery agent	N.A.	Investigative	[32]
3-(2-Amino-propyl)-1H-indol-5-ol	DMQPNUM	Discovery agent	N.A.	Investigative	[30]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol	DMKYZGD	Discovery agent	N.A.	Investigative	[31]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol	DM32MIE	Discovery agent	N.A.	Investigative	[31]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol	DM9BTLC	Discovery agent	N.A.	Investigative	[31]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol	DMMJP9D	Discovery agent	N.A.	Investigative	[31]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol	DM7VJPX	Discovery agent	N.A.	Investigative	[31]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol	DM0O2ZB	Discovery agent	N.A.	Investigative	[31]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol	DMDOIJM	Discovery agent	N.A.	Investigative	[31]
3-Dimethylaminomethyl-1H-indol-4-ol	DMSJUOH	Discovery agent	N.A.	Investigative	[31]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[33]
4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine	DMTNVFZ	Discovery agent	N.A.	Investigative	[32]
4-(piperazin-1-yl)furo[3,2-c]pyridine	DMNM8VY	Discovery agent	N.A.	Investigative	[32]
4-(piperazin-1-yl)thieno[2,3-d]pyrimidine	DMNU2RM	Discovery agent	N.A.	Investigative	[32]
4-(piperazin-1-yl)thieno[3,2-c]pyridine	DMJGTS7	Discovery agent	N.A.	Investigative	[32]
4-(piperazin-1-yl)thieno[3,2-d]pyrimidine	DM2KAG5	Discovery agent	N.A.	Investigative	[32]
5,6-dichloro-3,4-dihydroquinazolin-2-amine	DMN1S35	Discovery agent	N.A.	Investigative	[34]
5-chloro-3,4-dihydroquinazolin-2-amine	DMKEFJ0	Discovery agent	N.A.	Investigative	[34]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine	DMGDTNI	Discovery agent	N.A.	Investigative	[34]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine	DM7FZU2	Discovery agent	N.A.	Investigative	[34]
5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide	DMZ5MDY	Discovery agent	N.A.	Investigative	[29]
5-CT	DM260KD	Discovery agent	N.A.	Investigative	[35]
5-MEO-DMT	DMG0EL7	Discovery agent	N.A.	Investigative	[30]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine	DM592FB	Discovery agent	N.A.	Investigative	[36]
6-(piperazin-1-yl)-9-propyl-9H-purine	DMUNWJR	Discovery agent	N.A.	Investigative	[32]
6-bromo-2'-de-N-methylaplysinopsin	DM39VT6	Discovery agent	N.A.	Investigative	[37]
6-bromo-8-(piperazin-1-yl)imidazo[1,2-a]pyrazine	DMZJ6M8	Discovery agent	N.A.	Investigative	[32]
6-bromoaplysinopsin	DMQGB70	Discovery agent	N.A.	Investigative	[37]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide	DMUY9TF	Discovery agent	N.A.	Investigative	[29]
6-methyl-4-(piperazin-1-yl)furo[2,3-d]pyrimidine	DM1LW62	Discovery agent	N.A.	Investigative	[32]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine	DMIMLUO	Discovery agent	N.A.	Investigative	[36]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine	DMVZA27	Discovery agent	N.A.	Investigative	[36]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine	DMK6U2V	Discovery agent	N.A.	Investigative	[34]
AL-37350A	DMRJ2GK	Discovery agent	N.A.	Investigative	[38]
alpha-methyl-5-HT	DMCAYXF	Discovery agent	N.A.	Investigative	[39]
Aplysinopsin	DMUPL3J	Discovery agent	N.A.	Investigative	[29]
BARETTIN	DMU3D2O	Discovery agent	N.A.	Investigative	[40]
BRL-15572	DMM61Y2	Discovery agent	N.A.	Investigative	[41]
BVT 933	DM8N7BA	Obesity	5B81	Investigative	[42]
BW723C86	DME15JU	Discovery agent	N.A.	Investigative	[43]
CHLOROPHENYLPIPERAZINE	DMOA8L2	Discovery agent	N.A.	Investigative	[44]
CP-809101	DM3M1LA	Neurological disorder	6B60	Investigative	[45]
CSC-500297	DM6K123	Obesity	5B81	Investigative	[45]
cyamemazine	DMZ6YPV	Discovery agent	N.A.	Investigative	[46]
Cyclo[(6-bromotryptophan)arginine]	DM9ZCWV	Discovery agent	N.A.	Investigative	[40]
EGIS-7625	DMLK4X5	Discovery agent	N.A.	Investigative	[47]
FR260010	DMSQ6CV	Discovery agent	N.A.	Investigative	[48]
LY334362	DMFHT3U	Discovery agent	N.A.	Investigative	[49]
m-chlorophenylpiperazine	DMM1J2D	Discovery agent	N.A.	Investigative	[50]
