Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.
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.
Su
Dai-Shi
DS
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. daishi_su@merck.com
Markowitz
M Kristine
MK
Murphy
Kathy L
KL
Wan
Bang-Lin
BL
Zrada
Matthew M
MM
Harrell
C Meacham
CM
O'Malley
Stacy S
SS
Hess
J Fred
JF
Ransom
Rick W
RW
Chang
Ray S
RS
Wallace
Michael A
MA
Raab
Conrad E
CE
Dean
Dennis C
DC
Pettibone
Douglas J
DJ
Freidinger
Roger M
RM
Bock
Mark G
MG
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
D065169:Bradykinin B1 Receptor Antagonists; D008024:Ligands; D011810:Quinoxalines; D043783:Receptor, Bradykinin B1; D013462:Sulfur Radioisotopes