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

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

  • Bioorg Med Chem Lett. 2011 Nov 1;21(21):6451-5. doi: 10.1016/j.bmcl.2011.08.084.
Evan P Lebois 1,  Gregory J Digby,  Douglas J Sheffler,  Bruce J Melancon,  James C Tarr,  Hyekyung P Cho,  Nicole R Miller,  Ryan Morrison,  Thomas M Bridges,  Zixiu Xiang,  J Scott Daniels,  Michael R Wood,  P Jeffrey Conn,  Craig W Lindsley
Affiliations

Affiliation

  • 1 Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
PMID: 21930376 DOI: 10.1016/j.bmcl.2011.08.084
Abstract

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.

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