Protein / target
5-hydroxytryptamine receptor 2C
Protein at a glance
Biological role
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding
Strongest disease association
Autistic Disorder
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
G protein-coupled receptor for 5-hydroxytryptamine (serotonin).
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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.
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Synaptic signalling
- ·synapse
- ·neurotransmitter receptor activity
- ·chemical synaptic transmission
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…
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.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
37 medicines meet Open Targets' target-level approved-medicine definition; the 6 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Serotonin 2c (5-HT2c) receptor antagonist
Indicated for Autistic Disorder, Bipolar Disorder, Psychotic Disorders, Schizophrenia
Serotonin 2c (5-HT2c) receptor antagonist
Indicated for Bipolar Disorder, Schizophrenia
Serotonin 2c (5-HT2c) receptor antagonist
Indicated for Depressive Disorder
Serotonin 2c (5-HT2c) receptor antagonist
Indicated for Bipolar Disorder, Mental Disorders, Psychomotor Agitation, Psychotic Disorders
Serotonin 2c (5-HT2c) receptor antagonist
Indicated for Depressive Disorder, Sleep Initiation and Maintenance Disorders
Serotonin 2c (5-HT2c) receptor antagonist
Indicated for Bipolar Disorder, Mental Disorders, Psychomotor Agitation, Psychotic Disorders
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene HTR2C
Gene-level evidence surfaced through the gene HTR2Cthat encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
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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 per-type scores above show the calculation.
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Drug development
44 compounds recorded · 37 approved · 4 in clinical development · 3 earlier-stage
View all recorded compounds (10)Hide
Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Antibodies — Emerging
Protein degraders — Emerging
View underlying tractability evidence (8)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
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. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 4 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Label change
Label change: OLANZAPINE (ANDA076133)
- Label change
Label change: OLANZAPINE (ANDA076255)
- Label change
Label change: RISPERIDONE (ANDA076996)
- Label change
Label change: RISPERIDONE (ANDA077494)
- Label change
Label change: OLANZAPINE (ANDA076133)
- Label change
Label change: OLANZAPINE (ANDA076255)
- New publicationEffects of PDE10A inhibitor MK-8189 in people with an acute episode of schizophrenia: A randomized proof-of-concept clinical trial.
- New publicationCanadian Network for Mood and Anxiety Treatments (CANMAT) and International Society for Bipolar Disorders (ISBD) 2018 guidelines for the management of patients with bipolar disorder.
- Safety communication
Drug Safety Update: Agomelatine (Valdoxan): risk of liver toxicity
- Safety communication
Drug Safety Update: Agomelatine (Valdoxan/ Thymanax): risk of dose-related hepatotoxicity and liver failure
- New publicationCognitive-behavioral therapy vs risperidone for augmenting serotonin reuptake inhibitors in obsessive-compulsive disorder: a randomized clinical trial.
- New publicationEffectiveness of antipsychotic drugs in patients with chronic schizophrenia.
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.