Structure-Activity Relationships and Molecular Pharmacology of Positive Allosteric Modulators of the Mu-Opioid Receptor [0.03%]
μ-阿片受体激动剂的构效关系及分子药理学研究
Mengchu Li,Xinmin Gan,Kun Liu et al.
Mengchu Li et al.
Positive allosteric modulation of the mu-opioid receptor is a promising strategy to address the ever-growing problem of acute and chronic pain management. Positive allosteric modulators (PAMs) of the mu-opioid receptor could be employed to ...
Discovery of VU0467319: an M1 Positive Allosteric Modulator Candidate That Advanced into Clinical Trials [0.03%]
VU0467319的发现及其作为临床试验候选药物的M1正向变构调节剂的作用机制研究
Michael S Poslunsey,Michael R Wood,Changho Han et al.
Michael S Poslunsey et al.
Herein we detail the first disclosure of VU0467319 (VU319), an M1 Positive Allosteric Modulator (PAM) clinical candidate that successfully completed a Phase I Single Ascending Dose (SAD) clinical trial. VU319 (16) is a moderately potent M1 ...
Ramya Tokala,Jacob M Hooker
Ramya Tokala
Neuroreceptor mapping provides insights into neurotransmitter changes and receptor dynamics that improve the understanding of brain functions. This Viewpoint highlights the advancements in the development of novel radiotracers (imaging tool...
Guanidine Derivative ADS1017, a Potent Histamine H3 Receptor Antagonist with Promising Analgesic Activity and Satisfactory Safety Profile [0.03%]
具有镇痛作用和良好安全性结构的组胺H３受体拮抗剂ADS1017的研究
Tadeusz Karcz,Katarzyna Szczepańska,Szczepan Mogilski et al.
Tadeusz Karcz et al.
In this study, we selected 12 guanidine derivatives from the previously described ligand library and determined their affinity at histamine H3 and H4 receptors (H3R and H4R, respectively). Moreover, we also checked their intrinsic activity ...
Novel Perspective on Sevoflurane-Induced Cognitive Dysfunction: Implications of Neuronal SIRPα and Microglial Synaptic Remodeling [0.03%]
新型的异氟烷诱导的认知功能障碍的研究视角：神经元SIRPα和小胶质细胞突触重塑的影响
Wei Du,Xiaomin Zhang,Songze Li et al.
Wei Du et al.
This study aims to investigate the role of neuronal SIRPα and microglial synaptic remodeling in sevoflurane-induced cognitive dysfunction in newborn mice. Newborn mice were exposed to sevoflurane, followed by behavioral assessments and sin...
Structural Analysis of Variants of the Ferritin Light Chain Protein and Its Relationship with Neuroferritinopathy [0.03%]
神经铁蛋白病相关的轻链铁蛋白变异体的结构分析
Madelin Gómez Hernández,Alejandro Soto-Ospina,Cristian Andrés Osorio et al.
Madelin Gómez Hernández et al.
Ferritin is a highly conserved spherical protein that stores iron and possesses triple and quadruple symmetry input ports. Additionally, it is composed of light chains that can be affected by post-translational mutations, reducing the iron ...
Serotonin 1A Receptors Modulate Serotonin 2A Receptor-Mediated Behavioral Effects of 5-Methoxy- N, N-dimethyltryptamine Analogs in Mice [0.03%]
五甲氧基-N,N-二甲基色胺类似物对小鼠血清素2A受体介导的行为效应受到血清素1A受体调节
Grant C Glatfelter,Allison A Clark,Natalie G Cavalco et al.
Grant C Glatfelter et al.
5-methoxy-N,N-dimethyltrytpamine (5-MeO-DMT) analogs are used as recreational drugs, but they are also being developed as potential medicines, warranting further investigation into their pharmacology. Here, we investigated the neuropharmaco...
Correction to "Design, Synthesis, and Activity of an α-Conotoxin LtIA Fluorescent Analogue" [0.03%]
"α-康托毒素LtIA荧光类似物的设计、合成及活性研究”的更正
Yishuai Yang,Yao Tan,Dongting Zhangsun et al.
Yishuai Yang et al.
Published Erratum
ACS chemical neuroscience. 2024 Dec 18;15(24):4591. DOI:10.1021/acschemneuro.4c00776 2024
1H NMR-Based Metabolomic Signatures in Rodent Models of Sporadic Alzheimer's Disease and Metabolic Disorders [0.03%]
基于1H NMR的代谢组学谱图在散发性阿尔茨海默病和代谢障碍啮齿类模型中的变化规律
Ananya Shukla,Khushbhu Meena,Ashish Gupta et al.
Ananya Shukla et al.
Alzheimer's disease (AD) is a chronic neurological disorder that impacts the elderly population all over the globe. Evidence suggests association between AD and metabolic disorders such as diabetes mellitus (DM) and obesity (OB). The presen...
Exploring Cimetidine as a Potential Therapeutic Attenuator against Amyloid Formation in Parkinson's Disease: Spectroscopic and Microscopic Insights into Alpha-Synuclein and Human Insulin [0.03%]
西米替丁作为帕金森病潜在治疗减弱剂探究： alpha-突触核蛋白和人体胰岛素形成淀粉样物质的光谱学及显微镜研究见解
Md Nadir Hassan,Azeem Ahmad,Murtaza Hussain et al.
Md Nadir Hassan et al.
Neurodegenerative diseases, notably Alzheimer's and Parkinson's, hallmark their progression through the formation of amyloid aggregates resulting from misfolding. While current therapeutics alleviate symptoms, they do not impede disease ons...