Target Information

Target General Information

Target ID

T83813 (Former ID: TTDS00105)

Target 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

Target Type

Successful target

[1]

Disease

[+] 5 Target-related Diseases

Depression [ICD-11: 6A70-6A7Z]

Migraine [ICD-11: 8A80]

Obesity [ICD-11: 5B80-5B81]

Pain [ICD-11: MG30-MG3Z]

Pituitary gland disorder [ICD-11: 5A60-5A61]

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).

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BioChemical Class

GPCR rhodopsin

UniProt ID

5HT2C_HUMAN

Sequence

MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

HIT2.0 ID

T83COK

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 6 Approved Drugs

Lorcaserin

Drug Info

Approved

Obesity

[2], [3]

Metergolin

Drug Info

Approved

Hyperprolactinaemia

[4]

Methysergide

Drug Info

Approved

Migraine

[5], [6]

Mirtazapine

Drug Info

Approved

Depression

[7], [8]

Nefazodone

Drug Info

Approved

Major depressive disorder

[4]

Tramadol

Drug Info

Approved

Pain

[9], [10]

Clinical Trial Drug(s)

[+] 9 Clinical Trial Drugs

Eltoprazine

Drug Info

Phase 3

Attention deficit hyperactivity disorder

[11]

M100907

Drug Info

Phase 3

Sleep-wake disorder

[12]

SR46349B

Drug Info

Phase 3

Schizophrenia

[13]

ATHX-105

Drug Info

Phase 2

Obesity

[14]

Nuplazid

Drug Info

Phase 2

Alzheimer disease

[15]

PRX00933

Drug Info

Phase 2

Diabetic complication

[16]

Puerarin

Drug Info

Phase 2

Alcohol dependence

[17]

Vabicaserin

Drug Info

Phase 2

Psychotic disorder

[18]

Tedatioxetine

Drug Info

Phase 1

Major depressive disorder

[19]

Discontinued Drug(s)

[+] 8 Discontinued Drugs

Deramciclane

Drug Info

Discontinued in Phase 3

Anxiety disorder

[20], [21]

Ritanserin

Drug Info

Discontinued in Phase 3

Anxiety disorder

[22], [23]

MCPP

Drug Info

Discontinued in Phase 2

Mood disorder

[24]

R-1065

Drug Info

Discontinued in Phase 1

Obesity

[25]

SB-247853

Drug Info

Discontinued in Phase 1

Anxiety disorder

[26]

ICI-169369

Drug Info

Terminated

Anxiety disorder

[27], [28]

Org-37684

Drug Info

Terminated

Anxiety disorder

[29], [30]

SDZ-SER-082

Drug Info

Terminated

Neurological disorder

[31], [32]

Mode of Action

[+] 4 Modes of Action

Agonist

[+] 56 Agonist drugs

Lorcaserin

Drug Info

[33], [34]

ATHX-105

Drug Info

[46]

Nuplazid

Drug Info

[47]

PRX00933

Drug Info

[16]

Aryl piperazine derivative 10

Drug Info

[52]

Aryl piperazine derivative 8

Drug Info

[52]

Aryl piperazine derivative 9

Drug Info

[52]

Benzazepine derivative 1

Drug Info

[52]

Benzazepine derivative 2

Drug Info

[52]

Benzazepine derivative 3

Drug Info

[52]

Benzazepine derivative 4

Drug Info

[52]

Benzazepine derivative 5

Drug Info

[52]

Benzazepine derivative 6

Drug Info

[52]

Chromene derivative 1

Drug Info

[52]

Heteroaryl-azepine derivative 1

Drug Info

[52]

Heteroaryl-azepine derivative 10

Drug Info

[52]

Heteroaryl-azepine derivative 11

Drug Info

[52]

Heteroaryl-azepine derivative 12

Drug Info

[52]

Heteroaryl-azepine derivative 13

Drug Info

[52]

Heteroaryl-azepine derivative 14

Drug Info

[52]

Heteroaryl-azepine derivative 15

Drug Info

[52]

