Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation
摘要:
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. (C) 2009 Elsevier Ltd. All rights reserved.
Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation
作者: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
DOI:10.1016/j.bmcl.2009.03.005
日期:2009.5
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. (C) 2009 Elsevier Ltd. All rights reserved.