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Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.
Nance, Kellie D; Days, Emily L; Weaver, C David; Coldren, Anastasia; Farmer, Tiffany D; Cho, Hyekyung P; Niswender, Colleen M; Blobaum, Anna L; Niswender, Kevin D; Lindsley, Craig W.
Afiliación
  • Nance KD; Department of Medicine, Division of Diabetes, Endocrinology and Metabolism, ‡Department of Pharmacology, §Vanderbilt Center for Neuroscience Drug Discovery, ∥Vanderbilt Institute of Chemical Biology, and ⊥Vanderbilt Diabetes Center, Vanderbilt University School of Medicine , Nashville, Tennessee
  • Days EL; Tennessee Valley Healthcare System, ∇Department of Chemistry, and ○Vanderbilt Kennedy Center, Vanderbilt University , Nashville, Tennessee 37232, United States.
  • Weaver CD; Department of Medicine, Division of Diabetes, Endocrinology and Metabolism, ‡Department of Pharmacology, §Vanderbilt Center for Neuroscience Drug Discovery, ∥Vanderbilt Institute of Chemical Biology, and ⊥Vanderbilt Diabetes Center, Vanderbilt University School of Medicine , Nashville, Tennessee
  • Coldren A; Tennessee Valley Healthcare System, ∇Department of Chemistry, and ○Vanderbilt Kennedy Center, Vanderbilt University , Nashville, Tennessee 37232, United States.
  • Farmer TD; Department of Medicine, Division of Diabetes, Endocrinology and Metabolism, ‡Department of Pharmacology, §Vanderbilt Center for Neuroscience Drug Discovery, ∥Vanderbilt Institute of Chemical Biology, and ⊥Vanderbilt Diabetes Center, Vanderbilt University School of Medicine , Nashville, Tennessee
  • Cho HP; Tennessee Valley Healthcare System, ∇Department of Chemistry, and ○Vanderbilt Kennedy Center, Vanderbilt University , Nashville, Tennessee 37232, United States.
  • Niswender CM; Department of Medicine, Division of Diabetes, Endocrinology and Metabolism, ‡Department of Pharmacology, §Vanderbilt Center for Neuroscience Drug Discovery, ∥Vanderbilt Institute of Chemical Biology, and ⊥Vanderbilt Diabetes Center, Vanderbilt University School of Medicine , Nashville, Tennessee
  • Blobaum AL; Tennessee Valley Healthcare System, ∇Department of Chemistry, and ○Vanderbilt Kennedy Center, Vanderbilt University , Nashville, Tennessee 37232, United States.
  • Niswender KD; Department of Medicine, Division of Diabetes, Endocrinology and Metabolism, ‡Department of Pharmacology, §Vanderbilt Center for Neuroscience Drug Discovery, ∥Vanderbilt Institute of Chemical Biology, and ⊥Vanderbilt Diabetes Center, Vanderbilt University School of Medicine , Nashville, Tennessee
  • Lindsley CW; Tennessee Valley Healthcare System, ∇Department of Chemistry, and ○Vanderbilt Kennedy Center, Vanderbilt University , Nashville, Tennessee 37232, United States.
J Med Chem ; 60(4): 1611-1616, 2017 02 23.
Article en En | MEDLINE | ID: mdl-28103022
ABSTRACT
A duplexed, functional multiaddition high throughput screen and subsequent optimization effort identified the first orally bioavailable and CNS penetrant glucagon-like peptide-1 receptor (GLP-1R) noncompetitive antagonist. Antagonist 5d not only blocked exendin-4-stimulated insulin release in islets but also lowered insulin levels while increasing blood glucose in vivo.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Receptor del Péptido 1 Similar al Glucagón Límite: Animals / Humans / Male Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Receptor del Péptido 1 Similar al Glucagón Límite: Animals / Humans / Male Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article