FR167344 free base is an orally active, nonpeptide antagonist of the bradykinin receptor B2, exhibiting high-affinity binding (IC50: 65 nM) and showing no binding affinity for the B1 receptor.
Labradimil is a bradykininB2 receptor agonist. Labradimil increases the permeability of human brain microvascular endothelial cell monolayers. Labradimil enhances delivery of hydrophilic chemotherapeutics and increases survival in rats with metastatic tu
Fasitibant chloride (MEN16132 free base) is a powerful and specific nonpeptide antagonist of the bradykininB2 receptor (B2R). This compound effectively reduces joint pain and mitigates joint edema in a rat model of Carrageenan-induced arthritis.
Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]
Peptide antagonist of the B2bradykinin receptor (pKi = 10.3); conformationally constrained cyclized analog of HOE 140. Blocks hypotension and bronchoconstriction in vivo. Displays selectivity for B2 over 29 other receptors and ion channels (pIC50 < 5.5).
Selective bradykininB2 receptor agonist that is resistant to carboxypeptidase cleavage. 5-fold more potent and exhibits a more prolonged duration of action than bradykinin in vivo.