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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Bibliografski detalji
Glavni autori: 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.
Format: Artigo
Jezik:Inglês
Izdano: 2013
Teme:
Article
Online pristup: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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