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Benzodiazepines as potent and selective bradykinin B1 antagonists.
Wood, Michael R; Kim, June J; Han, Wei; Dorsey, Bruce D; Homnick, Carl F; DiPardo, Robert M; Kuduk, Scott D; MacNeil, Tanya; Murphy, Kathy L; Lis, Edward V; Ransom, Richard W; Stump, Gary L; Lynch, Joseph J; O'Malley, Stacey S; Miller, Patricia J; Chen, Tsing-Bau; Harrell, Charles M; Chang, Raymond S L; Sandhu, Punam; Ellis, Joan D; Bondiskey, Peter J; Pettibone, Douglas J; Freidinger, Roger M; Bock, Mark G.
Affiliation
  • Wood MR; Department of Medicinal Chemistry, Merck Research Laboratories, P.O. Box 4, West Point, Pennsylvania 19486, USA. michael_wood2@merck.com
J Med Chem ; 46(10): 1803-6, 2003 May 08.
Article in En | MEDLINE | ID: mdl-12723943
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.
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Collection: 01-internacional Database: MEDLINE Main subject: Benzodiazepines / Bradykinin Receptor Antagonists Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2003 Type: Article Affiliation country: United States
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Collection: 01-internacional Database: MEDLINE Main subject: Benzodiazepines / Bradykinin Receptor Antagonists Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2003 Type: Article Affiliation country: United States