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Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists.
Hu, Shuanghua; Huang, Yazhong; Deshpande, Milind; Luo, Guanglin; Bruce, Marc A; Chen, Ling; Mattson, Gail; Iben, Lawrence G; Zhang, Jie; Russell, John W; Clarke, Wendy J; Hogan, John B; Ortiz, Astrid; Flint, Oliver; Henwood, Andrew; Gao, Qi; Antal-Zimanyi, Ildiko; Poindexter, Graham S.
Afiliación
  • Hu S; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Huang Y; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Deshpande M; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Luo G; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Bruce MA; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Chen L; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Mattson G; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Iben LG; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Zhang J; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Russell JW; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Clarke WJ; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Hogan JB; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Ortiz A; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Flint O; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Henwood A; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Gao Q; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Antal-Zimanyi I; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
  • Poindexter GS; Research & Development, Bristol-Myers Squibb Company , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
ACS Med Chem Lett ; 3(3): 222-6, 2012 Mar 08.
Article en En | MEDLINE | ID: mdl-24900458
A novel class of bicyclo[3.1.0]hexanylpiperazine neuropeptide Y (NPY) Y1 antagonists has been designed and synthesized. Scatchard binding analysis showed these compounds to be noncompetitive with [(125)I]PYY binding to the Y1 receptor. The most potent member, 1-((1α,3α,5α,6ß)-6-(3-ethoxyphenyl)-3-methylbicyclo[3.1.0]hexan-6-yl)-4-phenylpiperazine (2) had an IC50 = 62 nM and displayed excellent oral bioavailability in rat (% F po = 80), as well as good brain penetration (B/P ratio = 0.61). In a spontaneous nocturnal feeding study with male Sprague-Dawley rats, 2 significantly reduced food intake during a 12 h period.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2012 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
Texto completo
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Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2012 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos