التفاصيل البيبلوغرافية
| العنوان: |
Discovery of VU6028418: A Highly Selective and Orally Bioavailable M 4 Muscarinic Acetylcholine Receptor Antagonist |
| المؤلفون: |
Matthew Spock (11219123), Trever R. Carter (11219126), Katrina A. Bollinger (4375849), Changho Han (1309563), Logan A. Baker (11219129), Alice L. Rodriguez (1270236), Li Peng (83452), Jonathan W. Dickerson (3628004), Aidong Qi (2204728), Jerri M. Rook (1315593), Jordan C. O’Neill (3778144), Katherine J. Watson (11218010), Sichen Chang (1475053), Thomas M. Bridges (1336731), Julie L. Engers (1475044), Darren W. Engers (655505), Colleen M. Niswender (353419), P. Jeffrey Conn (1270239), Craig W. Lindsley (203380), Aaron M. Bender (5155397) |
| سنة النشر: |
2021 |
| المجموعة: |
Smithsonian Institution: Digital Repository |
| مصطلحات موضوعية: |
Biochemistry, Medicine, Cell Biology, Pharmacology, Evolutionary Biology, Sociology, Cancer, Infectious Diseases, Chemical Sciences not elsewhere classified, novel use, DMPK properties, movement disorders, Orally Bioavailable M 4 Muscarinic ., CYP inhibition, deuterium incorporation, SAR, M 4 mAChR antagonist, VU 6028418 |
| الوصف: |
Herein, we report the SAR leading to the discovery of VU6028418, a potent M 4 mAChR antagonist with high subtype-selectivity and attractive DMPK properties in vitro and in vivo across multiple species. VU6028418 was subsequently evaluated as a preclinical candidate for the treatment of dystonia and other movement disorders. During the characterization of VU6028418, a novel use of deuterium incorporation as a means to modulate CYP inhibition was also discovered. |
| نوع الوثيقة: |
article in journal/newspaper |
| اللغة: |
unknown |
| Relation: |
https://figshare.com/articles/journal_contribution/Discovery_of_VU6028418_A_Highly_Selective_and_Orally_Bioavailable_M_sub_4_sub_Muscarinic_Acetylcholine_Receptor_Antagonist/15094160 |
| DOI: |
10.1021/acsmedchemlett.1c00363.s001 |
| الاتاحة: |
https://doi.org/10.1021/acsmedchemlett.1c00363.s001 |
| Rights: |
CC BY-NC 4.0 |
| رقم الانضمام: |
edsbas.2BC29576 |
| قاعدة البيانات: |
BASE |