Discovery of the first M(5)-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)

A functional high throughput screen and subsequent multi-dimensional, iterative parallel synthesis effort identified the first muscarinic acetylcholine receptor (mAChR) negative allosteric modulator (NAM) selective for the M(5) subtype. ML375 is a highly selective M(5) NAM with sub-micromolar potenc...

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Autori principali: Gentry, Patrick R., Kokubo, Masaya, Bridges, Thomas M., Kett, Nathan R., Harp, Joel M., Cho, Hyekyung P., Smith, Emery, Chase, Peter, Hodder, Peter S., Niswender, Colleen M., Daniels, J. Scott, Conn, P. Jeffrey, Wood, Michael R., Lindsley, Craig W.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2013
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC3876027/
https://ncbi.nlm.nih.gov/pubmed/24164599
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm4013246
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