日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

Drug Repurposing: Conversion of the Peripherally Restricted HIV Protease Inhibitor Amprenavir to Potent, Selective, and CNS-Penetrant Agonists for the Cannabinoid Receptor 2

药物再利用:将外周限制性 HIV 蛋白酶抑制剂安普那韦转化为强效、选择性强且能穿透血脑屏障的大麻素受体 2 激动剂

Haymer, Daniel H; Duncan, Renn A; Rodriguez, Alice L; Han, Allie; Lindsay, Richard J; Wijesiri, N Kithmini; Thompson Gray, Analisa; Krishnan, Srinivasan; Qi, Aidong; Brown, Benjamin P; Boutaud, Olivier; Engers, Darren W; Jones, Carrie K; Niswender, Colleen M; Lindsley, Craig W; Bender, Aaron M

Shank3 modulates Rpl3 expression and protein synthesis via mGlu5: implications for Phelan McDermid syndrome.

Shank3 通过 mGlu5 调节 Rpl3 表达和蛋白质合成:对 Phelan McDermid 综合征的意义

Giona Federica, Beretta Stefania, Zippo Antonio, Stefanoni Alessia, Tomasoni Zaira, Vicidomini Cinzia, Ponzoni Luisa, Sala Mariaelvina, Jones Carrie K, Conn P Jeffrey, Boeckers Tobias M, Sala Carlo, Verpelli Chiara

Safety, tolerability, pharmacokinetic and pharmacodynamic effects of the muscarinic M(1) positive allosteric modulator VU0467319 for Alzheimer's disease: a single ascending-dose study in healthy participants

毒蕈碱M(1)正向变构调节剂VU0467319治疗阿尔茨海默病的安全性、耐受性、药代动力学和药效学效应:一项在健康受试者中进行的单次递增剂量研究

Conley, Alexander C; Key, Alexandra P; Blackford, Jennifer U; Russell, Jason K; Albert, Kimberly M; Gong, Xuewen; Bubser, Michael; Rook, Jerri M; Conn, P Jeffrey; Lindsley, Craig W; Jones, Carrie K; Newhouse, Paul A

Optimization of Selective and CNS Penetrant Alkyne-Based TREK Inhibitors: The Discovery and Characterization of ONO-9517601 (VU6022856) and ONO-7927846 (VU6024391)

选择性和中枢神经系统渗透性炔基TREK抑制剂的优化:ONO-9517601 (VU6022856) 和 ONO-7927846 (VU6024391) 的发现和表征

Tanaka, Motoyuki; Sekioka, Yoko; Hashimoto, Gakuji; Mori, Takahiro; Shono, Tomoyuki; Isaji, Yuuki; Hisaichi, Katsuya; Childress, Elizabeth S; Bollinger, Sean; Schmitt, Joza A; Chopko, Trevor C; Garrison, Aaron T; Perry, Charles K; Chronister, Keagan; Kramer, Meghan; Chang, Sichen; Watson, Katherine J; Dickerson, Jonathan W; Bubser, Michael; Rook, Jerri M; Jones, Carrie K; Boutaud, Olivier; Bridges, Thomas M; Denton, Jerod S; Engers, Darren W; Kurata, Haruto; Lindsley, Craig W

Discovery of a Novel sp(3)‑Rich M(1) Positive Allosteric Modulators (PAMs) Chemotype via Scaffold Hopping

通过骨架跃迁发现一种新型富含sp(3)杂环的M(1)正变构调节剂(PAM)化学类型

Bungard, Joseph D; Spearing, Paul; Nishio, Yu; Rathnayake, Upendra; Presley, Chris C; Chang, Sichen; Kling, Haley E; Thompson, Analisa D; Cho, Hyekyung P; Peng, Li; Rodriguez, Alice L; Niswender, Colleen M; Boutaud, Olivier; Kramlinger, Valerie; Jones, Carrie K; Conn, P Jeffrey; Engers, Julie L; Engers, Darren W; Lindsley, Craig W; Han, Changho

