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.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-12, Vol.14 (24), p.6045-6048
Main Authors: SU, Dai-Shi, MARKOWITZ, M. Kristine, WALLACE, Michael A, RAAB, Conrad E, DEAN, Dennis C, PETTIBONE, Douglas J, FREIDINGER, Roger M, BOCK, Mark G, MURPHY, Kathy L, WAN, Bang-Lin, ZRADA, Matthew M, HARRELL, C. Meacham, O'MALLEY, Stacy S, HESS, J. Fred, RANSOM, Rick W, CHANG, Ray S
Format: Article
Language:English
Subjects:
Animals
Animals, Genetically Modified
Binding, Competitive - drug effects
Biological and medical sciences
Bradykinin B1 Receptor Antagonists
Contrast media. Radiopharmaceuticals
Humans
Isotope Labeling
Ligands
Medical sciences
Pharmacology. Drug treatments
Quinoxalines - chemical synthesis
Quinoxalines - pharmacology
Radioligand Assay
Rats
Receptor, Bradykinin B1 - chemistry
Structure-Activity Relationship
Sulfur Radioisotopes
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.09.074