Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

Lebois EP, Digby GJ, Sheffler DJ, Melancon BJ, Tarr JC, Cho HP, Miller NR, Morrison R, Bridges TM, Xiang Z, Daniels JS, Wood MR, Conn PJ, Lindsley CW
Bioorg Med Chem Lett. 2011 21 (21): 6451-5

PMID: 21930376 · PMCID: PMC3190051 · DOI:10.1016/j.bmcl.2011.08.084

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.

Copyright © 2011 Elsevier Ltd. All rights reserved.

MeSH Terms (10)

Administration, Oral Animals Biological Availability Cell Line Central Nervous System Humans Muscarinic Agonists Rats Receptor, Muscarinic M1 Structure-Activity Relationship

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