Development of a highly selective, orally bioavailable and CNS penetrant M-1 agonist derived from the MLPCN probe ML071

作者：Lebois Evan P; Digby Gregory J; Sheffler Douglas J; Melancon Bruce J; Tarr James C; Cho Hyekyung P; Miller Nicole R; Morrison Ryan; Bridges Thomas M; Xiang Zixiu; Daniels J Scott; Wood Michael R; Conn P Jeffrey; Lindsley Craig W^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(21): 6451-6455.

DOI：10.1016/j.bmcl.2011.08.084

• Muscarinic acetylcholine receptor 1
• mAChR1 (M-1)
• ML071
• Allosteric agonist

Herein we report the discovery and SAR of a novel series of M-1 agonists based on the MLPCN probe, ML071. From this, VU0364572 emerged as a potent, orally bioavailable and CNS penetrant M-1 agonist with high selectivity, clean ancillary pharmacology and enantiospecific activity.

• 出版日期2011-11-1