Bradykinin receptors in GtoPdb v.2023.1

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...

Autoregulation of Bradykinin Receptors

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...

Antagonists of B2 bradykinin receptors.

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...

Kallikrein 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...

Bradykinin Ligands and Receptors Involved in Neuropathic Pain