Sar-[D-Phe8]-des-Arg9-Bradykinin acetate is a potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

Lys-(Des-Arg9,Leu8)-Bradykinin is a selective antagonist of the bradykinin B1 receptor [1].

5-Hydroxy-1-methylhydantoin (HD-003) is an antioxidant potentially for the treatment of renal failure. A creatinine metabolite, 5-Hydroxy-1-methylhydantoin , a hydroxyl radical scavenger, has previously been shown to confer renoprotection by inhibiting the progression of chronic kidney disease in rats. 5-Hydroxy-1-methylhydantoin is a novel anti-oxidant drug completely suppressed the expression of B2-kinin receptors (B2KR) in response to high glucose (25 mM) stimulation in VSMC and was also shown to attenuate the effects of BK on VSMC remodeling. 5-Hydroxy-1-methylhydantoin inhibited the BK-induced increase in MAPK phosphorylation and attenuated the increase in connective tissue growth factor (CTGF) protein levels in VSMC. These findings suggest that 5-Hydroxy-1-methylhydantoin may confer vascular protection against high glucose concentrations and BK-stimulation to ameliorate vascular injury and remodeling through its anti-oxidant properties.

R715 TFA(185052-09-9 free base) is a potent and selective bradykinin B1 receptor antagonist (pA2 = 8.49). Displays no activity at B2 receptors. Reduces mechanical hypernociception in a mouse model of neuropathic pain. Metabolically stable.

SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors, respectively).