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

Scaffold Hopping to Imidazo[1,2-a]pyrazin-8-one Positive Allosteric Modulators of Metabotropic Glutamate 2 Receptor

骨架跃迁至咪唑并[1,2-a]吡嗪-8-酮代谢型谷氨酸受体2正变构调节剂

de Lucas, Ana I; Vega, Juan A; García Molina, Aránzazu; Linares, María Lourdes; Tresadern, Gary; Lavreysen, Hilde; Oehlrich, Daniel; Trabanco, Andrés A; Cid, José M

Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization

代谢型谷氨酸受体2的共价变构探针:设计、合成和药理学表征

Doornbos, Maarten L J; Wang, Xuesong; Vermond, Sophie C; Peeters, Luc; Pérez-Benito, Laura; Trabanco, Andrés A; Lavreysen, Hilde; Cid, José María; Heitman, Laura H; Tresadern, Gary; IJzerman, Adriaan P

Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia

对6,7-二氢吡唑并[1,5-a]吡嗪-4-酮衍生物作为一类新型mGlu5受体正向变构调节剂的初步研究,该类化合物在精神分裂症的临床前模型中显示出疗效

Conde-Ceide, Susana; Alcázar, Jesús; Alonso de Diego, Sergio A; López, Silvia; Martín-Martín, María Luz; Martínez-Viturro, Carlos M; Pena, Miguel-Angel; Tong, Han Min; Lavreysen, Hilde; Mackie, Claire; Bridges, Thomas M; Daniels, J Scott; Niswender, Colleen M; Jones, Carrie K; Macdonald, Gregor J; Steckler, Thomas; Conn, P Jeffrey; Stauffer, Shaun R; Lindsley, Craig W; Bartolomé-Nebreda, José Manuel

mGlu2 Receptor Agonism, but Not Positive Allosteric Modulation, Elicits Rapid Tolerance towards Their Primary Efficacy on Sleep Measures in Rats

mGlu2受体激动剂(而非正向变构调节剂)可迅速引起大鼠对其睡眠指标主要疗效的耐受性。

Ahnaou, Abdallah; Lavreysen, Hilde; Tresadern, Gary; Cid, Jose M; Drinkenburg, Wilhelmus H

Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5)

发现并研究新型咪唑并嘧啶酮和二氢咪唑并嘧啶酮类化合物作为代谢型谷氨酸受体5 (mGlu5) 正向变构调节剂的构效关系

Martín-Martín, María Luz; Bartolomé-Nebreda, José Manuel; Conde-Ceide, Susana; Alonso de Diego, Sergio A; López, Silvia; Martínez-Viturro, Carlos M; Tong, Han Min; Lavreysen, Hilde; Macdonald, Gregor J; Steckler, Thomas; Mackie, Claire; Bridges, Thomas M; Daniels, J Scott; Niswender, Colleen M; Noetzel, Meredith J; Jones, Carrie K; Conn, P Jeffrey; Lindsley, Craig W; Stauffer, Shaun R

Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound

mGlu5 PAM 临床候选药物 VU0409551/JNJ-46778212 的进一步优化:备选化合物的进展与挑战

Zhou, Ya; Malosh, Chrysa; Conde-Ceide, Susana; Martínez-Viturro, Carlos Manuel; Alcázar, Jesus; Lavreysen, Hilde; Mackie, Claire; Bridges, Thomas M; Daniels, J Scott; Niswender, Colleen M; Jones, Carrie K; Macdonald, Gregor J; Steckler, Thomas; Conn, P Jeffrey; Stauffer, Shaun R; Bartolomé-Nebreda, José Manuel; Lindsley, Craig W

Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators

酰基二氢吡唑并[1,5-a]嘧啶酮作为代谢型谷氨酸受体5正向变构调节剂

Malosh, Chrysa; Turlington, Mark; Bridges, Thomas M; Rook, Jerri M; Noetzel, Meredith J; Vinson, Paige N; Steckler, Thomas; Lavreysen, Hilde; Mackie, Claire; Bartolomé-Nebreda, José M; Conde-Ceide, Susana; Martínez-Viturro, Carlos M; Piedrafita, María; Sánchez-Casado, M Rosa; Macdonald, Gregor J; Daniels, J Scott; Jones, Carrie K; Niswender, Colleen M; Conn, P Jeffrey; Lindsley, Craig W; Stauffer, Shaun R

Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₠).

四氢萘啶和二氢萘啶酮醚作为代谢型谷氨酸受体 5 (mGluâ‚) 的正向变构调节剂

Turlington Mark, Malosh Chrysa, Jacobs Jon, Manka Jason T, Noetzel Meredith J, Vinson Paige N, Jadhav Satyawan, Herman Elizabeth J, Lavreysen Hilde, Mackie Claire, Bartolomé-Nebreda José M, Conde-Ceide Susana, Martín-Martín M Luz, Tong Han Min, López Silvia, MacDonald Gregor J, Steckler Thomas, Daniels J Scott, Weaver C David, Niswender Colleen M, Jones Carrie K, Conn P Jeffrey, Lindsley Craig W, Stauffer Shaun R

Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency

发现并研究了一系列新型代谢型谷氨酸受体5正向变构调节剂的构效关系及其配体效率

Turlington, Mark; Noetzel, Meredith J; Bridges, Thomas M; Vinson, Paige N; Steckler, Thomas; Lavreysen, Hilde; Mackie, Claire; Bartolomé-Nebreda, José M; Conde-Ceide, Susana; Tong, Han Min; Macdonald, Gregor J; Daniels, J Scott; Jones, Carrie K; Niswender, Colleen M; Conn, P Jeffrey; Lindsley, Craig W; Stauffer, Shaun R

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.

二氢噻唑并吡啶酮衍生物作为代谢型谷氨酸 5 (mGlu5) 受体的一类新型正向变构调节剂

Bartolomé-Nebreda José Manuel, Conde-Ceide Susana, Delgado Francisca, Iturrino Laura, Pastor Joaquín, Pena Miguel Ángel, Trabanco Andrés A, Tresadern Gary, Wassvik Carola M, Stauffer Shaun R, Jadhav Satyawan, Gogi Kiran, Vinson Paige N, Noetzel Meredith J, Days Emily, Weaver C David, Lindsley Craig W, Niswender Colleen M, Jones Carrie K, Conn P Jeffrey, Rombouts Frederik, Lavreysen Hilde, Macdonald Gregor J, Mackie Claire, Steckler Thomas