Optimization of a Green Extraction Technique for Kratom (Ketum) Leaf Extract via Accelerated Solvent Extraction: Phytochemical Profiles, Cytotoxicity, and Antinociceptive Activity [0.03%]
一种绿色提取技术的优化:采用加速溶剂萃取法提取 kratom(克特姆)叶提取物及其植物化学成分、细胞毒性和抗痛觉作用研究
Nurul Najwa Rusmadi,Thiruventhan Karunakaran,Faiqah Ramli et al.
Nurul Najwa Rusmadi et al.
Kratom (Mitragyna speciosa Korth.) has gained increasing scientific interest for its potential in pain management and addiction treatment. This study employs a green chemistry approach to optimize the extraction of kratom leaves by using Ac...
Evaluation of the Relationship between Vesicular Monoamine Transporter 2 (VMAT2) Inhibition and Neurologic Adverse Events in Approved Drugs [0.03%]
评估已批准药物中-vesicular单胺转运蛋白2(VMAT2)抑制与神经不良事件之间的关系
Rebecca Racz,Laura B Kozell,Amy J Eshleman et al.
Rebecca Racz et al.
Vesicular monoamine transporter 2 (VMAT2) is an internal membrane protein found predominantly in the central nervous system that plays an integral role in the transport of biogenic monoamines (e.g., dopamine, serotonin, and norepinephrine) ...
Deciphering Opioid Peptide Binding Modes at Atypical Chemokine Receptor 3 [0.03%]
阿片肽在非典型趋化因子受体3上的结合模式解析
Friederike Wunsch,Ester Cassano,Kristina Puls et al.
Friederike Wunsch et al.
ACKR3 is a class A G protein-coupled receptor that is considered as an atypical chemokine receptor. It does not activate G proteins but efficiently recruits β-arrestin and mediates ligand internalization and was thus proposed as a scavenge...
Digital Twin Modeling for Acanthamoeba Keratitis: From Empirical Therapy to Predictive Ophthalmology [0.03%]
阿卡纳氏amoeba角膜炎的数字孪生模型构建:从经验治疗到预测型眼科医学
Ruqaiyyah Siddiqui,Naveed Ahmed Khan
Ruqaiyyah Siddiqui
Acanthamoeba keratitis is a rare, vision-threatening corneal infection that remains difficult to diagnose and treat, with therapy often extending for many months. Despite recent advances, the management of Acanthamoeba keratitis still depen...
Neuronal Organoid Engineering and Disease-Focused High-Throughput Neuropharmacology: Advances, Limitations, and Translational Strategies [0.03%]
神经元器官体工程和疾病导向的高通量药物筛选研究:进展、局限性和转化策略
Bahareh Farasati Far,Kimia Omidvar,Ehsan Heidari et al.
Bahareh Farasati Far et al.
Although animal models offer the physiology of the entire organism, various cell populations, and circuit-level behaviors, their predictive ability for polygenic neuropsychiatric disorders may be limited by species-specific neurodevelopment...
Prediction of Monoclonal Antibodies Pharmacokinetics in Human: Identification of a Reference Neonatal Fc Receptor (FcRn) Binding Affinity Using Physiologically Based Pharmacokinetic (PBPK) Modeling [0.03%]
基于生理的药代动力学(PBPK)模型预测人用单克隆抗体药代动力学:使用生理学基础的药代动力学(PBPK)模型鉴定参考新生儿Fc受体(FcRn)结合亲和力
Salih Benamara,Erik Sjögren,Florence Gattacceca et al.
Salih Benamara et al.
Prediction of monoclonal antibody (mAb) pharmacokinetics (PK) in drug development remains challenging due to the lack of a standardized method for predicting elimination based on mechanistic pathways. Among the processes implemented in the ...
Protease-Activated Receptor 4 (PAR4)-Tethered Ligand Antagonists Demonstrate Thrombin Liability [0.03%]
新型血栓形成药剂的潜在危险性:蛋白酶激活受体4(PAR4)肽类拮抗剂引起凝血酶反应性增强
Emma M Webb,Jackson B Cassada,Heidi E Hamm
Emma M Webb
The Hamm laboratory recently published a cohort of PAR4 antagonists that were effective against the tethered ligand activation of PAR4. These compounds were generated from an ultralarge virtual screen using a homology model of PAR4. Upon fu...
Puhan Zhao,Hong Fang,Bahaa Elgendy et al.
Puhan Zhao et al.
Estrogen-related receptors (ERRs) are orphan nuclear receptors critical to the regulation of energy metabolism, mitochondrial biogenesis, and tissue-specific transcriptional programs. This review provides a comprehensive structural analysis...
Potent Competitive Inhibitors of Ecto-5'-nucleotidase (CD73) based on 6‑(Het)aryl-7-deazapurine Ribonucleoside 5'‑ O‑Bisphosphonates [0.03%]
一类基于6-(杂芳基)-7-脱氮鸟嘌呤核糖核苷5'-O-双磷酸酯的强效的针对CD73(ecto-5'-核苷酸酶)的竞争性抑制剂
Ugnė Šinkevičiu̅tė,Magdalena Šímová,Radek Staník et al.
Ugnė Šinkevičiu̅tė et al.
CD73 generates immunosuppressive adenosine in the tumor microenvironment and is a promising target for cancer immunotherapy. We have designed and systematically studied diverse 2-substituted 7-deazapurine ribonucleoside 5'-O-bisphosphonates...
Preclinical Characterization of Vindeburnol: Pharmacokinetics, Safety, and Cognitive-Enhancing Properties [0.03%]
vindeburnol的药代动力学、安全性和提高认知功能的特性的确证研究
Lyudmila Borets,Tatyana Azhikina,Eugene Zubkov et al.
Lyudmila Borets et al.
Cognitive impairment is a common symptom of many psychiatric disorders and can significantly reduce the patients' quality of life. Vindeburnol, a synthetic derivative of eburnamine-vincamine alkaloids, has shown potential in models of depre...