Question

What are the N-methyl D-aspartate (NMDA) antagonists for Alzheimer's?

Answer 1

N-methyl D-aspartate (NMDA) antagonists are used in the treatment of Alzheimer's disease to block NMDA receptors and prevent excitotoxicity. Examples include memantine and traxoprodil (CP-101,606). These medications can help manage symptoms and slow down the progression of the disease.

Step-by-step explanation:

N-methyl D-aspartate (NMDA) antagonists are a type of medication used in the treatment of Alzheimer's disease. These drugs work by blocking the action of NMDA receptors, which are involved in excitatory signal transmission in the brain. By inhibiting these receptors, NMDA antagonists help reduce the damage caused by excess glutamate and prevent excitotoxicity, a process that can lead to neuronal cell death.

Some examples of NMDA antagonists used in the treatment of Alzheimer's disease include memantine and traxoprodil (CP-101,606). Memantine is approved by the FDA for moderate to severe Alzheimer's disease, while traxoprodil is still being researched.

It is important to note that NMDA antagonists are not a cure for Alzheimer's disease, but they can help manage symptoms and slow down the progression of the disease.

Answer 2

NMDA antagonists like memantine target the glutamate system to reduce excitotoxicity in Alzheimer's disease. Experimental treatments targeting the NR2B subunit, like CP-101,606, have shown promise in clinical trials for dyskinetic symptoms. Additionally, AMPA receptor antagonists are being investigated as potential treatments to address glutamatergic dysregulation in Alzheimer's.

Step-by-step explanation:

NMDA Antagonists for Alzheimer's Disease

NMDA (N-methyl D-aspartate) antagonists are a class of medications that can modulate the effects of glutamate in the brain. Glutamate is an important neurotransmitter implicated in processes like learning and memory but can cause excitotoxicity when its levels become too high, potentially contributing to neurodegenerative conditions such as Alzheimer's disease. NMDA antagonists have been explored for their potential in treating Alzheimer's, with the goal of preventing this excitotoxicity. One particular NMDA antagonist that has been considered is memantine, which is currently approved for treating moderate to severe Alzheimer's disease. It acts by blocking the NMDA receptor in a voltage-dependent manner, thereby reducing abnormal glutamate activity without disrupting normal neurotransmission. Another experimental treatment mentioned in the literature includes compounds targeted at the NR2B subunit of the NMDA receptor, such as CP-101,606 (Traxoprodil). While successful in treating dyskinetic symptoms in human trials, it did not address Parkinsonian symptoms in the same way it did in animal models.

Recent findings also highlight the importance of AMPA receptors in Alzheimer's disease, particularly those that are calcium-permeable, as they have been implicated in synaptic dysregulation associated with the condition. The use of antagonists for these receptors, such as naphthylacetylspermine (NAS), has been considered as an emerging target for reducing synaptic dysfunction and excitotoxicity in various neurodegenerative diseases.