The mysterious power of NMDA receptor antagonists: How might they change the way we do anesthesia?

NMDA receptor antagonists are a class of drugs specifically designed to inhibit the function of N-methyl-D-aspartate receptors (NMDAR), which makes them occupy an important position in anesthesiology. The anesthetic state induced by this type of drug is called dissociative anesthesia and is widely used for anesthesia in humans and animals. Among many synthetic anesthetics, synthetic anesthetics such as halothane and diazepam also function as NMDAR antagonists, demonstrating their importance in the medical field.

More than just a therapy, these receptor antagonists can cause a variety of side effects, creating another level of challenge.

Main uses and effects

NMDA receptor antagonists can improve the safety of anesthesia. The dissociative anesthetic state they cause is known for its characteristic features such as tonicity, amnesia, and analgesia. For example, ketamine is widely used in emergency medicine, especially in patients with unknown medical records, because it has a mild respiratory and circulatory depressant effect.

In addition, certain drugs, such as demethylclothiazide and ketamine metabolites, have been confirmed to be NMDA receptor antagonists. With the deepening of the understanding of these drugs, more and more studies have shown that the inhibition of NMDA receptor function is closely related to memory impairment in the elderly, schizophrenia and other neurological diseases.

Some researchers believe that reduced NMDA receptor function in older adults may be partly responsible for memory decline, revealing the two-sided nature of these drugs.

Neurotoxicity and its potential effects

Olney's lesion is a vacuolization of neuronal mass observed in rodents. Although many experts believe this does not apply to human use, repeated long-term use of NMDA receptor antagonists (such as ketamine and PCP) has been associated with short-term cognitive impairment. Large-scale, long-term studies show that regular ketamine users may experience mild cognitive deficits, whereas former or occasional users are less likely to experience such problems.

This has led to concerns among the professional community that, for example, other drugs could be taken to reduce the risk of neurotoxicity from NMDA receptor antagonists.

Therapeutic potential for excitotoxicity

Because excessive activation of NMDA receptors is associated with excitotoxicity, NMDA receptor antagonists are useful in the treatment of drug withdrawal, traumatic brain injury, stroke, and neurodegenerative diseases (such as Alzheimer's disease, Parkinson's disease, etc.) and Huntington's disease). However, the side effects of these treatments often cause clinical trials to fail.

Mechanism and mode of action

NMDA receptor, as an ionotropic receptor, can transmit electrical signals between neurons. In order to keep the receptor activated, glutamate and glycine molecules must be bound to it. NMDAR antireceptors act on receptors and can be divided into four categories: competitive antagonists, glycine antagonists, noncompetitive antagonists, and noncompetitive channel blockers.

With the deepening of research, we have a clearer understanding of different types of NMDA receptor antagonists, which not only promotes the improvement of anesthesia methods, but also opens up new thinking directions for the medical community.

Conclusion

In the medical community, NMDA receptor antagonists have not only changed our understanding of anesthesia but also sparked widespread discussion because of the suggestive and modulatory properties of these drugs. As we continue to decipher the potential of these drugs, the question is beginning to emerge: Will these receptor antagonists bring more treatment options to patients in the future?

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