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Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.
Debenham, John S; Madsen-Duggan, Christina B; Wang, Junying; Tong, Xinchun; Lao, Julie; Fong, Tung M; Schaeffer, Marie-Therese; Xiao, Jing Chen; Huang, Cathy C R-R; Shen, Chun-Pyn; Sloan Stribling, D; Shearman, Lauren P; Strack, Alison M; Euan Macintyre, D; Hale, Jeffrey J; Walsh, Thomas F.
Afiliación
  • Debenham JS; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett ; 19(9): 2591-4, 2009 May 01.
Article en En | MEDLINE | ID: mdl-19328684
The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and heterotricyclic scaffolds. Food intake and pharmacokinetic evaluation of several of these compounds indicate that they are effective orally active modulators of CB1R.
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Pirimidinas / Agonistas de Receptores de Cannabinoides / Obesidad Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Pirimidinas / Agonistas de Receptores de Cannabinoides / Obesidad Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2009 Tipo del documento: Article País de afiliación: Estados Unidos