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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4175000/
https://www.ncbi.nlm.nih.gov/pubmed/25147929
http://dx.doi.org/10.1021/jm500995y

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4175000/
https://www.ncbi.nlm.nih.gov/pubmed/25147929
http://dx.doi.org/10.1021/jm500995y

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