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Discovery of ß-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.
Pinkerton, Anthony B; Peddibhotla, Satyamaheshwar; Yamamoto, Fusayo; Slosky, Lauren M; Bai, Yushi; Maloney, Patrick; Hershberger, Paul; Hedrick, Michael P; Falter, Bekhi; Ardecky, Robert J; Smith, Layton H; Chung, Thomas D Y; Jackson, Michael R; Caron, Marc G; Barak, Lawrence S.
Afiliação
  • Pinkerton AB; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Peddibhotla S; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Yamamoto F; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Slosky LM; Duke University Medical Center , Durham , North Carolina 27709 , United States.
  • Bai Y; Duke University Medical Center , Durham , North Carolina 27709 , United States.
  • Maloney P; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Hershberger P; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Hedrick MP; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Falter B; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Ardecky RJ; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Smith LH; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Chung TDY; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Jackson MR; Conrad Prebys Center for Chemical Genomics , Sanford Burnham Prebys Medical Discovery Institute , La Jolla , California 92037 , United States.
  • Caron MG; Duke University Medical Center , Durham , North Carolina 27709 , United States.
  • Barak LS; Duke University Medical Center , Durham , North Carolina 27709 , United States.
J Med Chem ; 62(17): 8357-8363, 2019 09 12.
Article em En | MEDLINE | ID: mdl-31390201
Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator. Neurotensin receptors have been implicated in a wide variety of CNS disorders, but despite extensive efforts to develop small molecule ligands there are few reports of such compounds. Herein we describe the optimization of a quinazoline based lead to give 18 (SBI-553), a potent and brain penetrant NTR1 allosteric modulator.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Quinazolinas / Doenças do Sistema Nervoso Central / Receptores de Neurotensina / Descoberta de Drogas / Beta-Arrestinas Limite: Animals Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Estados Unidos
Texto completo
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XML
PubMed Links
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Quinazolinas / Doenças do Sistema Nervoso Central / Receptores de Neurotensina / Descoberta de Drogas / Beta-Arrestinas Limite: Animals Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2019 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Estados Unidos