- Signaling Pathways
- GPCR/G Protein
- Bradykinin Receptor
Bradykinin Receptor
Bradykinin receptors are cell surface, G protein-coupled receptor (GPCR) family members. There are two subtypes of bradykinin receptors, B1 and B2. Bradykinin receptor-mediated signal transductions play a significant role in maintaining cardiovascular homeostasis, regulating pain and inflammation. Both receptors transduce extracellular signals through the activation of G-proteins.
Bradykinin B1 receptor is expressed at a very low level in healthy tissues, but is induced under stressful conditions such as shock or inflammation, whereas the bradykinin B2 receptor is ubiquitous and is constitutively expressed. Bradykinin B2 receptor is involved in vasodilation, osmoregulation, smooth muscle contraction, and nociceptor activation. Bradykinin B1 receptor and Bradykinin B2 receptor have emerged as therapeutic targets as they are implicated in inflammatory disease, vasculopathy, neuropathy, obesity, diabetes, and cancer. B1R and B2R can hold dichotomous roles in diseases. Agonists and antagonists have been evaluated as therapeutics.
Bradykinin Receptor Isoform Specific Products
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Bradykinin Receptor Related Products (69)
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Antibodies (1)
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Bradykinin Receptor Isoform Comparison
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Bradykinin
0 ImagesBradykinin is an effective endothelium-dependent vasodilator that can lower blood pressure. Bradykinin can induce contraction of bronchial and intestinal non-vascular smooth muscle, increase vascular permeability, and participate in the mechanism of pain. -
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Icatibant
0 ImagesSynonyms: HOE 140Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively. -
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Icatibant acetate
0 ImagesSynonyms: HOE 140 acetateIcatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC50 and Ki of 1.07 nM and 0.798 nM respectively. -
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[Des-Arg9]-Bradykinin acetate
0 Images[Des-Arg9]-Bradykinin acetate is a Bradykinin B1 receptor agonist that displays selectivity for B1 over B2 receptors. -
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Lobradimil
0 ImagesSynonyms: RMP 7Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors. -
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Lys-(Des-Arg9,Leu8)-Bradykinin TFA
0 ImagesCat. No.: HY-P4676ALys-(Des-Arg9,Leu8)-Bradykinin TFA is a selective bradykinin B1 receptor (BDKRB1) antagonist. Lys-(Des-Arg9,Leu8)-Bradykinin TFA inhibits local inflammatory edema. Lys-(Des-Arg9,Leu8)-Bradykinin TFA induces the production of systemic acute-phase proteins. Lys-(Des-Arg9,Leu8)-Bradykinin TFA is applicable to research related to peptidoglycan-polysaccharide-induced acute arthritis. -
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FR191413
0 ImagesCat. No.: HY-118945CAS No.: 194928-55-7FR191413 is a selective bradykinin B2 receptor agonist that stimulates prostaglandin E2 production in WI-38 cells and activates BK B2 receptor-mediated pathways such as vasodilation and organ protection. FR191413 competitively binds to [3H]-BK in guinea pig ileum (GPI) membranes and CHO cells transfected with the human BK B2 receptor, with IC50 values of 20.0 nM and 2.60 nM, respectively. FR191413 can be used in research related to cardiovascular diseases and diabetes, including hypertension, myocardial hypertrophy, myocardial infarction, arrhythmias, and diabetic nephropathy. -
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SSR240612
0 ImagesSSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively. -
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Mergetpa
0 ImagesCat. No.: HY-W704574CAS No.: 77102-28-4Mergetpa is a reversible Arg-carboxypeptidase inhibitor with high affinity. Mergetpa reduces B1R. Mergetpa blocks the overexpression of IL-1β protein and mRNA in glucose-fed rats. Mergetpa significantly increases the expression of IL-1β protein in the renal cortex. Mergetpa is used to block the conversion of kinins and B2 receptor antagonists into metabolites lacking the C-terminal arginine. Mergetpa inhibits the time-dependent enhancement of the response of isolated rabbit aorta to bradykinin. Mergetpa preserves the chemotactic activity of full-length SDF-1α on cells. Mergetpa reverses hyperglycemia, excessive weight gain, elevated levels of oxidative stress markers and overexpression of inflammatory markers in glucose-fed rats. -
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R715
0 ImagesR715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice. -
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Bradykinin (1-7)
0 ImagesSynonyms: Bradykinin Fragment 1-7Bradykinin (1-7) is an amino-truncated Bradykinin peptide. Bradykinin (1-7) is a metabolite of Bradykinin, cleaved by endopeptidase. -
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Anatibant hydrochloride
0 ImagesSynonyms: LF 16-0687 hydrochloride; XY-2405 hydrochlorideAnatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases. -
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Lys-Bradykinin TFA
0 ImagesCat. No.: HY-103293APurity: 99.85%Synonyms: Kallidin (380-389) (human, porcine, bovine) TFALys-Bradykinin TFA is the TFA salt form of Lys-Bradykinin (HY-103293). Lys-Bradykinin TFA is a ligand for kallidin and bradykinin receptor, which can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin TFA serves as a vasodilator, which widens blood vessels and increases blood flow. Lys-Bradykinin TFA stimulates net Na+ influx, and contributes to DNA synthesis. Lys-Bradykinin TFA involves in vascular regulation, inflammation and pain sensation. -
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Lys-[Des-Arg9]Bradykinin TFA
0 ImagesLys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitory activity on B2 receptors. -
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Bradykinin acetate
0 ImagesBradykinin acetate is an effective endothelium-dependent vasodilator that can lower blood pressure. Bradykinin acetate can induce contraction of bronchial and intestinal non-vascular smooth muscle, increase vascular permeability, and participate in the mechanism of pain. -
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- Sar-[D-Phe8]-des-Arg9-Bradykinin
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Bradykinin (1-6)
0 ImagesBradykinin (1-6) is an amino-truncated Bradykinin peptide. Bradykinin (1-6) is a stable metabolite of Bradykinin, cleaved by carboxypeptidase Y (CPY). -
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[Tyr8] Bradykinin
0 Images[Tyr8] Bradykinin is a B2 kinin receptor agonist. [Tyr8] Bradykinin also stimulates ERK1/2 phosphorylation. [Tyr8] Bradykinin can be used as an internal standard. -
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Fulimetibant
0 ImagesFulimetibant is a Bradykinin receptor antagonist. -
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Lys-(Des-Arg9,Leu8)-Bradykinin
0 ImagesLys-(Des-Arg9,Leu8)-Bradykinin is a selective bradykinin B1 receptor (BDKRB1) antagonist. Lys-(Des-Arg9,Leu8)-Bradykinin inhibits local inflammatory edema. Lys-(Des-Arg9,Leu8)-Bradykinin induces the production of systemic acute-phase proteins. Lys-(Des-Arg9,Leu8)-Bradykinin is applicable to research related to peptidoglycan-polysaccharide-induced acute arthritis. -
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