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Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation |
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| Authors: | John S. Debenham Christina B. Madsen-Duggan Junying Wang Xinchun Tong Julie Lao Tung M. Fong Marie-Therese Schaeffer Jing Chen Xiao Cathy C.R.-R. Huang Chun-Pyn Shen D. Sloan Stribling Lauren P. Shearman Alison M. Strack D. Euan MacIntyre Jeffrey J. Hale Thomas F. Walsh |
| Affiliation: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA;2. Department of Metabolic Disorders, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA;3. Department of Pharmacology, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA |
| Abstract: | 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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