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Discovery of (S)-2-Cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): A Novel, CNS Penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) Positive Allosteric Modulator (PAM)
[Image: see text] A duplexed, functional multiaddition high throughput screen and subsequent iterative parallel synthesis effort identified the first highly selective and CNS penetrant glucagon-like peptide-1R (GLP-1R) positive allosteric modulator (PAM). PAM (S)-9b potentiated low-dose exenatide to...
Autores principales: | Morris, Lindsey C., Nance, Kellie D., Gentry, Patrick R., Days, Emily L., Weaver, C. David, Niswender, Colleen M., Thompson, Analisa D., Jones, Carrie K., Locuson, Chuck W., Morrison, Ryan D., Daniels, J. Scott, Niswender, Kevin D., Lindsley, Craig W. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2014
|
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4266362/ https://www.ncbi.nlm.nih.gov/pubmed/25423411 http://dx.doi.org/10.1021/jm501375c |
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