Molecular Pharmacology of Selective NaV1.6 and Dual NaV1.6/NaV1.2 Channel Inhibitors that Suppress Excitatory Neuronal Activity Ex Vivo [0.03%]
选择性抑制Nav1.6和双重Nav1.6/Nav1.2通道抑制兴奋性神经元活性的分子药理学研究
Samuel J Goodchild,Noah Gregory Shuart,Aaron D Williams et al.
Samuel J Goodchild et al.
Voltage-gated sodium channel (NaV) inhibitors are used to treat neurological disorders of hyperexcitability such as epilepsy. These drugs act by attenuating neuronal action potential firing to reduce excitability in the brain. However, all ...
Mass Spectrometric Imaging of Anionic Phospholipids Desorbed from Human Hippocampal Sections: Discrimination between Temporal and Nontemporal Lobe Epilepsies [0.03%]
人类海马切片中阴离子磷脂的质谱成像：区分颞叶癫痫和非颞叶癫痫
Supratim Mondal,Abhijit Nandy,Geetha Dande et al.
Supratim Mondal et al.
Temporal lobe epilepsy (TLE) is one of the most common neurological disorders, often accompanied by hippocampal sclerosis. The molecular processes underlying this epileptogenesis are poorly understood. To examine the lipid profile, 39 fresh...
In Vitro Functional Profiling of Fentanyl and Nitazene Analogs at the μ-Opioid Receptor Reveals High Efficacy for Gi Protein Signaling [0.03%]
芬太尼和利坦佐烯类似物在μ-阿片受体的体外功能分析揭示了Gi蛋白信号传导的高度功效
Meng-Hua M Tsai,Li Chen,Michael H Baumann et al.
Meng-Hua M Tsai et al.
Novel synthetic opioids (NSOs), including both fentanyl and non-fentanyl analogs that act as μ-opioid receptor (MOR) agonists, are associated with serious intoxication and fatal overdose. Previous studies proposed that G-protein-biased MOR...
Omega-3 and -6 Fatty Acids Alter the Membrane Lipid Composition and Vesicle Size to Regulate Exocytosis and Storage of Catecholamines [0.03%]
Omega-3和-6脂肪酸通过改变膜脂成分和囊泡大小来调节儿茶酚胺的外排和储存
Chaoyi Gu,Mai H Philipsen,Andrew G Ewing
Chaoyi Gu
The two essential fatty acids, alpha-linolenic acid and linoleic acid, and the higher unsaturated fatty acids synthesized from them are critical for the development and maintenance of normal brain functions. Deficiencies of these fatty acid...
Transient Adenosine Modulates Serotonin Release Indirectly in the Dorsal Raphe Nuclei [0.03%]
腺苷对中缝背核5-羟色胺释放的间接调控作用
Kailash Shrestha,B Jill Venton
Kailash Shrestha
Rapid adenosine transiently regulates dopamine and glutamate via A1 receptors, but other neurotransmitters, such as serotonin, have not been studied. In this study, we examined the rapid modulatory effect of adenosine on serotonin release i...
New Alpha9 nAChR Ligands Based on a 5-(Quinuclidin-3-ylmethyl)-1,2,4-oxadiazole Scaffold [0.03%]
基于5-(喹尼克啶-3-基甲基)-1,2,4-氧杂二唑骨架的新Alpha9 nAChR配体
Clelia Dallanoce,Katrin Richter,Clare Stokes et al.
Clelia Dallanoce et al.
Several lines of evidence have indicated that nicotinic acetylcholine receptors (nAChR) that contain α9 subunits, probably in combination with α10 subunits, may be valuable targets for the management of pain associated with inflammatory d...
Design, Synthesis, and Biological Investigation of Quinazoline Derivatives as Multitargeting Therapeutics in Alzheimer's Disease Therapy [0.03%]
喹唑啉衍生物作为阿尔茨海默病多靶向治疗药物的设计、合成及生物学研究
Akash Verma,Digambar Kumar Waiker,Neha Singh et al.
Akash Verma et al.
An efficient and promising method of treating complex neurodegenerative diseases like Alzheimer's disease (AD) is the multitarget-directed approach. Here in this work, a series of quinazoline derivatives (AV-1 to AV-21) were rationally desi...
Efrat Naaman,Amanda Qarawani,Rony Ben-Zvi Elimelech et al.
Efrat Naaman et al.
Age-related macular degeneration (AMD) is a complex disease in which inflammation is implicated as a key factor but the precise molecular mechanisms are poorly understood. AMD lesions contain an excess of the pro-inflammatory S100A9 protein...
Novel Substituted Pyrimidine Derivatives as Potential Anti-Alzheimer's Agents: Synthesis, Biological, and Molecular Docking Studies [0.03%]
新型取代嘧啶衍生物作为潜在的抗阿尔茨海默症药物：合成、生物及分子对接研究
Swati Pant,Ranjith Kumar K,Preeti Rana et al.
Swati Pant et al.
The most frequent type of age-related dementia is Alzheimer's disease. To discover novel therapeutic agents for Alzheimer's disease, a series of substituted pyrimidine derivatives were synthesized and evaluated for anti-Alzheimer's activity...
High-Resolution NMR Structures of Intrastrand Hairpins Formed by CTG Trinucleotide Repeats [0.03%]
由CTG三核苷酸重复序列形成的链内发卡的高分辨率NMR结构
Liqi Wan,Axin He,Jinxing Li et al.
Liqi Wan et al.
The CAG and CTG trinucleotide repeat expansions cause more than 10 human neurodegenerative diseases. Intrastrand hairpins formed by trinucleotide repeats contribute to repeat expansions, establishing them as potential drug targets. High-res...