Heteroaryl-azepine derivative 2

Drug Info

[52]

Heteroaryl-azepine derivative 3

Drug Info

[52]

Heteroaryl-azepine derivative 4

Drug Info

[52]

Heteroaryl-azepine derivative 5

Drug Info

[52]

Heteroaryl-azepine derivative 6

Drug Info

[52]

Heteroaryl-azepine derivative 7

Drug Info

[52]

Heteroaryl-azepine derivative 8

Drug Info

[52]

Heteroaryl-azepine derivative 9

Drug Info

[52]

PMID26609882-Compound-83

Drug Info

[52]

Quinoline derivative 2

Drug Info

[52]

Tricyclic pyrrolidine derivative 1

Drug Info

[52]

Tricyclic pyrrolidine derivative 2

Drug Info

[52]

Tricyclic pyrrolidine derivative 3

Drug Info

[52]

Tricyclic pyrrolidine derivative 4

Drug Info

[52]

MCPP

Drug Info

[60], [4]

R-1065

Drug Info

[61]

SB-247853

Drug Info

[62], [4]

Org-37684

Drug Info

[67]

5-CT

Drug Info

[78]

AL-37350A

Drug Info

[81]

alpha-methyl-5-HT

Drug Info

[82]

BRL-15572

Drug Info

[84]

BW723C86

Drug Info

[86]

CP-809101

Drug Info

[88]

CSC-500297

Drug Info

[88]

m-chlorophenylpiperazine

Drug Info

[93]

METHYLENEDIOXYMETHAMPHETAMINE

Drug Info

[94]

Org 12962

Drug Info

[35]

SB 216641

Drug Info

[84]

SB 243213

Drug Info

[106]

TFMPP

Drug Info

[78]

TQ-1017

Drug Info

[4]

WAY-163909

Drug Info

[110]

[125I]DOI

Drug Info

[82]

[3H]LSD

Drug Info

[88]

Antagonist

[+] 29 Antagonist drugs

Metergolin

Drug Info

[35]

Methysergide

Drug Info

[1], [36], [37], [38]

Mirtazapine

Drug Info

[39], [40]

Nefazodone

Drug Info

[40], [41]

Eltoprazine

Drug Info

[43]

PMID26609882-Compound-58

Drug Info

[52]

Pyrimidine derivative 23

Drug Info

[52]

Pyrimidine derivative 24

Drug Info

[52]

Pyrimidine derivative 25

Drug Info

[52]

Pyrimidine derivative 26

Drug Info

[52]

Pyrimidine derivative 27

Drug Info

[52]

Pyrimidine derivative 28

Drug Info

[52]

Pyrimidine derivative 29

Drug Info

[52]

Ritanserin

Drug Info

[56], [57], [58], [59]

LY53857

Drug Info

[38], [64], [65], [66]

BVT 933

Drug Info

[85]

cyamemazine

Drug Info

[89]

EGIS-7625

Drug Info

[90]

FR260010

Drug Info

[91]

LY334362

Drug Info

[92]

MPDT

Drug Info

[97]

norfluoxetine

Drug Info

[99]

SB 204741

Drug Info

[35]

SB 215505

Drug Info

[103]

SB 221284

Drug Info

[35]

SB 228357

Drug Info

[104]

SB 242084

Drug Info

[105]

spiramide

Drug Info

[35]

[3H]mesulergine

Drug Info

[82]

Modulator

[+] 9 Modulator drugs

Tramadol

Drug Info

[42]

SR46349B

Drug Info

[45]

Puerarin

Drug Info

[48]

Vabicaserin

Drug Info

[49], [50]

Tedatioxetine

Drug Info

[51]

Deramciclane

Drug Info

[53], [54], [55]

ICI-169369

Drug Info

[63]

SDZ-SER-082

Drug Info

[69]

MK-212

Drug Info

[95], [96]

Inhibitor

[+] 77 Inhibitor drugs

M100907

Drug Info

[44]

Ro-60-0175

Drug Info

[68]

(+/-)-nantenine

Drug Info

[70]

(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine

Drug Info

[68]

