Bradykinin Receptor

Anatibant 2HCl is a small molecule bradykinin B2 receptor antagonist for the treatment of neurological disorders and may be used in the study of brain injury.

Bradykinin is an inflammatory mediator. It is a peptide that causes blood vessels to dilate (enlarge) via the release of prostacyclin, nitric oxide, and Endothelium-Derived Hyperpolarizing Factor. Bradykinin is a physiologically and pharmacologically active peptide of the kinin group of proteins, consisting of nine amino acids.

Icatibant Acetate, an antagonist of the bradykinin B2 receptor, is used in the treatment of hereditary angioedema.

ELN-441958 is a potent, neutral antagonist of the B1 receptor, inhibiting the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with a Ki of 0.26 nM. ELN-441958 (ELN 441958) is highly selective for B1 over B2 receptors.

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

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.

MK-0686 is an orally available bradykinin B1 receptor antagonist with potential anti-inflammatory activity.

Lys-[Des-Arg9]Bradykinin acetate is an 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]-Bradykinin.

Bradykinin (acetate) is an active peptide that is generated by the kallikrein-kinin system. It is a inflammatory mediator and also recognized as a neuromediator and regulator of several vascular and renal functions. Enzymatically produced from kallidin in the blood, it is a powerful vasodilator that causes smooth muscle contraction, and may mediate inflammation. It has a role as a human blood serum metabolite and a vasodilator agent. It is a tautomer of a bradykinin(2+).

Bradykinin (2-9) (Des-Arg1-bradykinin) is an amino-truncated peptide compound that is a metabolite of Bradykinin. It is formed by the cleavage action of Aminopeptidase P.

[Des-Arg9]-Bradykinin is an agonist of Bradykinin (B1) receptor that displays selectivity for B1 over B2 receptors.

[Des-Arg9]-Bradykinin acetate is a selective agonist of the Bradykinin B1 receptor.

Safotibant (LF-22-0542) is a bradykinin B1 receptor antagonist with anti-inflammatory and analgesic activity for the topical treatment of diabetic macular edema.

Lys-Bradykinin acetate is an endogenous bradykinin receptor agonist.

(Hyp³)-Bradykinin acetate is an agonist of bradykinin B2 receptor and stimulates inositol phosphate production in cultured human fibroblasts.

Lys-[Des-Arg9]Bradykinin,TFA is 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]-Bradykinin.

NPC 567 acetate is a bradykinin B2 antagonist and can be used in studies about the treatment of allergic airway disease.

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.

B-Raf IN 14 is a BRAF inhibitor.

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

[Des-Arg9]-Bradykinin ([Des-Arg9]-Bradykinin(2TFA))(2TFA) is an agonist of Bradykinin (B1) receptor.

Des-Arg9-[Leu8]-Bradykinin acetate is a potent antagonist of the bradykinin receptor 1 (B1R) used in renal fibrosis research [1].

Bombinakinin M acetate is a potent bradykinin receptor agonist with high selectivity for mammalian arterial smooth muscle bradykinin receptors and is approximately 50 times more potent than bradykinin.