Identification and In Vivo Evaluation of Myelination Agent PIPE-3297, a Selective Kappa Opioid Receptor Agonist Devoid of β-Arrestin-2 Recruitment Efficacy [0.03%]
髓鞘形成剂PIPE-3297的识别及其体内评估，作为一种选择性κ阿片受体激动剂且无β arrestin-2募集功效
Thomas O Schrader,Kym I Lorrain,Didier Bagnol et al.
Thomas O Schrader et al.
Structure-activity relationship studies led to the discovery of PIPE-3297, a fully efficacious and selective kappa opioid receptor (KOR) agonist. PIPE-3297, a potent activator of G-protein signaling (GTPγS EC50 = 1.1 nM, 91% Emax), did not...
In Vivo Two-Photon Microscopy Reveals Sensory-Evoked Serotonin (5-HT) Release in Adult Mammalian Neocortex [0.03%]
活体双光子显微镜揭示了成年哺乳动物新皮层中感觉驱动的血清素(5-HT)释放
Gabriel Ocana-Santero,Adam M Packer,Trevor Sharp et al.
Gabriel Ocana-Santero et al.
The recent development of genetically encoded fluorescent neurotransmitter biosensors has opened the door to recording serotonin (5-hydroxytryptamine, 5-HT) signaling dynamics with high temporal and spatial resolution in vivo. While this re...
Effect of Bulky N-Dibenzofuranylmethyl Substitution on the 5-HT2 Receptor Affinity and Efficacy of a Psychedelic Phenethylamine [0.03%]
大体积N-二苯并呋喃甲基取代对迷幻苯乙胺的5-HT2受体亲和力和效力的影响
Breno A Soares,Thirumal Yempala,Darío Martínez-Afani et al.
Breno A Soares et al.
The introduction of arylmethyl substituents on the amine nitrogen atom of phenethylamines and tryptamines often results in profound increases in their affinity and functional activity at 5-HT2 serotonin receptors. To probe the sensitivity o...
Decoding the Parkinson's Symphony: PARIS, Maestro of Transcriptional Regulation and Metal Coordination for Dopamine Release [0.03%]
破译帕金森氏症的交响乐：PARIS，在多巴胺释放中的转录调控和金属配位的指挥家
Yunha Hwang,Abul Kasem Mohammad Mydul Islam,Seongmin Park et al.
Yunha Hwang et al.
Parkin interacting substrate (PARIS) is a pivotal transcriptional regulator in the brain that orchestrates the activity of various enzymes through its intricate interactions with biomolecules, including nucleic acids. Notably, the binding o...
Identification of a Novel Subtype-Selective α1B-Adrenoceptor Antagonist [0.03%]
新型亚型选择性α1B-肾上腺素受体拮抗剂的鉴定
Alaa Abdul-Ridha,Lazarus A de Zhang,Ashenafi Haileyesus Betrie et al.
Alaa Abdul-Ridha et al.
α1A-, α1B-, and α1D-adrenoceptors (α1-ARs) are members of the adrenoceptor G protein-coupled receptor family that are activated by adrenaline (epinephrine) and noradrenaline. α1-ARs are clinically targeted using antagonists that have m...
Louis G Mueller,Barbara S Slusher,Takashi Tsukamoto
Louis G Mueller
The discovery and development of drugs to treat diseases of the nervous system remains challenging. There is a higher attrition rate in the clinical stage for nervous system experimental drugs compared to other disease areas. In the preclin...
Brain Glutamate Dynamics Predict Positive Agency in Healthy Women: Insights from Combined Application of Pharmacological Challenge, Comprehensive Affective Assessment, and Magnetic Resonance Spectroscopy [0.03%]
大脑谷氨酸动态预测健康女性的积极机构：药物挑战、综合情感评估和磁共振波谱成像的结合应用带来的启示
Tara L White,Meghan A Gonsalves,Ashley D Harris et al.
Tara L White et al.
Contributions of brain glutamate (Glu) to conscious emotion are not well understood. Here, we evaluate the relationship of experimentally induced change in neocortical Glu (ΔGlu) and subjective states in well individuals, using combined ap...
Molecular Insights into the Dynamics of Amyloid Fibril Growth: Elongation and Lateral Assembly of GNNQQNY Protofibrils [0.03%]
淀粉样原纤维生长的动力学分子研究：GNNQQNY 原纤维的延长和侧向组装
Torsten John,Aldo Rampioni,David Poger et al.
Torsten John et al.
The self-assembly of peptides and proteins into β-sheet rich amyloid fibrils is linked to both functional and pathological states. In this study, the growth of fibrillar structures of the short peptide GNNQQNY, a fragment from the yeast pr...
Determining Structural Changes for Ligand Recognition between Human and Rat Phosphorylated BACE1 in Silico and Its Phosphorylation by GSK3β at Thr252 by in Vitro Studies [0.03%]
通过计算模拟确定人和大鼠磷酸化BACE1在配体识别中的结构变化及其通过体外研究在Thr252处的GSK3β磷酸化
Jazziel Velazquez Toledano,Martiniano Bello,José Correa Basurto et al.
Jazziel Velazquez Toledano et al.
Alzheimer's disease (AD) is a neurodegenerative disease affecting older adults. AD pathogenesis involves the production of the highly neurotoxic amyloid-β peptide 1-42 (Aβ1-42) from β-site amyloid precursor protein cleaving enzyme 1 (BAC...
Antidepressant-like Effect of the Eburnamine-Type Molecule Vindeburnol in Rat and Mouse Models of Ultrasound-Induced Depression [0.03%]
伊贝卡品类化合物Vindeburnol对超声诱导抑郁大鼠和小鼠模型的抗抑郁样作用
Eugene Zubkov,Olga Riabova,Yana Zorkina et al.
Eugene Zubkov et al.
Vindeburnol (VIND, RU24722, BC19), a synthetic molecule derived from the eburnamine-vincamine alkaloid group, has many neuropsychopharmacological effects, but its antidepressant-like effects are poorly understood and have only been describe...