> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/target/gabra1-4391585d-ccfe-5231-89a4-e911338239fd
> Record changed: 2026-10-13

# GABRA1

ENSG00000022355

Target class

Ion channel

Chromosome

5

Approved drugs

58

Clinical candidates (approved and in development)

70

## Clinical evidence

**Approved drugs**

58

**ClinGen gene-disease validity**

Definitive

**Clinical candidates (approved and in development)**

70

## Druggability

**Chemical probe available**

No

## Names

**Other names**

- EJM5

**Target name**

GABRA1

**Gene name**

Gamma-aminobutyric acid type A receptor subunit alpha1

**Gene symbol**

GABRA1

**Protein name**

Gamma-aminobutyric acid receptor subunit alpha-1 (GABA(A) receptor subunit alpha-1) (GABAAR subunit alpha-1)

## Classification

**Gene biotype**

Protein coding

**Gene family**

Gamma-aminobutyric acid type A receptor subunits

**Target class**

Ion channel

**Target type**

Human gene

## Expression and localisation

**Tissues expressed in**

12

**Protein localisation evidence grade**

Supported

**Highest tissue expression**

82.71

**Tissue specificity (Gini)**

0.894

**Tissue specificity (tau)**

0.951

## Pathways and interactions

**KEGG gene identifiers**

- hsa:2554

**Protein interaction confidence**

0.832706

**Protein interaction partners**

34

### Reactome pathways (2)

- R-HSA-1236394
- R-HSA-977443

## Genomic location

**End position**

161899981

**Start position**

161847063

**Chromosome**

5

**Strand**

Forward

## Identifiers

**Ensembl gene ID**

ENSG00000022355

**HGNC ID**

HGNC:4075

Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:4075)

**NCBI Gene ID**

2554

**UniProt ID**

P14867

## Cellular location

- Postsynaptic cell membrane
- Multi-pass membrane protein . Cell membrane
- Multi-pass membrane protein . Cytoplasmic vesicle membrane
- Multi-pass membrane protein . Note=Mainly located in GABAergic synapses in granule cells, and also in the extrasynaptic membrane at a lower concentration. .
- Plasma membrane

### Publication evidence (3)

- PubMed 29950725  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/29950725/)
- PubMed 2465923  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/2465923/)
- PubMed 25489750  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/25489750/)

## Tissue expression

**Tissue specificity (tau)**

0.951111

**Expression inequality (Gini)**

0.893764

### Highest expression

Expression in transcripts per million

**Brain - Cerebellar Hemisphere**

82.71

**Brain - Frontal Cortex (BA9)**

58.46

**Brain - Cerebellum**

55.67

**Brain - Cortex**

31.14

**Brain - Anterior cingulate cortex (BA24)**

23.3

### All tissues (54)

Expression in transcripts per million

- Brain - Cerebellar Hemisphere82.71
- Brain - Frontal Cortex (BA9)58.46
- Brain - Cerebellum55.67
- Brain - Cortex31.14
- Brain - Anterior cingulate cortex (BA24)23.3
- Brain - Hippocampus8.45
- Brain - Hypothalamus8.18
- Brain - Amygdala7.79
- Brain - Nucleus accumbens (basal ganglia)7.75
- Brain - Caudate (basal ganglia)4.7
- Brain - Putamen (basal ganglia)4.06
- Brain - Substantia nigra3.38
- Brain - Spinal cord (cervical c-1)0.96
- Testis0.17
- Stomach0.08
- Pituitary0.07
- Prostate0.02
- Spleen0.02
- Colon - Sigmoid0.01
- Adrenal Gland0.01
- Colon - Transverse0.01
- Adipose - Visceral (Omentum)0.01
- Lung0.01
- Small Intestine - Terminal Ileum0.01
- Thyroid0.01

And 29 more, listed on the interactive page.

## Biological functions

### Biological processes (4)

- GO:0007214  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007214)
- GO:0051932  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0051932)
- GO:1902476  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:1902476)
- GO:1904862  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:1904862)

### Cellular components (3)

- GO:0005886  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005886)
- GO:0043197  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0043197)
- GO:1902711  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:1902711)

### Molecular functions (2)

- GO:0004890  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0004890)
- GO:0022851  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0022851)

## On-target safety

- decreased sleep  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased sleep  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased eating  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased eating  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased blood pressure  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased blood pressure  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased body temperature  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased body temperature  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased pain  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased pain  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- Occurrence, Epileptic seizure  
### Studies

