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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Bibliographic Details
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.
Format:	Artigo
Language:	Inglês
Published:	American Chemical Society 2014
Online Access:	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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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)

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