title: Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.
abstract: We have developed an efficient and selective radioligand, the [35S]-radiolabeled dihydroquinoxalinone derivative, 4, for an ex vivo receptor occupancy assay in transgenic rats over-expressing the human bradykinin B1 receptor.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. daishi_su@merck.com
authors.forename: Dai-Shi
authors.initials: DS
authors.lastname: Su
authors.forename: M Kristine
authors.initials: MK
authors.lastname: Markowitz
authors.forename: Kathy L
authors.initials: KL
authors.lastname: Murphy
authors.forename: Bang-Lin
authors.initials: BL
authors.lastname: Wan
authors.forename: Matthew M
authors.initials: MM
authors.lastname: Zrada
authors.forename: C Meacham
authors.initials: CM
authors.lastname: Harrell
authors.forename: Stacy S
authors.initials: SS
authors.lastname: O'Malley
authors.forename: J Fred
authors.initials: JF
authors.lastname: Hess
authors.forename: Rick W
authors.initials: RW
authors.lastname: Ransom
authors.forename: Ray S
authors.initials: RS
authors.lastname: Chang
authors.forename: Michael A
authors.initials: MA
authors.lastname: Wallace
authors.forename: Conrad E
authors.initials: CE
authors.lastname: Raab
authors.forename: Dennis C
authors.initials: DC
authors.lastname: Dean
authors.forename: Douglas J
authors.initials: DJ
authors.lastname: Pettibone
authors.forename: Roger M
authors.initials: RM
authors.lastname: Freidinger
authors.forename: Mark G
authors.initials: MG
authors.lastname: Bock
mesh_terms: D000818:Animals; D030801:Animals, Genetically Modified; D001667:Binding, Competitive / Q000187:drug effects; D065169:Bradykinin B1 Receptor Antagonists; D006801:Humans; D007553:Isotope Labeling; D008024:Ligands; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D043783:Receptor, Bradykinin B1 / Q000737:chemistry; D013329:Structure-Activity Relationship; D013462:Sulfur Radioisotopes
chemical_list: D065169:Bradykinin B1 Receptor Antagonists; D008024:Ligands; D011810:Quinoxalines; D043783:Receptor, Bradykinin B1; D013462:Sulfur Radioisotopes