Protein / target
Glutamate receptor 3
Protein at a glance
Biological role
Glutamate-gated calcium ion channel
Strongest disease association
Genetic Diseases, Inborn
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
Ionotropic glutamate receptor that functions as a ligand-gated cation channel, gated by L-glutamate and glutamatergic agonists such as alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), quisqualic acid, and kainic acid.
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Ionotropic glutamate receptor that functions as a ligand-gated cation channel, gated by L-glutamate and glutamatergic agonists such as alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), quisqualic acid, and kainic acid (By similarity). L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system and plays an important role in fast excitatory synaptic transmission by inducing long-term potentiation (By similarity). Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse upon entry of calcium (PubMed:17989220). The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist (PubMed:17989220). In the presence of CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate (PubMed:21172611)
Subcellular location
Domains and Gene Ontology detail (19)Hide
Gene Ontology
- CAMPA glutamate receptor complex
- Cdendritic spine
- Cendocytic vesicle membrane
- Cparallel fiber to Purkinje cell synapse
- Cplasma membrane
- Cpostsynaptic density membrane
- Cpostsynaptic membrane
- FAMPA glutamate receptor activity
- Famyloid-beta binding
- Fglutamate-gated calcium ion channel activity
- Fglutamate-gated receptor activity
- Fligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Ligand-gated signalling
- ·Ionotropic glutamate receptor that functions as a ligand-gated cation channel, gated by…
- ·ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membr…
- ·transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic…
Excitatory neurotransmission
- ·Ionotropic glutamate receptor that functions as a ligand-gated cation channel, gated by…
- ·synaptic transmission, glutamatergic
Ion channel gating
- ·glutamate-gated calcium ion channel activity
- ·ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membr…
- ·transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic…
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
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.
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.
Glutamate receptor ionotropic AMPA antagonist
Indicated for Epilepsy, Migraine Disorders, Seizures
Glutamate receptor ionotropic AMPA antagonist
Indicated for Epilepsies, Partial, Epilepsy, Seizures
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 GRIA3
Gene-level evidence surfaced through the gene GRIA3that 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.
View evidence synthesis (4)Hide
This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. 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
13 compounds recorded · 2 approved · 11 in clinical development
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 (9)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 2 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.
- Regulatory approval
Approval: TOPIRAMATE (ANDA220943)
- Product recall
Recall (Class III): TOPIRAMATE
- Supplemental approval
Supplemental approval: PHENTERMINE AND TOPIRAMATE (NDA022580)
- Product recall
Recall (Class II): PERAMPANEL
- Regulatory approval
Approval: PERAMPANEL (ANDA219052)
- Label change
Label change: TOPIRAMATE (ANDA078499)
- Safety communication
Drug Safety Update: Topiramate (Topamax): introduction of new safety measures, including a Pregnancy Prevention Programme
- Safety communication
Drug Safety Update: Topiramate (Topamax): start of safety review triggered by a study reporting an increased risk of neurodevelopmental disabilities in children with prenatal exposure
- New publicationA randomized pilot trial of topiramate for alcohol use disorder in veterans with traumatic brain injury: Effects on alcohol use, cognition, and post-concussive symptoms.
- New publicationCognitive and behavioral effects of lamotrigine and topiramate in healthy volunteers.
- New publicationA double-blind, randomized trial of topiramate in Lennox-Gastaut syndrome. Topiramate YL Study Group.
- New publicationA randomized, placebo-controlled study of topiramate in primary generalized tonic-clonic seizures. Topiramate YTC Study Group.
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.