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Discovery of Procognitive Antipsychotics by Combining Muscarinic M<sub>1</sub> Receptor Structure-Activity Relationship with Systems Response Profiles in Zebrafish Larvae.
Author: EkFredrik, HellmanKarin, MaloMarcus, OhlssonJörgen, OlssonRoger
Original Abstract of the Article :
Current antipsychotic drugs are notably ineffective at addressing the cognitive deficits associated with schizophrenia. <i>N</i>-Desmethylclozapine (NDMC), the major metabolite of clozapine, displays muscarinic M<sub>1</sub> receptor (M<sub>1</sub>) agonism, an activity associated with improvement i...See full text at original site
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ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
難解な医学論文を、専門知識のない方にも理解しやすいように、噛み砕いて説明することを目指しています。
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引用元:
https://doi.org/10.1021/acschemneuro.9b00524
データ提供:米国国立医学図書館(NLM)
Unveiling the Potential of Procognitive Antipsychotics: A Quest for Cognitive Enhancement
Schizophrenia is a complex mental disorder that creates an oasis of confusion in the desert of the human mind. While current antipsychotic drugs are effective in controlling the hallucinations and delusions associated with schizophrenia, they often fail to address the debilitating cognitive impairments that can severely impact a person's quality of life. This research dives deep into the world of antipsychotics, aiming to discover novel drugs that not only control psychotic symptoms but also enhance cognitive function. The researchers focused on the M1 receptor, a key player in cognitive processes. They synthesized a series of analogues of N-desmethylclozapine (NDMC), a known M1 receptor agonist, to investigate the structure-activity relationship (SAR) at this receptor. Their findings revealed that specific modifications in the tricyclic core of NDMC led to increased M1 agonist activity, suggesting a potential pathway for procognitive antipsychotics.
A New Oasis for Cognitive Enhancement: The Promise of M1 Agonism
This study sheds light on the potential of M1 receptor agonism as a target for developing procognitive antipsychotics. The researchers demonstrated that specific modifications in the structure of NDMC resulted in increased M1 agonist activity, leading to promising preclinical results. The results indicate that targeting the M1 receptor could be a valuable approach for mitigating the cognitive deficits associated with schizophrenia.
Navigating the Desert of Mental Health: A New Path for Treatment
The discovery of procognitive antipsychotics could offer a much-needed lifeline for individuals struggling with the cognitive impairments of schizophrenia. This research provides a promising new direction for drug development, highlighting the potential of M1 receptor agonism as a target for enhancing cognitive function.
Dr.Camel's Conclusion
This research points toward a potential oasis in the desert of cognitive impairments associated with schizophrenia, suggesting that targeting the M1 receptor could lead to the development of new antipsychotic drugs that not only control psychotic symptoms but also enhance cognitive function.
Date :
- Date Completed 2020-12-21
- Date Revised 2020-12-21
Further Info :
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English
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