【摘 要】
:
Large-conductance calcium-activated potassium channels(BK channels),widely expressed in various cells and tissues of mammals except myocardial cells,responding to two distinct physiological stimuli,i.
【机 构】
:
Department of Chemistry,Shanghai University,Shanghai 200444
【出 处】
:
第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
Large-conductance calcium-activated potassium channels(BK channels),widely expressed in various cells and tissues 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-7 were possibly essential for the activity.
其他文献
The pharmacophore models of diketo acid derivatives integrase inhibitors have established through camparing the structure,activity and side effects of six diketo acid derivatives which have been appro
RNA interference (RNAi) technology has developed rapidly as a powerful tool for functional genomic analysis and target validation.Due to its potential for highly specific targeted effects in vivo,ther
Robust strategies to rapidly access compound libraries featuring high levels of structural complexity,skeletal diversity and drug-likeness for drug discovery remain in urgent demand.We propose a highl
Introduction of fluorine in organic molecules constitutes a great interest in pharmaceuticals.It can change chemical and physical properties of molecules due to the great stability of C-F bond and lip
Recently,3-iodo-4-phenoxypyridinone derivatives (IOPYs) were identified as a novel class of highly potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) with superior activity against both w
Pyrimidines have been recognized as important heterocyclic compounds due to their diverse biological activities such as HIV-1 inhibitor,antimalarial,antibacterial,anticancer,analgesic,cardiovascular,a
There were several strategies enhancing permeation of gancyclovir (GCV) into the retinal and corneal tissues.These approaches could lead to significant improvement in therapeutic options and efficacy,