METHYLENEDIOXYMETHAMPHETAMINE	DMYVU47	Discovery agent	N.A.	Investigative	[51]
MK-212	DMYO8T6	Discovery agent	N.A.	Investigative	[52]
MPDT	DMYX31S	Discovery agent	N.A.	Investigative	[53]
N-(6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide	DM2E5OX	Discovery agent	N.A.	Investigative	[54]
N-(pyridin-3-yl)indoline-1-carboxamide	DMTHJL4	Discovery agent	N.A.	Investigative	[29]
N-3'-ethylaplysinopsin	DMWZTKD	Discovery agent	N.A.	Investigative	[37]
norfluoxetine	DMKNUP3	Discovery agent	N.A.	Investigative	[55]
OCTOCLOTHEPIN	DM0UADK	Discovery agent	N.A.	Investigative	[56]
Org 12962	DM8JUBG	Discovery agent	N.A.	Investigative	[3]
PG-01037	DM2TP4Q	Discovery agent	N.A.	Investigative	[57]
RS-102,221	DMHDYBN	Discovery agent	N.A.	Investigative	[58]
SB 204741	DM3LQF4	Discovery agent	N.A.	Investigative	[3]
SB 215505	DMCM4LT	Discovery agent	N.A.	Investigative	[59]
SB 216641	DMB3R4Z	Discovery agent	N.A.	Investigative	[41]
SB 221284	DM8DVY2	Discovery agent	N.A.	Investigative	[3]
SB 228357	DMKA8R4	Discovery agent	N.A.	Investigative	[60]
SB 242084	DMISBDC	Discovery agent	N.A.	Investigative	[61]
SB 243213	DMAFWRT	Discovery agent	N.A.	Investigative	[62]
SB-271046	DM5VJAF	Discovery agent	N.A.	Investigative	[63]
SEROTONIN	DMOFCRY	Discovery agent	N.A.	Investigative	[40]
spiramide	DM5KNMD	Discovery agent	N.A.	Investigative	[3]
TFMPP	DMAC8TP	Discovery agent	N.A.	Investigative	[35]
TQ-1017	DMEF32D	Pain	MG30-MG3Z	Investigative	[64]
VER-2692	DM5WAM8	Discovery agent	N.A.	Investigative	[65]
VER-3323	DM7O2K1	Discovery agent	N.A.	Investigative	[66]
VER-5384	DMC2EO9	Discovery agent	N.A.	Investigative	[66]
VER-5593	DMZ2V0A	Discovery agent	N.A.	Investigative	[66]
WAY-163909	DMNMO4Q	Discovery agent	N.A.	Investigative	[67]
WAY-208466	DM9K2LU	Discovery agent	N.A.	Investigative	[68]
WAY-466	DMMOH51	Discovery agent	N.A.	Investigative	[69]
YM-348	DM38F9T	Discovery agent	N.A.	Investigative	[36]
[125I]DOI	DMQUY08	Discovery agent	N.A.	Investigative	[39]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine	DMDIH96	Discovery agent	N.A.	Investigative	[31]
[3H]LSD	DM0YJHS	Discovery agent	N.A.	Investigative	[45]
[3H]mesulergine	DM8K6VF	Discovery agent	N.A.	Investigative	[39]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Schizophrenia	6A20	Pre-frontal cortex	1.02E-02	-0.45	-0.37
Schizophrenia	6A20	Superior temporal cortex	2.27E-01	0.27	0.6
Major depressive disorder	6A20	Pre-frontal cortex	8.66E-01	-0.13	-0.12

References

• [1] Spinal serotonin receptor activation modulates the exercise ventilatory response with increased dead space in goats. Respir Physiol Neurobiol. 2008 May 31;161(3):230-8.
• [2] Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
• [3] Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.
• [4] Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulatio... Mol Pharmacol. 2008 Mar;73(3):748-57.
• [5] Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies. Therapie. 2005 Sep-Oct;60(5):441-60.
• [6] The inhibitory effects of tramadol on 5-hydroxytryptamine type 2C receptors expressed in Xenopus oocytes. Anesth Analg. 2004 May;98(5):1401-6, table of contents.
• [7] Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
• [8] Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists ... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12.
• [9] SR46349-B, a 5-HT(2A/2C) receptor antagonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. Neuropsychopharmacology. 2002 Sep;27(3):430-41.
• [10] Pharmacological targeting of the serotonergic system for the treatment of obesity. J Physiol. 2009 January 1; 587(Pt 1): 49-60.
• [11] The neuropharmacology of sleep paralysis hallucinations: serotonin 2A activation and a novel therapeutic drug. Psychopharmacology (Berl). 2018 Nov;235(11):3083-3091.
• [12] 2011 Pipeline of Proximagen Group plc.
• [13] NPI-031G (puerarin) reduces anxiogenic effects of alcohol withdrawal or benzodiazepine inverse or 5-HT2C agonists. Pharmacol Biochem Behav. 2003 Jun;75(3):619-25.
