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The putative cognitive enhancer KA‐672. HCl is an uncompetitive voltage‐dependent NMDA receptor antagonist

 

作者: Polina Lishko,   Oleksandr Maximyuk,   Shyam Chatterjee,   Michael Nöldner,   Oleg Krishtal,  

 

期刊: NeuroReport  (OVID Available online 1998)
卷期: Volume 9, issue 18  

页码: 4193-4197

 

ISSN:0959-4965

 

年代: 1998

 

出版商: OVID

 

关键词: Alzheimer's disease;Concentration clamp;Dementia;Hippocampal neurons;Neuroprotection;NMDA receptor antagonist;KA-672.HCl

 

数据来源: OVID

 

摘要:

KA-672.HCl (KA-672) is a new substance demonstrating anti-dementia properties. It shows modulatory effects on several neurotransmitter systems known to be affected in patients with Alzheimer's disease. In this study the action of KA-672 on the NMDA receptors was examined by applying patch clamp techniques to acutely isolated hippocampal neurons. KA-672 antagonizes NMDA responses in a voltage-dependent manner. At a holding potential of 90 mV the IC50value for the blocking action of KA-672 was 20 ± 7 μM. This action of KA-672 is independent on the concentration either of agonist or coagonist of NMDA receptor. Ketamine, which interacts with the PCP center, does not occlude the action of KA-672. Evidently, KA-672.HCl is a weak NMDA receptor-operated channel blocker. This property may account for its pharmacological profile.

 

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