Non-peptide antagonists for kinin B1 receptors: new insights into their therapeutic potential for the management of inflammation and pain.
Kinin B1 and B2 receptors are central to the aetiology of pain and inflammation. Constitutive B2 receptors are commonly associated with the acute phase of inflammation and nociception, whereas the inducible B1 receptors are mostly linked to the chronic or persistent phase (or both). Therefore, selective, orally active kinin B1 receptor antagonists could be potentially therapeutic. B1 receptor antagonists have long been exclusively peptides, but recently a few non-peptide representatives have been identified. The clinical potential of these non-peptide molecules has not yet been evaluated, but they might have a role in treating persistent inflammation and pain, especially when no satisfactory therapy is available. This review summarizes recent advances in the identification and the potential therapeutic properties of these molecules.
Campos
Maria M
MM
Department of Pharmacology, Centre of Biological Sciences, Universidade Federal de Santa Catarina, Florianópolis, SC 88049-900, Brazil.
Leal
Paulo C
PC
Yunes
Rosendo A
RA
Calixto
João B
JB
D000818:Animals; D065169:Bradykinin B1 Receptor Antagonists; D004149:Dioxoles / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D007249:Inflammation / Q000188:drug therapy*; D008967:Molecular Biology; D010146:Pain / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology / Q000627:therapeutic use
C487113:2-((3-(1,3-benzodioxol-5-yl)-3-(((6-methoxy-2-naphthyl)sulfonyl)amino)propanoyl)amino)-3-(4-((2,6-dimethylpiperidinyl)methyl)phenyl)-N-isopropyl-N-methylpropanamide; D065169:Bradykinin B1 Receptor Antagonists; D004149:Dioxoles; D013449:Sulfonamides