565460-55-1Relevant articles and documents
Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists
Chen, Jian Jeffrey,Qian, Wenyuan,Biswas, Kaustav,Viswanadhan, Vellarkad N.,Askew, Benny C.,Hitchcock, Stephen,Hungate, Randall W.,Arik, Leyla,Johnson, Eileen
scheme or table, p. 4477 - 4481 (2009/04/08)
Replacement of the core β-amino acid in our previously reported piperidine acetic acid and β-phenylalanine-based Bradykinin B1 antagonists by dihydroquinoxalinone acetic acid increases the in vitro potency and metabolic stability. The most potent compounds from this series have IC50s a human B1 receptor functional assay. A molecular modeling study of the binding modes of key compounds, based on a B1 homology model, explains the structure-activity relationship (SAR) for these analogs.
Development of an efficient and selective radioligand for bradykinin B 1 receptor occupancy studies
Su, Dai-Shi,Markowitz, M. Kristine,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.,Wallace, Michael A.,Raab, Conrad E.,Dean, Dennis C.,Pettibone, Douglas J.,Freidinger, Roger M.,Bock, Mark G.
, p. 6045 - 6048 (2007/10/03)
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.
Discovery of a potent, non-peptide bradykinin B1 receptor antagonist
Su, Dai-Shi,Markowitz, M. Kristine,DiPardo, Robert M.,Murphy, Kathy L.,Harrell, C. Meacham,O'Malley, Stacy S.,Ransom, Richard W.,Chang, Raymond S. L.,Ha, Sookhee,Hess, Fred J.,Pettibone, Douglas J.,Mason, Glenn S.,Boyce, Susan,Freidinger, Roger M.,Bock, Mark G.
, p. 7516 - 7517 (2007/10/03)
Bradykinin (BK) plays an important role in the pathophysiological processes accompanying pain and inflammation. Selective bradykinin B1 receptor antagonists have been shown to be anti-nociceptive in animal models and could be novel therapeutic