Abstract
Bradykinin B1 receptor antagonists embody a potentially novel approach for the treatment of chronic pain and inflammation. A series of 2,3-diaminopyridine B1 antagonists was optimized to have sub-nanomolar affinity and good pharmacokinetic properties. Lead compounds were shown to exhibit good efficacy in rabbit in vivo models of pain and inflammation.
MeSH terms
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Aminopyridines / chemical synthesis*
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Aminopyridines / chemistry
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Aminopyridines / pharmacology
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Analgesics / chemical synthesis*
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Analgesics / chemistry
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Analgesics / pharmacology
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Bradykinin B1 Receptor Antagonists*
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Dogs
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Half-Life
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Inflammation / drug therapy
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Pain Measurement
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Rabbits
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Rats
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Species Specificity
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Structure-Activity Relationship
Substances
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Aminopyridines
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Analgesics
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Anti-Inflammatory Agents, Non-Steroidal
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Bradykinin B1 Receptor Antagonists
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2,3-diaminopyridine