Potent, Selective, and Orally Efficacious Antagonists of Melanin-Concentrating Hormone Receptor 1

The high expression of MCH in the hypothalamus with the lean hypophagic phenotype coupled with increased resting metabolic rate and resistance to high fat diet-induced obesity of MCH KO mice has spurred considerable efforts to develop small molecule MCHR1 antagonists. Starting from a lead thienopyri...

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Veröffentlicht in:	Journal of medicinal chemistry 2006-11, Vol.49 (24), p.7095-7107
Hauptverfasser:	Tavares, Francis X, Al-Barazanji, Kamal A, Bigham, Eric C, Bishop, Michael J, Britt, Christy S, Carlton, David L, Feldman, Paul L, Goetz, Aaron S, Grizzle, Mary K, Guo, Yu C, Handlon, Anthony L, Hertzog, Donald L, Ignar, Diane M, Lang, Daniel G, Ott, Ronda J, Peat, Andrew J, Zhou, Hui-Qiang
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Anti-Obesity Agents - chemical synthesis Anti-Obesity Agents - chemistry Anti-Obesity Agents - pharmacology Biological and medical sciences Biological Availability CHO Cells Cricetinae Cricetulus ERG1 Potassium Channel Ether-A-Go-Go Potassium Channels - drug effects Ether-A-Go-Go Potassium Channels - physiology Genes, Reporter Half-Life Hormones. Endocrine system Humans Medical sciences Mice Mice, Obese Models, Molecular Pharmacology. Drug treatments Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Rats Receptors, Somatostatin - antagonists & inhibitors Structure-Activity Relationship Thiophenes - chemical synthesis Thiophenes - chemistry Thiophenes - pharmacology
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