Preladenant

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Overview[edit | edit source]

Preladenant is a pharmacological compound that acts as an adenosine receptor antagonist. It is primarily investigated for its potential use in the treatment of Parkinson's disease. Preladenant works by blocking the action of adenosine at the A2A receptor, which is thought to play a role in the modulation of dopaminergic activity in the brain.

Mechanism of Action[edit | edit source]

Preladenant is a selective antagonist of the adenosine A2A receptor. Adenosine is a neuromodulator that influences various physiological processes, including neurotransmission and cerebral blood flow. In the context of Parkinson's disease, adenosine A2A receptors are found in high concentrations in the striatum, a brain region involved in motor control. By blocking these receptors, preladenant may enhance dopaminergic signaling, thereby improving motor function in patients with Parkinson's disease.

Clinical Development[edit | edit source]

Preladenant has been the subject of several clinical trials to evaluate its efficacy and safety in the treatment of Parkinson's disease. These studies have explored its potential to improve motor symptoms and reduce "off" time in patients who are already receiving levodopa therapy. While some trials have shown promising results, others have not demonstrated significant benefits over existing treatments.

Pharmacokinetics[edit | edit source]

The pharmacokinetic profile of preladenant includes its absorption, distribution, metabolism, and excretion. Preladenant is administered orally and is absorbed into the bloodstream, where it reaches peak plasma concentrations within a few hours. It is metabolized primarily in the liver and excreted through the kidneys.

Side Effects[edit | edit source]

Common side effects of preladenant may include nausea, dizziness, and insomnia. As with any medication, the risk of side effects must be weighed against the potential benefits, and patients should be monitored for any adverse reactions during treatment.

Research and Future Directions[edit | edit source]

Research into preladenant and other adenosine receptor antagonists continues, as scientists seek to better understand their role in the treatment of Parkinson's disease and other neurological disorders. Future studies may focus on optimizing dosing regimens, identifying patient populations that may benefit most, and exploring combination therapies with other neuroprotective agents.

Related Pages[edit | edit source]

Chemical structure of Preladenant
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Contributors: Prab R. Tumpati, MD