title: Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
authors.forename: John S
authors.initials: JS
authors.lastname: Debenham
authors.forename: Christina B
authors.initials: CB
authors.lastname: Madsen-Duggan
authors.forename: Junying
authors.initials: J
authors.lastname: Wang
authors.forename: Xinchun
authors.initials: X
authors.lastname: Tong
authors.forename: Julie
authors.initials: J
authors.lastname: Lao
authors.forename: Tung M
authors.initials: TM
authors.lastname: Fong
authors.forename: Marie-Therese
authors.initials: MT
authors.lastname: Schaeffer
authors.forename: Jing Chen
authors.initials: JC
authors.lastname: Xiao
authors.forename: Cathy C R-R
authors.initials: CC
authors.lastname: Huang
authors.forename: Chun-Pyn
authors.initials: CP
authors.lastname: Shen
authors.forename: D
authors.initials: D
authors.lastname: Sloan Stribling
authors.forename: Lauren P
authors.initials: LP
authors.lastname: Shearman
authors.forename: Alison M
authors.initials: AM
authors.lastname: Strack
authors.forename: D
authors.initials: D
authors.lastname: Euan Macintyre
authors.forename: Jeffrey J
authors.initials: JJ
authors.lastname: Hale
authors.forename: Thomas F
authors.initials: TF
authors.lastname: Walsh