• [14] Prediction of Efficacy of Vabicaserin, a 5-HT2C Agonist, for the Treatment of Schizophrenia Using a Quantitative Systems Pharmacology Model.CPT Pharmacometrics Syst Pharmacol.2014 Apr 23;3:e111.
• [15] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [16] Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.
• [17] Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation. Psychopharmacology (Berl). 1998 Mar;136(2):99-104.
• [18] Characterization of contractile 5-hydroxytryptamine receptor subtypes in the in situ autoperfused kidney in the anaesthetized rat. Eur J Pharmacol. 2008 Sep 11;592(1-3):133-7.
• [19] mCPP-induced hyperactivity in 5-HT2C receptor mutant mice is mediated by activation of multiple 5-HT receptor subtypes. Neuropharmacology. 2004 Apr;46(5):663-71.
• [20] Antiaversive effects of 5HT2C receptor agonists and fluoxetine in a model of panic-like anxiety in rats. Eur Neuropsychopharmacol. 1998 Aug;8(3):161-8.
• [21] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016366)
• [22] Serotonin 5-HT(2A) receptor antagonists in the treatment of insomnia: present status and future prospects.Drugs Today (Barc).2010 Mar;46(3):183-93.
• [23] The 5-hydroxytryptamine2A receptor is involved in (+)-norfenfluramine-induced arterial contraction and blood pressure increase in deoxycorticostero... J Pharmacol Exp Ther. 2007 May;321(2):485-91.
• [24] Role of 5-hT2C receptors in the hypophagic effect of m-CPP, ORG 37684 and CP-94,253 in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2002 Apr;26(3):441-9.
• [25] Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor a... Bioorg Med Chem. 2008 Feb 15;16(4):1966-82.
• [26] Effect of the activation of central 5-HT2C receptors by the 5-HT2C agonist mCPP on blood pressure and heart rate in rats. Brain Res. 2005 Apr 8;1040(1-2):64-72.
• [27] Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
• [28] 2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands. Bioorg Med Chem Lett. 2007 May 1;17(9):2643-8.
• [29] Synthesis and structure-affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes. Bioorg Med Chem. 2010 Jul 1;18(13):4783-92.
• [30] 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28.
• [31] SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.
• [32] Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity. Bioorg Med Chem Lett. 2010 Jan 1;20(1):266-71.
• [33] Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
• [34] Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.
• [35] Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors. Synapse. 2000 Feb;35(2):144-50.
• [36] Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists. Bioorg Med Chem. 2008 Mar 15;16(6):3309-20.
• [37] New antiinfective and human 5-HT2 receptor binding natural and semisynthetic compounds from the Jamaican sponge Smenospongia aurea. J Nat Prod. 2002 Apr;65(4):476-80.
• [38] A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole. J Med Chem. 2003 Sep 11;46(19):4188-95.
• [39] High-affinity agonist binding correlates with efficacy (intrinsic activity) at the human serotonin 5-HT2A and 5-HT2C receptors: evidence favoring the ternary complex and two-state models of agonist action. J Neurochem. 1999 May;72(5):2127-34.
• [40] Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. J Nat Prod. 2006 Oct;69(10):1421-4.
• [41] SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.
• [42] Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.
• [43] Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. Br J Pharmacol. 2003 Sep;140(2):277-84.
• [44] Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33.
• [45] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 8).
• [46] Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40.
• [47] Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther. 2003 Sep-Nov;17(5-6):427-34.
• [48] Anxiolytic activity of a novel potent serotonin 5-HT2C receptor antagonist FR260010: a comparison with diazepam and buspirone. Eur J Pharmacol. 2006 Dec 28;553(1-3):171-84.
• [49] A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines. Life Sci. 1996;59(15):1259-68.
• [50] Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist. Eur J Pharmacol. 2004 Jan 1;483(1):37-43.
• [51] The origin of MDMA (ecstasy) revisited: the true story reconstructed from the original documents. Addiction. 2006 Sep;101(9):1241-5.
• [52] [Agonists of 5HT2C-receptors SCH 23390 and MK 212 incresase the force of rat aorta contraction in the presence of vasopressin and angiotensin II].Patol Fiziol Eksp Ter.2014 Oct-Dec;(4):17-29.
• [53] 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
• [54] Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3844-7.
• [55] Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation. 2000 Dec 5;102(23):2836-41.
• [56] Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for (1)-adre... J Med Chem. 2010 Oct 14;53(19):7021-34.
• [57] Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3... J Med Chem. 2007 Aug 23;50(17):4135-46.
• [58] cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
• [59] Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4.
• [60] 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. 2000 Mar 23;43(6):1123-34.
• [61] SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
• [62] SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology. 2001 Aug;41(2):186-99.
• [63] Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43.
• [64] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [65] Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2006 Feb;16(3):677-80.
• [66] Indoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.
• [67] WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine 2C receptor-sele... J Pharmacol Exp Ther. 2005 May;313(2):862-9.
• [68] Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. Bioorg Med Chem. 2009 Jul 15;17(14):5153-63.
• [69] Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. J Med Chem. 2005 Jan 27;48(2):353-6.