Continued optimization of the M(5) NAM ML375: Discovery of VU6008667, an M(5) NAM with high CNS penetration and a desired short half-life in rat for addiction studies

This letter describes the continued optimization of M(5) NAM ML375 (VU0483253). While a valuable in vivo tool compound, ML375 has an excessively long elimination half-life in rat (t(1/2) = 80 hours), which can be problematic in certain rodent addiction paradigms (e.g., reinstatement). Thus, we requi...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: McGowan, Kevin M., Nance, Kellie D., Cho, Hykeyung P., Bridges, Thomas M., Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2017
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5508536/
https://ncbi.nlm.nih.gov/pubmed/28237763
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.02.020
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