(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine

Drug Info

[68]

(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine

Drug Info

[68]

(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine

Drug Info

[68]

(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine

Drug Info

[71]

(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine

Drug Info

[72]

(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine

Drug Info

[72]

(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine

Drug Info

[72]

(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine

Drug Info

[72]

(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine

Drug Info

[72]

(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine

Drug Info

[72]

1-((R)-2-aminopropyl)-1H-indazol-6-ol

Drug Info

[73]

1-((S)-2-aminopropyl)-1H-indazol-6-ol

Drug Info

[73]

1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol

Drug Info

[73]

1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol

Drug Info

[73]

1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol

Drug Info

[73]

1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol

Drug Info

[73]

1-(2-aminoethyl)-1H-indazol-6-ol

Drug Info

[73]

1-(2-Dimethylamino-ethyl)-1H-indol-4-ol

Drug Info

[74]

1-(piperazin-1-yl)isoquinoline

Drug Info

[75]

1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol

Drug Info

[74]

2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine

Drug Info

[73]

2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline

Drug Info

[75]

3-(2-Amino-propyl)-1H-indol-5-ol

Drug Info

[73]

3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol

Drug Info

[74]

3-(2-Dimethylamino-ethyl)-1H-indol-6-ol

Drug Info

[74]

3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol

Drug Info

[74]

3-(2-Dimethylamino-propyl)-1H-indol-4-ol

Drug Info

[74]

3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol

Drug Info

[74]

3-(3-Dimethylamino-propyl)-1H-indol-4-ol

Drug Info

[74]

3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol

Drug Info

[74]

3-Dimethylaminomethyl-1H-indol-4-ol

Drug Info

[74]

4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one

Drug Info

[76]

4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine

Drug Info

[75]

4-(piperazin-1-yl)furo[3,2-c]pyridine

Drug Info

[75]

4-(piperazin-1-yl)thieno[2,3-d]pyrimidine

Drug Info

[75]

4-(piperazin-1-yl)thieno[3,2-c]pyridine

Drug Info

[75]

4-(piperazin-1-yl)thieno[3,2-d]pyrimidine

Drug Info

[75]

5,6-dichloro-3,4-dihydroquinazolin-2-amine

Drug Info

[77]

5-chloro-3,4-dihydroquinazolin-2-amine

Drug Info

[77]

5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine

Drug Info

[77]

5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine

Drug Info

[77]

5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide

Drug Info

[72]

5-MEO-DMT

Drug Info

[73]

6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine

Drug Info

[79]

6-(piperazin-1-yl)-9-propyl-9H-purine

Drug Info

[75]

6-bromo-2'-de-N-methylaplysinopsin

Drug Info

[80]

6-bromo-8-(piperazin-1-yl)imidazo[1,2-a]pyrazine

Drug Info

[75]

6-bromoaplysinopsin

Drug Info

[80]

6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide

Drug Info

[72]

6-methyl-4-(piperazin-1-yl)furo[2,3-d]pyrimidine

Drug Info

[75]

7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine

Drug Info

[79]

7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine

Drug Info

[79]

8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine

Drug Info

[77]

Aplysinopsin

Drug Info

[72]

BARETTIN

Drug Info

[83]

CHLOROPHENYLPIPERAZINE

Drug Info

[87]

Cyclo[(6-bromotryptophan)arginine]

Drug Info

[83]

N-(6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide

Drug Info

[98]

N-(pyridin-3-yl)indoline-1-carboxamide

Drug Info

[72]

N-3'-ethylaplysinopsin

Drug Info

[80]

OCTOCLOTHEPIN

Drug Info

[100]

PG-01037

Drug Info

[101]

RS-102,221

Drug Info

[102]

SB-271046

Drug Info

[107]

SEROTONIN

Drug Info

[83]

VER-2692

Drug Info

[108]

VER-3323

Drug Info

[109]

VER-5384

Drug Info

[109]

VER-5593

Drug Info

[109]

