Bradykinin B1 Receptor Antagonist

011_B1R_F (cropped)

Product Description

Product: Bradykinin B1 Receptor Antagonist (R-954)
Description: The R-954 compound was developed by scientists at the University of Sherbrooke and is composed of a novel peptidic antagonist for the bradykinin B1 receptor (BKB1) having very good to excellent affinities and selectivity for BKB1 (in vitro and in vivo). The metabolically stable antagonist of BKB1 receptor has superior pharmacokinetic properties and is based in a sequence with natural and unnatural amino acids to help resist enzymatic degradation in vivo.
Application: Compound is proven to have potent therapeutic effect in vivo for various disease states. It has been shown to significantly reduce the state of hyperalgesia alongside diabetes, reduce infiltration of pro-inflammatory cells and general state of inflammation alongside allergic asthma as well as many other therapeutic applications.
Disciplines: Research into pain syndromes, cancer, pain associated with diabetes mellitus, inflammation, different types of vasculopathies, angiogenesis, multiple sclerosis, epilepsy, and Alzheimer disease, arthritis.
Sequence: N-acetylatedOrn-Arg-Oic-Pro-Gly-(αMe)Phe-Ser-DβNal-Ile-OH
CAS#: NA
Molecular weight: 1194.42 Daltons
Chemical structure: Bradykinin B1R Antagonist

Publications

Imaging

  1. Kuo HT, Pan J, Lau J, Zhang C, Zeisler J, Colpo N, Bénard F, Lin KS. Radiolabeled R954 Derivatives for Imaging Bradykinin B1 Receptor Expression with Positron Emission Tomography. Mol. Pharmaceutics 2017, 14, 821−829

Therapeutic

  1. Shen, J; Wei, C; Sirois, P. Inhibitory Effect of Bradykinin B1 Receptor Antagonist R-954 on Breast Xenograft Tumors in BALB/c Mice. Gene and Gene Editing. Vol. 1, 149–154, 2015
  2. Fernandes PD, Gomes N de M, Sirois P. The bradykinin B1 receptor antagonist R-954 inhibits Ehrlich tumor growth in rodents. Peptides. 2011 32: 1849–1854
  3. Kaufman GN, Zaouter C, Valteau B, Sirois P, Moldovan F. Nociceptive tolerance is improved by bradykinin receptor B1 antagonism and joint morphology is protected by both endothelin type A and bradykinin receptor B1 antagonism in a surgical model of osteoarthritis. Arthritis Research & Therapy. 2011;13(3):R76. doi:10.1186/ar3338.
  4. Catanzaro O., Capponi J. A., Michieli J., Labal E., Di Martino I., Sirois P. (2013). Bradykinin B(1) antagonism inhibits oxidative stress and restores Na+K+ ATPase activity in diabetic rat peripheral nervous system. Peptides 44, 100–104. 10.1016/j.peptides.2013.01.019
  5. Catanzaro O, Labal E, Andornino A, Capponi JA, Di Martino I, Sirois P. Blockade of early and late retinal biochemical alterations associated with diabetes development by the selective bradykinin B1 receptor antagonist R-954. Peptides. 2012;34:349–352.
  6. Catanzaro OL, Dziubecki D, Obregon P, et al. Antidiabetic efficacy of bradykinin antagonist R-954 on glucose tolerance test in diabetic type 1 mice. Neuropeptides. 2010;44:187–189.
  7. Vasquez-Pinto L. M., Nantel F., Sirois P., Jancar S. (2010). Bradykinin B(1) receptor antagonist R954 inhibits eosinophil activation/proliferation/migration and increases TGF-beta and VEGF in a murine model of asthma. Neuropeptides 44 107–113

Safety and Pharmacokinetics

  1. Savard M, Côté J, Tremblay L, Neugebauer W, Regoli D, Gariépy S, Hébert N, Gobeil F. Preclinical pharmacology, metabolic stability, pharmacokinetics and toxicology of the peptidic kinin B1 receptor antagonist R-954. Peptides. 2014 Feb;52:82-9. doi: 10.1016/j.peptides.2013.12.009. Epub 2013 Dec 18.

Certificate of Analysis

medilumine-mouse

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