  - cell-based  
### Biological samples

  - brain  
Evidence source  
Source: [aopwiki.org](https://aopwiki.org/aops/10)
- convulsions  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: convulsions  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- ataxia  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: ataxia  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased cardiac output  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased cardiac output  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased cardiac contractility  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased cardiac contractility  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- drug abuse/dependence  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: drug abuse/dependence  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased memory  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased memory  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased convulsions  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased convulsions  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased locomotor activity  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased locomotor activity  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- muscle relaxation  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: muscle relaxation  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased anxiety  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased anxiety  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased respiratory rate  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased respiratory rate  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased sleep  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased sleep  
### Biological samples (2)

  - central nervous system
  - cardiovascular  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)

## Off-target safety

- seizure (when used as a BZD antidote)  
### Effects

  - Inhibition/Decrease/Downregulation: general  
### Studies

  - preclinical: seizure (when used as a BZD antidote)  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- muscle relaxation  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: muscle relaxation  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- dizziness  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: dizziness  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- anterograde amnesia  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: anterograde amnesia  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- abuse potential  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: abuse potential  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- sedation  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: sedation  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- depression  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: depression  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- anxiolysis  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: anxiolysis  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- ataxia  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: ataxia  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- anticonvulsant  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: anticonvulsant  
### Biological samples

  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)

## Related records

### Trials (4,014)

- "Chou's Tiaoshen" Acupoints for Short-term Insomnia.
- "Volatile Anesthetic Protection Of Renal Transplants: VAPOR-1-trail
- (Peak) A Phase 3 Randomized Trial of CGT9486+Sunitinib vs. Sunitinib in Subjects With Gastrointestinal Stromal Tumors
- \[18F\]Fluciclovine in Post-treatment Glioblastoma ( Axumin )
- 1-1-8 Wash-in for Sevoflurane Low Flow Anesthesia
- 12-Month Real-World Safety & Efficacy of Lecanemab in Early Alzheimer's Disease
- 28-day Repeat Dose and Drug Interaction Study With Orvepitant (GW823296)
- 3 mL Inhaled Methoxyflurane for Intrauterine Device (IUD) Insertion
- 50% Effective Concentration of Sevoflurane for Immobility
- 6-Month Chronic Efficacy & Safety Study of Eszopiclone in Adult Subjects With Primary Insomnia
- A 2-Part Single Dose Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of E2006
- A 2-Part Study to Assess Potential Metabolism-Based Drug-Drug Interactions of E2006 When Coadministered With Itraconazole, Rifampin, Midazolam, or Bupropion
- A 5-Week Trial Of PD 0332334 And Alprazolam Extended Release Compared To Placebo In Patients With Generalized Anxiety Disorder
- A Better Choice for Patients Undergoing Endovascular Coil Embolization
- A Bioequivalence and Food Effect Study of SEP-190 in Japanese Healthy Subjects (Study SEP 190-102)
- A Bioequivalence Study Of A New Alprazolam Dropped Formulation Versus Alprazolam Tablets
- A Clinical Drug-Drug Interaction (DDI) Study With Omaveloxolone
- A Clinical Study Evaluating Sedation of Intravenous Administration of HSK3486 in ICU Patients Undergoing Long-Term Mechanical Ventilation
- A Clinical Study of Remimazolam Tosilate Compared to Propofol for General Anesthesia During Elective Surgery
- A Clinical Study of Remimazolam Tosilate in Patients Undergoing Bronchoscopy

### Drugs (81)

- ABP-700 GABA-A receptor; anion channel agonist
- Acamprosate GABA-A receptor; anion channel positive modulator
- Acamprosate calcium GABA-A receptor; anion channel positive modulator
- Adipiplon GABA-A receptor; anion channel partial agonist
- Alprazolam GABA-A receptor; anion channel positive allosteric modulator
- Brexanolone GABA-A receptor; anion channel positive allosteric modulator
- Butabarbital GABA-A receptor; anion channel positive allosteric modulator
- Butabarbital sodium GABA-A receptor; anion channel positive allosteric modulator
- Butalbital GABA-A receptor; anion channel positive allosteric modulator
- Cenobamate GABA-A receptor; anion channel positive allosteric modulator
- Chlordiazepoxide GABA-A receptor; anion channel positive allosteric modulator
- Chlordiazepoxide hydrochloride GABA-A receptor; anion channel positive allosteric modulator
- Cipepofol GABA-A receptor; anion channel agonist
- Clobazam GABA-A receptor; anion channel positive allosteric modulator
- Clomethiazole GABA-A receptor; anion channel positive allosteric modulator
- Clonazepam GABA-A receptor; anion channel positive allosteric modulator
- Clorazepate dipotassium GABA-A receptor; anion channel positive allosteric modulator
- Clorazepic acid GABA-A receptor; anion channel positive allosteric modulator
- Clotiazepam GABA-A receptor; anion channel positive allosteric modulator
- Darigabat GABA-A receptor; anion channel agonist

---

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