Discovery of ML314, a Brain Penetrant Nonpeptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor

[Image: see text] The neurotensin 1 receptor (NTR1) is an important therapeutic target for a range of disease states including addiction. A high-throughput screening campaign, followed by medicinal chemistry optimization, led to the discovery of a nonpeptidic β-arrestin biased agonist for NTR1. The...

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Main Authors: Peddibhotla, Satyamaheshwar, Hedrick, Michael P., Hershberger, Paul, Maloney, Patrick R., Li, Yujie, Milewski, Monika, Gosalia, Palak, Gray, Wilson, Mehta, Alka, Sugarman, Eliot, Hood, Becky, Suyama, Eigo, Nguyen, Kevin, Heynen-Genel, Susanne, Vasile, Stefan, Salaniwal, Sumeet, Stonich, Derek, Su, Ying, Mangravita-Novo, Arianna, Vicchiarelli, Michael, Roth, Gregory P., Smith, Layton H., Chung, Thomas D. Y., Hanson, Glen R., Thomas, James B., Caron, Marc G., Barak, Lawrence S., Pinkerton, Anthony B.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2013
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3940307/
https://ncbi.nlm.nih.gov/pubmed/24611085
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml400176n
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