GSK-598809

A selective dopamine D3 receptor antagonist

GSK-598809
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CAS Number	957118-49-9
PubChem	11550036
DrugBank
ChemSpider	9720483
KEGG	D09995

GSK-598809 is a selective dopamine D3 receptor antagonist that has been investigated for its potential use in the treatment of schizophrenia and other neuropsychiatric disorders.

Pharmacology

GSK-598809 acts as a selective antagonist at the dopamine D3 receptor, which is a subtype of the dopamine receptor family. The D3 receptor is primarily located in the limbic system of the brain, an area associated with emotion, cognition, and reward. By blocking the D3 receptor, GSK-598809 may help modulate the dopaminergic system, which is often dysregulated in conditions such as schizophrenia.

Mechanism of Action

The mechanism of action of GSK-598809 involves the inhibition of dopamine binding to the D3 receptor. This action is thought to reduce the hyperactivity of dopaminergic pathways that are implicated in the positive symptoms of schizophrenia, such as hallucinations and delusions. Additionally, by targeting the D3 receptor, GSK-598809 may have fewer side effects compared to non-selective dopamine antagonists, which affect multiple dopamine receptor subtypes.

Clinical Development

GSK-598809 has undergone various stages of clinical trials to assess its efficacy and safety in humans. Initial studies have focused on its potential to improve cognitive deficits and reduce symptoms in patients with schizophrenia. However, as of the latest updates, GSK-598809 has not yet been approved for clinical use, and further research is needed to fully understand its therapeutic potential and safety profile.

Potential Applications

Beyond schizophrenia, GSK-598809 may have applications in other neuropsychiatric disorders where dopamine dysregulation is a factor. These include conditions such as bipolar disorder, addiction, and certain types of depression. The selective nature of GSK-598809 makes it a promising candidate for these applications, as it may offer therapeutic benefits with a reduced risk of side effects.

Chemical Properties

Chemical structure of GSK-598809

GSK-598809 is chemically classified as a pyrimidine derivative. Its molecular formula is C₁₆H₂₀ClN₅, and it has a molecular weight of 317.82 g/mol. The compound is characterized by the presence of a piperazine ring, which is a common feature in many psychoactive drugs.

Related Pages

• Dopamine receptor
• Schizophrenia
• Neurotransmitter
• Antipsychotic