Discovery of VU6053371/BI03738809: A First-in-Class Selective and CNS-Penetrant mGlu3 Positive Allosteric Modulator (PAM) with Efficacy in a Preclinical Cognition Model [0.03%]
VU6053371/BI03738809的发现：一种新型且能透过中枢神经系统的高选择性mGlu3正向别构调节剂(PAM)，并在治疗认知障碍疾病的临床前模型中表现出疗效
Caleb A Jones,Renn A Duncan,Kristen M Gilliland et al.
Caleb A Jones et al.
Herein, we report the discovery and development of the first-in-class (FIC), selective, and centrally active metabotropic glutamate receptor subtype 3 (mGlu3) positive allosteric modulator (PAM), VU6053371/BI03738809. A high-throughput scre...
Targeted Mutations Activate Allosteric Modulation of α5-Containing Nicotinic Acetylcholine Receptors [0.03%]
靶向突变激活α5型烟碱乙酰胆碱受体的别构调节作用
Christopher B Marotta,Henry A Lester,Dennis A Dougherty
Christopher B Marotta
Nicotinic acetylcholine receptors play vital roles in neuronal communication. The α5 subunit is unique, in that it assembles only into the auxiliary position (the "5th" subunit of the pentamer) of a functional receptor, yet it can have a s...
Adinath Markad,Taiba Nafis,Ashutosh Kumar Dubey et al.
Adinath Markad et al.
Chronic pain typically develops in situations such as tissue injury, inflammation, and ischemia, where extracellular acidity increases in the altered microenvironment. Acid-sensing ion channels (ASICs) are proton-gated membrane proteins tha...
Peptide-Based Delivery Systems: Selected Insights into Cell-Penetrating Peptides [0.03%]
基于肽的递送系统：细胞穿透肽的部分见解
Hussan Adam,Sara Abdollahi,Othman Al Musaimi
Hussan Adam
The blood-brain barrier (BBB) is a highly selective biological interface that regulates molecular transport between the bloodstream and the central nervous system (CNS). Its primary function is to protect the brain from harmful substances w...
Lipid Droplet-Accumulating Microglia as a Therapeutic Node in Neurodegenerative Disease [0.03%]
神经退行性疾病治疗中的蓄脂小胶质细胞节点疗法
Siqi Guo,Qingyu Zhang,Rui Guo et al.
Siqi Guo et al.
Neurodegenerative disorders increasingly reflect failures of cellular state control rather than the linear accumulation of a single toxic lesion. Microglia become trapped in maladaptive states in which inflammatory activation is decoupled f...
Glucose-Dependent Insulinotropic Polypeptide Receptors Are Expressed in the Lateral Septum and Reduce Electrically-Evoked Dopamine Release as well as the Ability of Cocaine to Increase Extracellular Dopamine [0.03%]
葡萄糖依赖性胰岛素分泌多肽受体在侧隔核的表达及其减少电诱发多巴胺释放和可卡因诱导的多巴胺升高的作用
Anna Marie Buchanan,Sonja Virkus,N Dalton Fitzgerald et al.
Anna Marie Buchanan et al.
Tirzepatide, a dual agonist of the glucagon-like peptide 1 receptor (GLP-1R) and glucose-dependent insulinotropic polypeptide receptor (GIPR), represents a new class of medication for obesity and type II diabetes treatment. Using laboratory...
Cu(ATSM) Restores Blood-Brain Barrier Abundance of P-Glycoprotein and Improves Cognitive Function in the APP/PS1 Mouse Model of Alzheimer's Disease [0.03%]
Cu（ATSM）恢复APP / PS1阿尔茨海默氏病小鼠模型血脑屏障中P-糖蛋白的丰富性并改善认知功能
Jae Pyun,Asif Noor,Pranav Runwal et al.
Jae Pyun et al.
Alzheimer's disease (AD) is a prevalent neurodegenerative disorder characterized by the accumulation of amyloid-beta (Aβ) peptides in the brain. P-glycoprotein (P-gp), a key efflux transporter at the blood-brain barrier (BBB), plays a cruc...
Caffeic Acid Ameliorates l-Methionine-Induced Hyperhomocysteinemia, Leading to Decreased Adult Neurogenesis and Oxidative Stress Status in Adult Rats [0.03%]
咖啡酸改善l-蛋氨酸诱导的高同型半胱氨酸血症，减少成年大鼠神经发生和氧化应激状况
Oabnithi Dornlakorn,Apiwat Sirichoat,Wanassanan Pannangrong et al.
Oabnithi Dornlakorn et al.
Chronic l-methionine (l-met) treatment induces hyperhomocysteinemia, which impairs neurogenesis and memory by increasing oxidative stress. Caffeic acid (CA) possesses antioxidant properties that reduce brain oxidative damage and promote neu...
Targeting 5-HT7 Receptor with Biased Ligands to Alleviate Pain and Spinal Neuroinflammation [0.03%]
偏向性激活5-羟色胺7型受体以缓解疼痛和脊髓神经炎症
Fahima Madouri,Cyril Guimpied,Enora Pigeon et al.
Fahima Madouri et al.
The serotonin 5-HT7 receptor (5-HT7R), a member of the rhodopsin-like family of G protein-coupled receptors (GPCRs), is highly expressed in the central nervous system (CNS) and represents a promising target for treating CNS disorders such a...
Xerogel-Engineered Graphitic Carbon Nitride Interfaces Enable Aptamer-Based Detection of Salivary Lactoferrin for Noninvasive Diagnosis of Alzheimer's Disease [0.03%]
用于无创诊断阿尔茨海默病的唾液转铁蛋白适配子检测的气凝胶石墨碳氮化物界面
Bivas Talukdar,Damini Verma,Gopinath Packirisamy
Bivas Talukdar
Alzheimer's disease (AD), the primary cause of dementia, is a progressive neurodegenerative disorder that requires early diagnosis using noninvasive biosensing strategies. Salivary lactoferrin has consequently emerged as a compelling early-...