1208222-41-6Relevant articles and documents
Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M5 PAM
Bridges, Thomas M.,Kennedy, J. Phillip,Cho, Hyekyung P.,Breininger, Micah L.,Gentry, Patrick R.,Hopkins, Corey R.,Conn, P. Jeffrey,Lindsley, Craig W.
scheme or table, p. 558 - 562 (2010/08/06)
This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M5-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan Gq mAChR M1, M3, M5 PAM. An iterative library synthesis approach delivered the first selective M5 PAM (no activity at M1-M4 @ 30 μM), and an important tool compound to study the role of M5 in the CNS.