| Literature DB >> 12723943 |
Michael R Wood1, June J Kim, Wei Han, Bruce D Dorsey, Carl F Homnick, Robert M DiPardo, Scott D Kuduk, Tanya MacNeil, Kathy L Murphy, Edward V Lis, Richard W Ransom, Gary L Stump, Joseph J Lynch, Stacey S O'Malley, Patricia J Miller, Tsing-Bau Chen, Charles M Harrell, Raymond S L Chang, Punam Sandhu, Joan D Ellis, Peter J Bondiskey, Douglas J Pettibone, Roger M Freidinger, Mark G Bock.
Abstract
Antagonism of the bradykinin B(1) receptor was demonstrated to be a potential treatment for chronic pain and inflammation. Novel benzodiazepines were designed that display subnanomolar affinity for the bradykinin B(1) receptor (K(i) = 0.59 nM) and high selectivity against the bradykinin B(2) receptor (K(i) > 10 microM). In vivo efficacy, comparable to morphine, was demonstrated for lead compounds in a rodent hyperalgesia model.Entities:
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Year: 2003 PMID： 12723943 DOI： 10.1021/jm034020y
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446