Bradykinin B2 Receptor (B2R)

Bradykinin B2 receptor (B2R) mediates common kinin responses, including hypotension, bronchoconstriction, epithelial secretion, vascular permeability, pain, cytokine release, and eicosanoid formation^[1]. Mechanistically, bradykinin-induced B2R activation drives vasodilation in human forearm resistance vessels, and icatibant dose-dependently inhibits this B2R-mediated vascular response^[2]. In airway inflammation models, B2R blockade with icatibant reduces antigen-induced nasal hyperresponsiveness, eosinophils, eosinophil cationic protein, kinin, and IL-8 in seasonal allergic rhinitis^[3]. In hereditary angioedema, bradykinin acts as the key mediator of symptoms, and the selective B2R antagonist icatibant provides clinically significant symptom relief in acute cutaneous or abdominal attacks^[4]. Compared with B1 receptor, which is inducible after injury and inflammation, B2R represents the common kinin receptor subtype and remains central to acute bradykinin signaling^[1]^[5]. For experimental applications, icatibant is useful for testing B2R-dependent vascular leakage and inflammatory responses, although micromolar icatibant can inhibit aminopeptidase N and alter B1 or angiotensin receptor signaling^[6].

References:

[1]. Steranka LR, et al. Antagonists of B2 bradykinin receptors. FASEB J. 1989 Jul;3(9):2019-25.

[2]. Cockcroft JR, et al. Inhibition of bradykinin-induced vasodilation in human forearm vasculature by icatibant, a potent B2-receptor antagonist. Br J Clin Pharmacol. 1994 Oct;38(4):317-21.

[3]. Turner P, et al. Role of kinins in seasonal allergic rhinitis: icatibant, a bradykinin B2 receptor antagonist, abolishes the hyperresponsiveness and nasal eosinophilia induced by antigen. J Allergy Clin Immunol. 2001 Jan;107(1):105-13.

[4]. Cicardi M, et al. Icatibant, a new bradykinin-receptor antagonist, in hereditary angioedema. N Engl J Med. 2010 Aug 5;363(6):532-41.

[5]. Schanstra JP, et al. The B1-agonist [des-Arg10]-kallidin activates transcription factor NF-kappaB and induces homologous upregulation of the bradykinin B1-receptor in cultured human lung fibroblasts. J Clin Invest. 1998 May 15;101(10):2080-91.

[6]. Bawolak MT, et al. The bradykinin B2 receptor antagonist icatibant (Hoe 140) blocks aminopeptidase N at micromolar concentrations: off-target alterations of signaling mediated by the bradykinin B1 and angiotensin receptors. Eur J Pharmacol. 2006 Dec 3;551(1-3):108-11. [Content Brief]

Bradykinin B2 Receptor (B2R) Related Products (16):

By Type:	Pan (1) Selective (4)
By Effects:	Agonists (3) Antagonists (11) Modulators (2)

Cat. No.	Product Name	Effect	Purity

HY-P0206

Bradykinin	Modulator	99.98%
Bradykinin 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.

HY-17446

Icatibant	Antagonist	99.97%
Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC₅₀ and K_i of 1.07 nM and 0.798 nM respectively.

HY-108896

Icatibant acetate	Antagonist	99.87%
Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with an IC₅₀ and K_i of 1.07 nM and 0.798 nM respectively.

HY-105155

Lobradimil	Agonist	99.76%
Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (K_i: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors.

HY-121156A

Anatibant hydrochloride	Antagonist	99.44%
Anatibant (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 K_i 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.

HY-118945

FR191413	Agonist
FR191413 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.

HY-P1650

Breceptin	Antagonist
Breceptin (B 9870) is an antagonist of the bradykinin B₁/B₂ receptor (B₁/B₂R). Breceptin exhibits an irreversible antagonist effect on B₂R, inhibiting the vasodilation induced by Bradykinin (HY-P0206) in the rabbit carotid vein contraction experiment. B-9870 shows partial agonist properties in HEK 293 cells with high expression of B₂R, and can activate ERK1/2 phosphorylation, calcium ion mobilization, arachidonic acid release, and receptor internalization. Breceptin can be used in research to inhibit breast cancer and non-small cell lung cancer.

HY-P0206A

Bradykinin acetate	Modulator	99.58%
Bradykinin 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.

HY-121156

Anatibant	Antagonist
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with K_i values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases.

HY-106277

Fasitibant free base	Antagonist
Fasitibant (free base) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B₂ (BK₂) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis.

HY-P3232

B 9430	Antagonist
B 9430 is a potent bradykinin B1/B2 receptor antagonist.

HY-106277A

Fasitibant chloride hydrochloride	Antagonist
Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B₂ (BK₂) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis.

HY-100301

FR167344 free base	Antagonist
FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC₅₀ value of 65 nM and no binding affinity for the B1 receptor.

HY-101368

WIN 64338	Antagonist
WIN 64338 is a non-peptide bradykinin B2 receptor antagonist. WIN 64338 can inhibit bradykinin-evoked trigeminal nerve stimulation.

HY-123376

FR-190997	Agonist
FR-190997 is a non-peptide Bradykinin B2 receptor selective agonist, K_i value is 9.8 nM. FR-190997 is also an effective antihypertensive agent.

HY-101368A

WIN 64338 hydrochloride	Antagonist
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [³H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a K_i of 64 nM. WIN 64338 hydrochloride also can inhibits [³H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (K_i=350 nM).

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