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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Bibliografski detalji
Glavni autori: 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
Jezik:Inglês
Izdano: American Chemical Society 2014
Online pristup: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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