Protein / target
5-hydroxytryptamine receptor 2C
Protein at a glance
Biological role
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding
Primary system
Nervous system
Strongest disease association
autism
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
37 approved · 4 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
G protein-coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:12970106, PubMed:18703043, PubMed:19057895, PubMed:29398112, PubMed:7895773). 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) (PubMed:19057895, PubMed:29398112). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors (PubMed:18703043, PubMed:29398112). HTR2C is coupled to G(q)/G(11) G alpha proteins and activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively (PubMed:18703043, PubMed:29398112). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:29398112). Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelanocortin neurons and the release of CRH that then regulates the release of corticosterone (By similarity). Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress (By similarity). Plays a role in insulin sensitivity and glucose homeostasis (By similarity)
Subcellular location
Domains and Gene Ontology detail (27)Hide
Gene Ontology
- Cdendrite
- CG protein-coupled serotonin receptor complex
- Cplasma membrane
- Csynapse
- F1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding
- FG protein-coupled serotonin receptor activity
- FGq/11-coupled serotonin receptor activity
- Fidentical protein binding
- Fneurotransmitter receptor activity
- Fserotonin binding
- Fserotonin receptor activity
- Pbehavioral fear response
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
G protein-coupled signalling
- ·G protein-coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:12970106, PubMed:…
- ·G protein-coupled serotonin receptor complex
- ·G protein-coupled serotonin receptor activity
- ·G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messen…
Synaptic signalling
- ·synapse
- ·neurotransmitter receptor activity
- ·chemical synaptic transmission
Motor control
- ·locomotory behavior
View underlying pathways (2)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Serotonin 2c (5-HT2c) receptor antagonist
Appears in clinical studies involving bipolar disorder, schizophrenia, aggressive behavior, autism
Serotonin 2c (5-HT2c) receptor antagonist
Appears in clinical studies involving schizophrenia, bipolar disorder, bipolar I disorder, major depressive disorder
Serotonin 2c (5-HT2c) receptor antagonist
Appears in clinical studies involving major depressive disorder, treatment resistant depression, obsessive-compulsive disorder, depressive disorder
Serotonin 2c (5-HT2c) receptor antagonist
Appears in clinical studies involving bipolar disorder, schizophrenia, major depressive disorder, Agitation
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Highest overall evidence
Remaining associations by Open Targets' aggregated evidence score.
Show all associationsHide all associations
Open Targets ranks 648 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 44 total
Seizure · Dravet syndrome · encephalopathy, progressive, early-onset, with brain edema and/or leukoencephalopathy
psychotic disorder · psychotic disorder
obesity disorder · Obesity · Overweight
psychotic disorder · schizophrenia
schizophrenia · psychotic disorder · alcohol dependence
major depressive disorder · glioblastoma
schizophrenia · psychotic disorder
major depressive disorder · generalized anxiety disorder
bipolar disorder · schizophrenia · Agitation
Tractability
Safety liabilities
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through 4 drugs that target this protein, so each event is news about that drug rather than about the protein directly.
- Label change
Label change: RISPERIDONE (ANDA076996)
- Label change
Label change: RISPERIDONE (ANDA077494)
- New publicationSTAT3 Signaling Mediates Agomelatine Restoration of Prefrontal Cortex Synaptic Plasticity in Chronic Social Defeat Stress Mice.
- Label change
Label change: RISPERIDONE (ANDA091384)
- Withdrawn from market
Market withdrawal: Olanzapine Apotex (EMA)
- Label change
Label change: RISPERIDONE (ANDA079088)
- Label change
Label change: RISPERIDONE (ANDA076996)
- Label change
Label change: RISPERIDONE (ANDA076996)
- Label change
Label change: RISPERIDONE (ANDA091384)
- Label change
Label change: RISPERIDONE (ANDA079088)
- Label change
Label change: RISPERIDONE (ANDA079088)
- Label change
Label change: RISPERIDONE (ANDA079088)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.