Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies

Dai-Shi Su; M Kristine Markowitz; Kathy L Murphy; Bang-Lin Wan; Matthew M Zrada; C Meacham Harrell; Stacy S O'Malley; J Fred Hess; Rick W Ransom; Ray S Chang; Michael A Wallace; Conrad E Raab; Dennis C Dean; Douglas J Pettibone; Roger M Freidinger; Mark G Bock

doi:10.1016/j.bmcl.2004.09.074

Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6045-8. doi: 10.1016/j.bmcl.2004.09.074.

Authors

Dai-Shi Su¹, M Kristine Markowitz, Kathy L Murphy, Bang-Lin Wan, Matthew M Zrada, C Meacham Harrell, Stacy S O'Malley, J Fred Hess, Rick W Ransom, Ray S Chang, Michael A Wallace, Conrad E Raab, Dennis C Dean, Douglas J Pettibone, Roger M Freidinger, Mark G Bock

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. [email protected]

PMID: 15546726
DOI: 10.1016/j.bmcl.2004.09.074

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.

MeSH terms

Animals
Animals, Genetically Modified
Binding, Competitive / drug effects
Bradykinin B1 Receptor Antagonists*
Humans
Isotope Labeling
Ligands
Quinoxalines / chemical synthesis*
Quinoxalines / pharmacology*
Radioligand Assay
Rats
Receptor, Bradykinin B1 / chemistry
Structure-Activity Relationship
Sulfur Radioisotopes

Substances

Bradykinin B1 Receptor Antagonists
Ligands
Quinoxalines
Receptor, Bradykinin B1
Sulfur Radioisotopes