Bradykinin receptors in GtoPdb v.2023.1
نویسندگان
چکیده
Bradykinin (or kinin) receptors (nomenclature as agreed by the NC-IUPHAR subcommittee on (kinin) Receptors [92]) are activated 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 activity of B1 B2 receptor antagonists at species orthologs has been documented. icatibant (Hoe140, Firazir) is approved North America Europe for treatment acute attacks hereditary angioedema. Inhibition with COVID-19 infection under clinical evaluation, trial NCT05407597 expected to complete mid 2023.
منابع مشابه
Preparation of a Photoactivable Ligand for Bradykinin Receptors
ABSTRACT Most of physiological effects of bradykinin is due to its effect on bradykinin B2 receptors. There is no reports of preparation of a photoactivatable analogue of bradykinin reactive with sloubilized bradykinin B2 recpetors. Photoactivatable radioactive ligands are powerful tools in purification of receptors. In this study we report preparation of a photoactivatable iodinatable analo...
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As bstract. The interaction of bradykinin (BK) with its specific receptors on intact cultured human fibroblasts results in production ofprostaglandins, including prostacyclin (PG12), and accumulation of cyclic AMP. Incubation of cells with 1 ,tM BK for 5 min at 37°C led to a marked reduction (75-90%) in BK-induced PGI2 release and in total number of [3H]BK-binding sites with no change in dissoc...
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Bradykinin and its active metabolites, produced by kallikreins at their sites of action, potently elicit a variety of biological effects: hypotension, bronchoconstriction, gut and uterine contraction, epithelial secretion in airway, gut, and exocrine glands, vascular permeability, pain, connective tissue proliferation, cytokine release, and eicosanoid formation. These effects are mediated by at...
متن کاملKallikrein activates bradykinin B2 receptors in absence of kininogen.
Kallikreins cleave plasma kininogens to release the bioactive peptides bradykinin (BK) or kallidin (Lys-BK). These peptides then activate widely disseminated B2 receptors with consequences that may be either noxious or beneficial. We used cultured cells to show that kallikrein can bypass kinin release to activate BK B2 receptors directly. To exclude intermediate kinin release or kininogen uptak...
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ژورنال
عنوان ژورنال: IUPHAR/BPS guide to pharmacology CITE
سال: 2023
ISSN: ['2633-1020']
DOI: https://doi.org/10.2218/gtopdb/f10/2023.1