what receptor would a medication bind to that helps to prevent parkinsons

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Parkinson'southward disease (PD) is a chronic neurological disease caused by the loss of dopamine-producing nervus cells in the encephalon. PD is marked by motor symptoms like tremor, stiffness, and slowed movements. Non-motor symptoms, similar depression, sleep bug, and diminished cognitive function, are also common.

The current treatment of PD focuses on dopamine replacement, namely with the use of a drug chosen levodopa. While levodopa is the most effective drug for reducing symptoms and improving quality of life in patients with PD, it's associated with undesirable side effects, motor fluctuations (on-off), and involuntary movements (dyskinesia).

Equally a result, experts have been looking into other drug targets (besides dopamine) for reducing the symptoms of PD. Ane such emerging drug target is a brain chemical messenger called adenosine.

Adenosine and Parkinson'southward Disease

Adenosine is a molecule present in all trunk fluids and tissues and has been studied for decades for its therapeutic potential. Even though adenosine is found throughout the brain, its role is, unfortunately, still poorly understood, peculiarly when information technology comes to Parkinson'due south illness and dopamine signaling.

That said, nosotros do know that adenosine has four receptor (binding site) subtypes—A1, A2A, A2B, and A3.

The A2A receptors have piqued scientists' interest because they are found on dopamine-producing nerve cells in the area of the brain called the basal ganglia. These receptors uniquely collaborate with (and are conveniently located next to) dopamine receptors on the same cells.

Cause of Parkinson's Disease

The loss of dopamine-producing nerve cells in the substantial nigra (a region inside the basal ganglia) is what causes the symptoms of Parkinson'south disease. Scientists aren't certain exactly, merely genes and environmental factors likely contribute to this nerve jail cell loss.

Researchers have found that by blocking ("antagonizing") the adenosine A2A receptors, the motor symptoms of patients with PD improve. As such, various drugs that target and cake the adenosine A2A receptor have been examined in multiple homo studies of patients with PD.

One such drug—Nourianz (istradefylline)—is the showtime adenosine A2A receptor antagonist medication to be approved in the U.s.a. for the treatment of PD.

Nourianz: An Add-On Drug in PD

Nourianz is an oral drug taken once daily with or without food. It was canonical in the Us in 2019 specifically as an improver treatment to levodopa in patients with PD experiencing "off" episodes.

"Off" episodes are a known long-term complication of levodopa that occur when PD-related symptoms reappear earlier the next scheduled levodopa dose is due. During an "off' episode, a person may feel stiff and slow, frozen in place, or like they cannot form words.

In studies examining thousands of patients with PD, Nourianz has been establish to reduce these uncomfortable, sad "off" episodes, so patients tin feel energized for longer periods of time during the 24-hour interval.

In addition to the promising motor benefit of Nourianz, the drug is well-tolerated and appears prophylactic. Across a series of studies, side effects similar orthostatic hypotension (a sudden drop in blood pressure level when going from sitting or lying down to standing), sleepiness, confusion, and psychosis—all known adverse effects related to levodopa, especially in older patients—were similar for patients receiving Nourianz and those receiving placebo.

Moreover, compared to levodopa, Nourianz has been institute to be less likely to induce dyskinesia, which refers to twitching, jerking, twisting, or writhing musculus movements that are out of a person's control. Similar "off" episodes, dyskinesia is a known complication of long-term levodopa use.

Levodopa-Induced Dyskinesia

Information technology's non entirely clear why levodopa-induced dyskinesia occurs. Experts doubtable that both disturbances in dopamine signaling betwixt nerve cells (which lead to fluctuating dopamine levels in the brain) and the continued loss of dopamine-producing nerve cells play a role.

Keep in mind, though, Nourianz does not forbid the onset of dyskinesia caused past levodopa (and Nourianz is but canonical to be taken with levodopa).

Co-ordinate to the drug manufacturer, common side furnishings associated with Nourianz include:

• Dizziness
• Constipation
• Nausea
• Hallucinations
• Insomnia

Unusual urges or compulsive behaviors may too occur when taking Nourianz.

Other Benefits of Nourianz

Information technology'southward important to mention that also improving the motor symptoms of PD, there are other potential benefits to taking Nourianz (and perhaps other adenosine A2A receptor antagonists in the pipeline).

Research suggests that adenosine A2A receptor blockers have neuroprotective furnishings, meaning they may decrease the death charge per unit of dopamine-producing nerve cells in the brain.

Supporting this neuroprotective part is the fact that the consumption of caffeine, which is a natural compound that blocks adenosine A2A receptors, is associated with a lower chance for developing PD in good for you individuals. Caffeine has besides been constitute to reduce the progression or worsening of motor symptoms in patients with PD.

Adenosine A2A receptor antagonists may also improve mood disorders, which are common in PD. I written report found that patients with PD taking Nourianz had an improvement in apathy and depressive-like symptoms.

While the precise upshot of Nourianz on knowledge dysfunction in patients with PD remains unknown, more studies on its therapeutic potentials will likely be done now that the drug is approved.

That said, in creature models of PD, the blockade of adenosine A2A receptors reversed working memory impairments. Caffeine consumption has as well been linked to less severe cognitive symptoms in patients with PD, as well every bit a lower prevalence of lack of motivation and lack of pleasure compared to non-java drinkers.

Finally, pocket-size studies accept revealed that Nourianz may reduce daytime sleepiness and freezing of gait (an aberrant walking design) and improve urinary dysfunction and postural abnormalities in patients with PD. More than investigation with larger studies is needed to confirm these findings.

A Give-and-take From Verywell

Targeting adenosine offers a novel approach to optimally caring for patients with PD, especially older patients and those with avant-garde PD.

Also encouraging is the prospect that Nourianz and perhaps other future drugs that block the adenosine A2A receptor may improve non-motor symptoms, similar mood or cognitive issues. These symptoms often unintentionally take a backseat in importance to the motor symptoms of Parkinson's disease, even though they can be as if non more disabling.

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Source: https://www.verywellhealth.com/role-of-adenosine-in-parkinson-s-disease-5176185

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