Bradykinin Receptor

Bradykinin receptor agonists and antagonists act on B1 and B2, two G protein-coupled kinin receptors. Kinin peptides such as bradykinin are released from kininogens by kallikreins and regulate vascular tone, permeability and pain signaling. The B2 receptor is expressed constitutively in many tissues, and the human receptor was cloned in 1992. The B1 receptor, cloned in 1994, is induced by tissue injury and inflammation and prefers des-Arg kinin metabolites. A 2005 International Union of Pharmacology (IUPHAR) review set out this classification of the kinin receptor family. Icatibant is a peptide B2 antagonist, and FR167344 free base is a nonpeptide B2 antagonist. R715 and SSR240612 block the B1 receptor, while Lys-[Des-Arg9]Bradykinin TFA acts as a B1 agonist.

10 Items

  • Lobradimil
    Cat. No.
    A59122

    Lobradimil

    Synonyms: RMP 7

    Lobradimil, a synthetic bradykinin analog, acts as a potent and selective agonist of the bradykinin B2 receptor (Ki: 0.54 nM). This compound enhances blood-brain barrier permeability, making it valuable for investigations into neuropharmacology and brain tumor research. Its unique properties facilitate studies aimed at drug delivery across the blood-brain barrier and potential therapeutic applications in CNS disorders.

    1 mg
    $360.00
    5 mg
    $900.00
    All 6 sizes
  • FR191413
    Cat. No.
    A59124

    FR191413

    FR191413 is a selective bradykinin B2 receptor agonist that activates bradykinin-mediated pathways including vasodilation and organ protection through the stimulation of prostaglandin E2 production in WI-38 cells. It competitively binds to [3H]-BK in guinea pig ileum membranes and CHO cells transfected with the human B2 receptor, exhibiting IC50 values of 20.0 nM and 2.60 nM, respectively. This compound is useful in researching cardiovascular conditions such as hypertension, myocardial hypertrophy, myocardial infarction, arrhythmias, and diabetic nephropathy.

    25 mg
    $1,275.00
    All 1 sizes
  • Lys-[Des-Arg9]Bradykinin TFA
    Cat. No.
    A59126

    Lys-[Des-Arg9]Bradykinin TFA

    Lys-[Des-Arg9]Bradykinin TFA is a selective agonist of the bradykinin B1 receptor, exhibiting high affinity with Ki values of 0.12 nM, 1.7 nM, and 0.23 nM for human, mouse, and rabbit B1 receptors, respectively. This compound demonstrates minimal inhibitory activity on B2 receptors, making it a valuable tool for studying the B1 receptor's role in inflammation and pain pathways. Its potent activity supports its use in various biological and pharmacological research applications focused on the modulation of kinin pathways.

    2 mg
    $50.00
    5 mg
    $100.00
    All 5 sizes
  • [Des-Arg9]-Bradykinin
    Cat. No.
    A59134

    [Des-Arg9]-Bradykinin

    [Des-Arg9]-Bradykinin is a potent agonist of the bradykinin (B1) receptor, exhibiting selectivity for B1 receptors over B2 receptors. This selectivity allows for targeted studies on inflammation and pain pathways where B1 receptor activation plays a crucial role. It is primarily utilized in research focused on cardiovascular and renal physiology, as well as exploring potential therapeutic interventions for pain management.

    5 mg
    $315.00
    10 mg
    $570.00
    All 4 sizes
  • L-366811
    Cat. No.
    A59145

    L-366811

    L-366811 is a bradykinin receptor agonist that stimulates phosphatidylinositol turnover and induces uterine contractions. This compound demonstrates activity in rat uterine slices, effectively promoting in vitro uterine contractions with moderate affinity for the [3H]BK binding site. L-366811 serves as a valuable tool for research in uterine physiology and related studies on bradykinin receptor signaling pathways.

    25 mg
    $2,410.00
    50 mg
    $3,100.00
    All 3 sizes
  • FR-190997
    Cat. No.
    A59146

    FR-190997

    FR-190997 is a selective agonist for the Bradykinin B2 receptor, with a Ki value of 9.8 nM. This non-peptide compound demonstrates significant biological activity as an antihypertensive agent. It is suitable for research applications focused on cardiovascular physiology and the study of bradykinin signaling pathways.

    Out of stock

    All 3 sizes
  • Lys-[Hyp3]-Bradykinin
    Cat. No.
    A59150

    Lys-[Hyp3]-Bradykinin

    Lys-[Hyp3]-Bradykinin is a potent bradykinin agonist that facilitates the activation of bradykinin receptors. This kinin, which can be isolated from human urine, is significant for studying inflammatory pathways and related biological responses. Its application extends to research in pain modulation, cardiovascular regulation, and various inflammatory conditions.

    Out of stock

    All 3 sizes
  • Methionyl-Lysyl-Bradykinin
    Cat. No.
    A59152

    Methionyl-Lysyl-Bradykinin

    Synonyms: Met-Lys-Bradykinin

    Methionyl-Lysyl-Bradykinin is a bradykinin receptor agonist that exhibits potent activity by mimicking the action of natural kinins. This peptide stimulates the bradykinin receptor, triggering various physiological responses such as vasodilation and pain perception modulation. It serves as a valuable tool in research focused on cardiovascular function, inflammation, and pain signaling pathways.

    Out of stock

    All 3 sizes
  • Bombinakinin M
    Cat. No.
    A59159

    Bombinakinin M

    Bombinakinin M is a bradykinin receptor agonist that exhibits contractile activity in the guinea pig ileum. This compound is of particular interest in studies exploring the physiological effects of bradykinin signaling pathways and gastrointestinal motility. Its ability to activate bradykinin receptors makes it a valuable tool for research in cardiovascular and inflammatory responses.

    1 mg
    $185.00
    All 1 sizes
  • [Phe8Ψ(CH-NH)Arg9]-Bradykinin
    Cat. No.
    A59162

    [Phe8Ψ(CH-NH)Arg9]-Bradykinin

    [Phe8Ψ(CH-NH)Arg9]-Bradykinin is a selective agonist of the Bradykinin receptor B2, demonstrating resistance to cleavage by protein kinase I/II. This compound exhibits significant biological activity relevant to cardiovascular research, particularly in the study of hypertension. Its ability to selectively activate the B2 receptor positions it as a valuable tool for investigating bradykinin-related pathways in various physiological and pathological contexts.

    1 mg
    $190.00
    All 1 sizes

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