Selective bradykininB2receptor agonist that is resistant to carboxypeptidase cleavage. 5-fold more potent and exhibits a more prolonged duration of action than bradykinin in vivo.
Labradimil is a bradykininB2receptor 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
Potent and selective bradykinin B1 receptor antagonist (ID50 values are 2.8 and > 600 nM at B1 and B2receptors respectively). Exhibits no intrinsic agonist activity and is resistant to aminopeptidase and kininase II (ACE) cleavage. Displays hypertensive
Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]
FR167344 free base is an orally active, nonpeptide antagonist of the bradykininreceptorB2, exhibiting high-affinity binding (IC50: 65 nM) and showing no binding affinity for the B1 receptor.
Peptide antagonist of the B2bradykininreceptor (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).
Fasitibant chloride (MEN16132 free base) is a powerful and specific nonpeptide antagonist of the bradykininB2receptor (B2R). This compound effectively reduces joint pain and mitigates joint edema in a rat model of Carrageenan-induced arthritis.