【摘 要】
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Large-conductance calcium-activated potassium channels (BK channels), widely expressed in various cells and issues of mammals except myocardial cells, responding to two distinct physiological stimuli,
【机 构】
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Department of Chemistry, Shanghai University, Shanghai 200444
【出 处】
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中国化学会全国第十一届有机合成化学学术研讨会
论文部分内容阅读
Large-conductance calcium-activated potassium channels (BK channels), widely expressed in various cells and issues of mammals except myocardial cells, responding to two distinct physiological stimuli, i.e., changes in membrane voltage and in cytosolic Ca2+ concentration, and may serve as a negative feedback pathway to control ionic homeostasis and cell excitability.Agents that open these channels could have profound impacts on diseases such as acute stroke,epilepsy, asthma, and bladder overactivity.Preliminary research showed dehydroabietic acid (DHAA, 1) derivatives had the potential biological activities in opening BK channels.Structure-activity relationship (SAR) studies have also revealed that the 4-carboxyl group was necessary for the activity as the BK channel opener and the substituents of C-12 were possibly essential for the activity.Therefore, we devoted a great deal of efforts to screen 12-substitued oxime and oxime ether derivatives from dehydroabietic acid, aiming at obtaining new bioactive compounds with stronger activities.These analogues may not only help to elucidate the mechanism of action of BK channels in physiological and pathological conditions, but also lay the foundation for the drug researches on the treatment of cardiovascular and cerebrovascular diseases.
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