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Review

A Systematic Review of Molecular Imaging Agents Targeting Bradykinin B1 and B2 Receptors

1
Department of Molecular Oncology, BC Cancer, Vancouver, BC V5Z 1L3 Canada
2
Department of Radiology, University of British Columbia, Vancouver, BC V6T 1Z4, Canada
*
Authors to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(8), 199; https://doi.org/10.3390/ph13080199
Received: 27 July 2020 / Revised: 11 August 2020 / Accepted: 13 August 2020 / Published: 17 August 2020
Kinins, bradykinin and kallidin are vasoactive peptides that signal through the bradykinin B1 and B2 receptors (B1R and B2R). B2R is constitutively expressed in healthy tissues and mediates responses such as vasodilation, fluid balance and retention, smooth muscle contraction, and algesia, while B1R is absent in normal tissues and is induced by tissue trauma or inflammation. B2R is activated by kinins, while B1R is activated by kinins that lack the C-terminal arginine residue. Perturbations of the kinin system have been implicated in inflammation, chronic pain, vasculopathy, neuropathy, obesity, diabetes, and cancer. In general, excess activation and signaling of the kinin system lead to a pro-inflammatory state. Depending on the disease context, agonism or antagonism of the bradykinin receptors have been considered as therapeutic options. In this review, we summarize molecular imaging agents targeting these G protein-coupled receptors, including optical and radioactive probes that have been used to interrogate B1R/B2R expression at the cellular and anatomical levels, respectively. Several of these preclinical agents, described herein, have the potential to guide therapeutic interventions for these receptors. View Full-Text
Keywords: kinins; bradykinin receptors; optical imaging; nuclear imaging; personalized medicine kinins; bradykinin receptors; optical imaging; nuclear imaging; personalized medicine
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MDPI and ACS Style

Lau, J.; Rousseau, J.; Kwon, D.; Bénard, F.; Lin, K.-S. A Systematic Review of Molecular Imaging Agents Targeting Bradykinin B1 and B2 Receptors. Pharmaceuticals 2020, 13, 199. https://doi.org/10.3390/ph13080199

AMA Style

Lau J, Rousseau J, Kwon D, Bénard F, Lin K-S. A Systematic Review of Molecular Imaging Agents Targeting Bradykinin B1 and B2 Receptors. Pharmaceuticals. 2020; 13(8):199. https://doi.org/10.3390/ph13080199

Chicago/Turabian Style

Lau, Joseph, Julie Rousseau, Daniel Kwon, François Bénard, and Kuo-Shyan Lin. 2020. "A Systematic Review of Molecular Imaging Agents Targeting Bradykinin B1 and B2 Receptors" Pharmaceuticals 13, no. 8: 199. https://doi.org/10.3390/ph13080199

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