title: Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.
abstract: Obesity remains a significant public health issue leading to Type II diabetes and cardiovascular disease. CB1 antagonists have been shown to suppress appetite and reduce body weight in animal models as well as in humans. Evaluation of pre-clinical CB1 antagonists to establish relationships between in vitro affinity and in vivo efficacy parameters are enhanced by ex vivo receptor occupancy data. Synthesis and biological evaluation of a novel and highly selective radiolabeled CB1 antagonist is described. The radioligand was used to conduct ex vivo receptor occupancy studies.
authors.affiliation: Research & Development, Bristol-Myers Squibb Co., PO Box 4000, Princeton, New Jersey 08543, USA.
authors.forename: Yifan
authors.initials: Y
authors.lastname: Yang
authors.forename: Keith J
authors.initials: KJ
authors.lastname: Miller
authors.forename: Yeheng
authors.initials: Y
authors.lastname: Zhu
authors.forename: Yang
authors.initials: Y
authors.lastname: Hong
authors.forename: Yuan
authors.initials: Y
authors.lastname: Tian
authors.forename: Natesan
authors.initials: N
authors.lastname: Murugesan
authors.forename: Zhengxiang
authors.initials: Z
authors.lastname: Gu
authors.forename: Eva
authors.initials: E
authors.lastname: O'Tanyi
authors.forename: William J
authors.initials: WJ
authors.lastname: Keim
authors.forename: Kenneth W
authors.initials: KW
authors.lastname: Rohrbach
authors.forename: Susan
authors.initials: S
authors.lastname: Johnghar
authors.forename: Kamelia
authors.initials: K
authors.lastname: Behnia
authors.forename: Mary Ann
authors.initials: MA
authors.lastname: Pelleymounter
authors.forename: Kenneth E
authors.initials: KE
authors.lastname: Carlson
authors.forename: William R
authors.initials: WR
authors.lastname: Ewing
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000737:chemistry* / Q000494:pharmacology*; D001921:Brain / Q000000981:diagnostic imaging; D006801:Humans; D009765:Obesity / Q000188:drug therapy; D011859:Radiography; D011869:Radioligand Assay / Q000379:methods*; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D019440:Anti-Obesity Agents; D043884:Receptor, Cannabinoid, CB1