WAY-208466

Drug Info

[111]

WAY-466

Drug Info

[112]

YM-348

Drug Info

[79]

[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine

Drug Info

[74]

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

Top

Target-regulating microRNAs

Target-regulating microRNAs Info

Target-interacting Proteins

Target-interacting Proteins Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 5 KEGG Pathways

Calcium signaling pathway

Neuroactive ligand-receptor interaction

Gap junction

Serotonergic synapse

Inflammatory mediator regulation of TRP channels

Panther Pathway

[+] 1 Panther Pathways

5HT2 type receptor mediated signaling pathway

Reactome

[+] 2 Reactome Pathways

Serotonin receptors

G alpha (q) signalling events

WikiPathways

[+] 6 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

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 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.

REF 2

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. (Ligand id: 2941).

REF 3

Nat Rev Drug Discov. 2013 Feb;12(2):87-90.

REF 4

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 5

REF 6

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 012516.

REF 7

REF 8

Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39.

REF 9

REF 10

Local effect of tramadol on formalin evoked flinching behavior in rats. Rev Bras Anestesiol. 2008 Jul-Aug;58(4):375-9, 371-5.

REF 11

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 12

ClinicalTrials.gov (NCT00495885) Efficacy and Safety of M100907 on Sleep Maintenance Insomnia With a Sub-study in Stable Type II Diabetes Mellitus. U.S. National Institutes of Health.

REF 13

The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.

REF 14

ClinicalTrials.gov (NCT00735683) A Short-Term Study to Examine the Effects of ATHX-105 Phosphate on Weight Loss and Safety. U.S. National Institutes of Health.

REF 15

ClinicalTrials.gov (NCT02035553) A Study of the Safety and Efficacy of Pimavanserin in Patients With Alzheimer's Disease Psychosis. U.S. National Institutes of Health.

REF 16

2011 Pipeline of Proximagen Group plc.

REF 17

ClinicalTrials.gov (NCT00854724) Puerarin Effects on Alcohol Drinking. U.S. National Institutes of Health.

REF 18

ClinicalTrials.gov (NCT00768612) Study Evaluating Safety and Tolerability of Vabicaserin in Patients With Sudden Worsening of Schizophrenia. U.S. National Institutes of Health.

REF 19

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023694)

REF 20

REF 21

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001479)

REF 22

REF 23

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000237)

REF 24

Dopaminergic mechanisms of reinstatement of MDMA-seeking behaviour in rats. Br J Pharmacol. 2011 Apr;162(8):1770-80.

REF 25

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017316)

REF 26

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016366)

REF 27

REF 28

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000690)

REF 29

REF 30

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009204)

REF 31

REF 32

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006463)

REF 33

Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.

REF 34

Clinical pipeline report, company report or official report of Arena Pharmaceuticals (2011).

REF 35

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.

REF 36

Intake of fermented soybean (natto) increased locomotor activity in mice. Biol Pharm Bull. 2007 Apr;30(4):845-6.

REF 37

Serotonergic mechanisms of the lateral parabrachial nucleus in renal and hormonal responses to isotonic blood volume expansion. Am J Physiol Regul Integr Comp Physiol. 2007 Mar;292(3):R1190-7.

REF 38

p-Chloroamphetamine, a serotonin-releasing drug, elicited in rats a hyperglycemia mediated by the 5-HT1A and 5-HT2B/2C receptors. Eur J Pharmacol. 1998 Oct 23;359(2-3):185-90.

REF 39

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.

REF 40

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.

REF 41

Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey. Curr Top Med Chem. 2006;6(17):1801-23.

REF 42

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.

REF 43

Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.

REF 44

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.

REF 45

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.

REF 46

Pharmacological targeting of the serotonergic system for the treatment of obesity. J Physiol. 2009 January 1; 587(Pt 1): 49-60.

REF 47

The neuropharmacology of sleep paralysis hallucinations: serotonin 2A activation and a novel therapeutic drug. Psychopharmacology (Berl). 2018 Nov;235(11):3083-3091.

REF 48

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.

REF 49

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.

REF 50

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