Development of a Highly Potent, Novel M(5) Positive Allosteric Modulator (PAM) Demonstrating CNS Exposure: 1-((1H-Indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)

[Image: see text] A functional high throughput screen identified a novel chemotype for the positive allosteric modulation (PAM) of the muscarinic acetylcholine receptor (mAChR) subtype 5 (M(5)). Application of rapid analog, iterative parallel synthesis efficiently optimized M(5) potency to arrive at...

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Detalhes bibliográficos
Main Authors: Gentry, Patrick R., Kokubo, Masaya, Bridges, Thomas M., Noetzel, Meredith J., Cho, Hyekyung P., Lamsal, Atin, Smith, Emery, Chase, Peter, Hodder, Peter S., Niswender, Colleen M., Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W., Wood, Michael R.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2014
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4175000/
https://ncbi.nlm.nih.gov/pubmed/25147929
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm500995y
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