Further exploration of M(1) allosteric agonists: Subtle structural changes abolish M(1) allosteric agonism and result in pan-mAChR orthosteric antagonism

This letter describes the further exploration of two series of M(1)allosteric agonists, TBPB and VU0357017, previously reported from our lab. Within the TPBP scaffold, either electronic or steric perturbations to the central piperidine ring led to a loss of selective M(1) allosteric agonism and affo...

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Главные авторы: Sheffler, Douglas J., Sevel, Christian, Le, Uyen, Lovell, Kimberly M., Tarr, James C., Carrington, Sheridan J. S., Cho, Hyekyung P., Digby, Gregory J., Niswender, Colleen M., Conn, P. Jeffrey, Hopkins, Corey R., Wood, Michael R., Lindsley, Craig W.
Формат: Artigo
Язык:Inglês
Опубликовано: 2012
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Article
Online-ссылка:https://ncbi.nlm.nih.gov/pmc/articles/PMC3525729/
https://ncbi.nlm.nih.gov/pubmed/23200253
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2012.10.132
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