Differences in affinities of bradykinin B2 receptor antagonists may be attributable to species
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Bradykinin (or kinin) receptors (nomenclature as agreed by the NC-IUPHAR subcommittee on Bradykinin (kinin) Receptors [76]) are activated by the endogenous peptides bradykinin (BK), [des-Arg9]bradykinin, Lys-BK (kallidin), [des-Arg10]kallidin, [Phospho-Ser6]-Bradykinin, T-kinin (Ile-Ser-BK), [Hyp3]bradykinin and Lys-[Hyp3]-bradykinin. Variation in pharmacology and activity of B1 and B2 receptor antagonists at species orthologs has been documented. icatibant (Hoe140, Firazir) is approved in North America and Europe for the treatment of acute attacks of hereditary angioedema.
Kallidin
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Bradykinin receptor
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Over 100 reduced-bond analogs of bradykinin and bradykinin antagonists were designed, synthesized, and assayed in the classic smooth muscle and blood pressure assays in a further study of the structure-activity relationships of bradykinin. Both potent BK-like agonists and antagonists of BK activity were found among the reduced-bond analogs.
Bradykinin receptor
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Bradykinin (or kinin) receptors (nomenclature as agreed by the NC-IUPHAR subcommittee on Bradykinin (kinin) Receptors [91]) are activated by the endogenous peptides bradykinin (BK), [des-Arg9]bradykinin, Lys-BK (kallidin), [des-Arg10]kallidin, [Phospho-Ser6]-Bradykinin, T-kinin (Ile-Ser-BK), [Hyp3]bradykinin and Lys-[Hyp3]-bradykinin. Variation in pharmacology and activity of B1 and B2 receptor antagonists at species orthologs has been documented. icatibant (Hoe140, Firazir) is approved in North America and Europe for the treatment of acute attacks of hereditary angioedema.
Kallidin
Icatibant
B2 receptor
Bradykinin receptor
Hereditary Angioedema
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Diabetic nephropathy is the leading cause of chronic renal failure in countries in the western world. Human polymorphism studies have suggested a nephroprotective effect that is mediated by bradykinin B2 receptors. Angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor blockers have an additive nephroprotective effect in patients with diabetes, which may be due to ACE-inhibitor-mediated increases in the levels of bradykinin. There is also evidence from studies conducted in genetically altered mice to suggest that bradykinin is nephroprotective. Finally, evidence from animal models of nephropathy indicates that some of the beneficial effects of ACE inhibitors and vasopeptidase inhibitors are due to the action of bradykinin at B2 receptors. These data establish that stimulation of bradykinin B2 receptors is a target in diabetic nephropathy, and should provide impetus for the development of non-peptide, selective bradykinin B2 agonists.
B2 receptor
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Kallidin
Bradykinin receptor
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B2 receptor
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Bradykinin (or kinin) receptors (nomenclature as agreed by the NC-IUPHAR subcommittee on Bradykinin (kinin) Receptors [92]) are activated by the endogenous peptides bradykinin (BK), [des-Arg9]bradykinin, Lys-BK (kallidin), [des-Arg10]kallidin, [Phospho-Ser6]-Bradykinin, T-kinin (Ile-Ser-BK), [Hyp3]bradykinin and Lys-[Hyp3]-bradykinin. Variation in pharmacology and activity of B1 and B2 receptor antagonists at species orthologs has been documented. icatibant (Hoe140, Firazir) is approved in North America and Europe for the treatment of acute attacks of hereditary angioedema. Inhibition of bradykinin with icatibant in COVID-19 infection is under clinical evaluation, with trial NCT05407597 expected to complete in mid 2023.
Icatibant
Kallidin
B2 receptor
Bradykinin receptor
Hereditary Angioedema
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B2 receptor
Bradykinin receptor
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