Search Results - "MARKOWITZ, M. Kristine"
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Discovery of a Potent, Non-peptide Bradykinin B1 Receptor Antagonist
Published in Journal of the American Chemical Society (25-06-2003)“…Bradykinin (BK) plays an important role in the pathophysiological processes accompanying pain and inflammation. Selective bradykinin B1 receptor antagonists…”
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2
Potent bradykinin B1 receptor antagonists : 4-Substituted phenyl cyclohexanes
Published in Bioorganic & medicinal chemistry letters (01-06-2007)“…Selective bradykinin (BK) B(1) receptor antagonists have been shown to be antinociceptive in animal models and could be novel therapeutic agents for the…”
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3
Generation and characterization of a human bradykinin receptor B1 transgenic rat as a pharmacodynamic model
Published in The Journal of pharmacology and experimental therapeutics (01-08-2004)“…Antagonists of the B1 bradykinin receptor (B1R) offer the promise of novel therapeutic agents for the treatment of inflammatory and neuropathic pain. However,…”
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4
Binding modes of dihydroquinoxalinones in a homology model of bradykinin receptor 1
Published in Biochemical and biophysical research communications (27-05-2005)“…We report the first homology model of human bradykinin receptor B1 generated from the crystal structure of bovine rhodopsin as a template. Using an automated…”
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Pharmacological characterization and radioligand binding properties of a high-affinity, nonpeptide, bradykinin B1 receptor antagonist
Published in European journal of pharmacology (19-09-2004)“…Compound A (N-[2-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]ethyl]-2-[(2R)-1-(2-napthylsulfonyl)-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]acetamide) is a member of…”
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6
Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies
Published in Bioorganic & medicinal chemistry letters (20-12-2004)“…We have developed an efficient and selective radioligand, the [35S]-radiolabeled dihydroquinoxalinone derivative, 4, for an ex vivo receptor occupancy assay in…”
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7
Discovery of a Potent, Non-peptide Bradykinin B 1 Receptor Antagonist
Published in Journal of the American Chemical Society (25-06-2003)Get full text
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8
Potent bradykinin B 1 receptor antagonists: 4-Substituted phenyl cyclohexanes
Published in Bioorganic & medicinal chemistry letters (01-06-2007)“…4-Substituted phenyl cyclohexanes were identified as alternative isosteres for the biphenyl moiety of the lead compound 1. The syntheses, SAR optimization, and…”
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9
Pharmacological characterization and radioligand binding properties of a high-affinity, nonpeptide, bradykinin B 1 receptor antagonist
Published in European journal of pharmacology (19-09-2004)“…Compound A ( N-{2-[4-(4,5-dihydro-1 H-imidazol-2-yl)phenyl]ethyl}-2-[(2 R)-1-(2-napthylsulfonyl)-3-oxo-1,2,3,4-tetrahydroquinoxalin-2-yl]acetamide) is a member…”
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10
Development of an efficient and selective radioligand for bradykinin B 1 receptor occupancy studies
Published in Bioorganic & medicinal chemistry letters (20-12-2004)“…[Display omitted] We have developed an efficient and selective radioligand, the [ 35S]-radiolabeled dihydroquinoxalinone derivative, 4, for an ex vivo receptor…”
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