Discovery of VU0467319: an M(1) Positive Allosteric Modulator Candidate That Advanced into Clinical Trials

VU0467319 的发现:一种进入临床试验的 M(1) 正向变构调节剂候选药物

Poslunsey, Michael S; Wood, Michael R; Han, Changho; Stauffer, Shaun R; Panarese, Joseph D; Melancon, Bruce J; Engers, Julie L; Dickerson, Jonathan W; Peng, Weimin; Noetzel, Meredith J; Cho, Hyekyung P; Rodriguez, Alice L; Hopkins, Corey R; Morrison, Ryan; Crouch, Rachel D; Bridges, Thomas M; Blobaum, Anna L; Boutaud, Olivier; Daniels, J Scott; Kates, Michael J; Castelhano, Arlindo; Rook, Jerri M; Niswender, Colleen M; Jones, Carrie K; Conn, P Jeffrey; Lindsley, Craig W

Discovery of VU6052254: A Novel, Potent M(1) Positive Allosteric Modulator

VU6052254 的发现:一种新型、强效的 M(1) 正向变构调节剂

Engers, Julie L; Bungard, Joseph D; Presley, Christopher C; Zagol-Ikapitte, Irene; Watson, Katherine J; Chang, Sichen; O'Carroll, Colin; Dey, P Markus; Burstein, Ethan S; Dickerson, Jonathan W; Thompson Gray, Analisa; Bubser, Michael; Rook, Jerri M; Cho, Hyekyung P; Kramlinger, Valerie M; Boutaud, Olivier; Jones, Carrie K; Conn, P Jeffrey; Engers, Darren W; Lindsley, Craig W

Highly Potent and Subtype-Selective Sperm-Specific Potassium Channel SLO3 Inhibitors Display High Tissue Exposure in the Murine Female Reproductive Tract

高效且具有亚型选择性的精子特异性钾通道SLO3抑制剂在小鼠雌性生殖道中表现出高组织暴露量

Temple, Kayla J; Li, Ping; McKinnie, Hallie G; Thompson Gray, Analisa; Bertron, Jeanette L; Ringuette, Anna E; de Andrade Horn, Pedro; Lyon, Maximilian D; Bhagwat, Shweta; Asadi, Leila; Li, Sophia; Lazarenko, Roman M; McCarthy, Ronald; Chang, Sichen; Turkett, Jeremy A; Kramlinger, Valerie; Watson, Katherine J; Zagol-Ikapitte, Irene A; Denton, Jerod S; Santi, Celia M; Jones, Carrie K; Lindsley, Craig W; Boutaud, Olivier

Safety, Tolerability, Pharmacokinetic and Pharmacodynamic Effects of the Muscarinic M 1 Positive Allosteric Modulator VU0467319 for Alzheimer's disease: A Single Ascending-Dose Study in Healthy Participants

毒蕈碱M1正向变构调节剂VU0467319治疗阿尔茨海默病的安全性、耐受性、药代动力学和药效学效应:一项在健康受试者中进行的单次递增剂量研究

Conley, Alexander C; Key, Alexandra P; Blackford, Jennifer U; Russell, Jason K; Albert, Kimberly M; Gong, Xuewen; Bubser, Michael; Rook, Jerri M; Conn, P Jeffrey; Lindsley, Craig W; Jones, Carrie K; Newhouse, Paul A

Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M(5) Muscarinic Acetylcholine Receptor

VU6036864 的开发:一种基于三唑并吡啶的高质量 M(5) 毒蕈碱乙酰胆碱受体拮抗剂工具化合物

Li, Jinming; Orsi, Douglas L; Engers, Julie L; Long, Madeline F; Capstick, Rory A; Maurer, Mallory A; Presley, Christopher C; Vinson, Paige N; Rodriguez, Alice L; Han, Allie; Cho, Hyekyung P; Chang, Sichen; Jackson, Megan; Bubser, Michael; Blobaum, Anna L; Boutaud, Olivier; Nader, Michael A; Niswender, Colleen M; Conn, P Jeffrey; Jones, Carrie K; Lindsley, Craig W; Han, Changho