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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