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

Bioorganic & Medicinal Chemistry Letters（2005）

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摘要

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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关键词

Bradykinin B1 receptor,Antagonist,Radioligand,Ex vivo

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